Publications

Portola’s lead product candidates are supported by a number of research and clinical
presentations and papers.

2013   :   2012   :   2011   :   2010   :   2009   :   2008   :   2007   :   2006   :   2005   :   2004   :   2003 – 2000

2013


An J, Waitara M, Bordas M, Arumugam V, Hoffmann R, Petrich B, Sinha U, North P, Sood R
Heparin rescues factor V Leiden-associated placental failure independent of anticoagulation in a murine high-risk pregnancy model. Blood. 2013 March 14; 121(11):2127-34. Epub 2013 Jan 16.

Coffey G, Rani A, Betz A, Pak Y, Pandey A, Hollenbach S, Gretler D, Mant T, Jurcevic S, Sinha U
Single ascending dose escalation study of the specific Syk inhibitor P505-15 investigating pharmacokinetics, pharmacodynamics, and safety in healthy male volunteers. Presented at the American Society of Clinical Oncology Annual Meeting, 2013.

Connolly SJ, Eikelboom J, Dorian P, Hohnloser SH, Gretler DD, Sinha U, Ezekowitz MD
Betrixaban compared with warfarin in patients with atrial fibrillation: results of a phase 2, randomized, dose-ranging study (Explore-Xa). European Heart Journal. Epub. 2013 March 13.

Crowther M, Kitt M, Lorenz T, Mathur V,Lu G, Hutchaleelaha A, Hollenbach S, Curnutte J, Becker R
A phase 2 randomized, double-blind, placebo-controlled trial of PRT4445, a novel, universal antidote for direct and indirect Factor Xa inhibitors. Presented at the International Society on Thrombosis and Haemostasis Congress, 2013.

Lu G, DeGuzman FR, Hollenbach SJ, Karbarz MJ, Abe K, Lee G, Luan P, Hutchaleelaha A, Inagaki M, Conley PB, Phillips DR, Sinha U
A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nature Medicine. 2013 April; 19(4):446-51. Epub. 2013 March 3.

Morganroth J, Gretler DD, Hollenbach S, Lambing J, Mandema J, Sinha U
Absence of QTc prolongation with betrixaban: a randomized, double-blind, placebo- and positive-controlled thorough ECG study. Presented at the American College of Cardiology Annual Meeting, 2013.

2012


Angiolillo DJ, Welsh R, Trenk D, Neumann F-J, Conley PB, McClure MW, Stephens G, Kochman J, Jennings LK, Gurbel PA, Wojcik J, Dabrowski M, Saucedo JF, Stumpf J, Buerke M, Harrington RA, Rao S
Pharmacokinetic and pharmacodynamic effects of elinogrel: results of the platelet function substudy from the intravenous and oral administration of elinogrel to evaluate tolerability and efficacy in non-urgent PCI patients (INNOVATE-PCI) trial. Circ Cardiovasc Interv. 2012 Jun 1;5(3):347-56. Epub 2012 May 22.

Coffey G
PRT062070: a dual Syk/JAK inhibitor with potent immune regulatory capacity in rodent models of inflammation and cancer. Presented at the American Society of Hematology Annual Meeting, 2012.

Hollenbach S
PRT064445 but not recombinant FVIIa reverses rivaroxaban induced anticoagulation as measured by reduction in blood loss in a rabbit liver laceration model. Presented at the American Society of Hematology Annual Meeting, 2012.

Hollenbach S, Lu G, DeGuzman F, Curnutte J, Conley PB, Sinha U
Bolus administration of PRT064445, a recombinant Factor Xa inhibitor antidote, reverses blood loss and PD markers in a rat model following enoxaparin induced anticoagulation. Presented at the European Society of Cardiology Annual Meeting, 2012.

Hutchaleelaha A
Metabolism and disposition of betrixaban and its lack of interaction with major CYP enzymes. Presented at the American Society of Hematology Annual Meeting, 2012.

Hutchaleelaha A, Lambing JL, Romanko K, Gretler DD
Lack of pharmacokinetic interaction between a novel Factor Xa inhibitor, betrixaban, and digoxin. Presented at the Annual Meeting of the American College of Clinical Pharmacy, 2012.

Hutchaleelaha A, Lambing JL, Romanko K, Gretler DD
Effect of a proton pump inhibitor or an antacid on pharmacokinetics of betrixaban, a novel Factor Xa inhibitor. Presented at the Annual Meeting of the American College of Clinical Pharmacy, 2012.

Hutchchaleelaha A, Lu G, DeGuzman F, Karbarz M, Hollenbach S, Inagaki M, Yau S, Conley P, Sinha U
Recombinant Factor Xa antidote protein (PRT064445) mediates reversal of anticoagulation through reduction of free drug concentration: a common mechanism for direct Factor Xa inhibitors. Presented at the European Society of Cardiology Annual Meeting, 2012.

Hutchaleelaha A, Lu G, DeGuzman F, Karbarz M, Inagaki M, Yau S, Conley P, Sinha U, Hollenbach S
Recombinant factor Xa inhibitor antidote (PRT064445) mediates reversal of anticoagulation through reduction of free drug concentration: a common mechanism for direct factor Xa inhibitors. Presented at the European Society of Cardiology Annual Meeting, 2012.

Kamen L, Stephens G, Pandey A, Sinha U
A Syk-specific inhibitor is a potent modulator of innate immune cell function. Presented at the American College of Rheumatology/Association of Rheumatology Health Professionals Annual Meeting, 2012.

Köhrer S
Efficacy of PRT060318, a novel highly specific Syk inhibitor, in acute lymphoblastic leukemia. Presented at the American Society of Hematology Annual Meeting, 2012.

Lu G, DeGuzman F, Hollenbach S, Conley P, Sinha U
Bolus administration of PRT064445, a recombinant Factor Xa inhibitor antidote, reverses PD markers and blood loss in a rat model following enoxaparin administration. Presented at the European Society of Cardiology Annual Meeting, 2012.

Stephens G
Evaluation of patients with bleeding symptoms using a novel perfusion chamber assay. Presented at the American Society of Hematology Annual Meeting, 2012.

Welsh RC, Rao SV, Zeymer U, Thompson VP, Huber K, Kochman J, McClure MW, Gretler D, Bhatt DL, Gibson M, Angiolillo DJ, Gurber PA, Berdan LG, Paynter G, Leonardi S, Madan M, French WJ, Harrington RA
A randomized, double-blind, active controlled Phase 2 trial to evaluate a novel selective and reversible intravenous and oral P2Y12 inhibitor elinogrel versus clopidogrel in patients undergoing nonurgent percutaneous coronary intervention: the INNOVATE-PCI Trial. Circ Cardiovasc Interv. 2012 Jun 1;5(3):336-346. Epub 2012 May 29.

2011


Andre P, DeGuzman F, Haberstock-Debic H, Mills S, Pak Y, Inagaki M, Pandey A, Hollenbach, Phillips DR, Conley PB
Thienopyridines, but not elinogrel, result in off-target effects at the vessel wall that contribute to bleeding. Pharmacol Exp Ther 2011;338:22-30.

Andre P, Morooka T, Sim, D, Abe K, Lowell C, Nanda N, Delaney S, Siu G, Yan Y, Hollenbach S, Pandey A, Gao H, Wang Y, Parikh S, Phillips D, Owen W, Sinha U, Simon DI
Critical role for syk in responses to vascular injury. Blood. 2011; 118(18):5000-5010.

Angiolillo DJ, Rao S, Trenk D, Neumann FJ, Conley PB, Stephens G, Kochman J, Gurbel PA, Harrington RA, Welsh R
Pharmacodynamic substudy from the intravenous and oral administration of elinogrel to evaluate tolerability and efficacy in non-urgent PCI patients (INNOVATE-PCI). Presented at the European Society of Cardiology Congress 2011.

Basharat A, Turner W, Stephens G, Badillo B, Lumpkin R, Andre P, Perera A
Tracking flow of leukocytes in blood for drug analysis. Presented at the Society for Imaging Science and Technology (IS&T)/SPIE 23rd Annual Symposium on Electronic Imaging 2011.

Chen L, Chen G, Fecteau JF , Zhang L, Coffey G, Prussak C, Carson D, Kipps TJ
Highly specific inhibitor for Syk induces chronic lymphocytic leukemia cell apoptosis. Presented at the 53rd American Society of Hematology Annual Meeting and Exposition 2011.

Cheng S, Coffey G, Zhang XH, Shaknovich R, Song Z, Lu P, Pandey A, Melnick AM, Sinha U, Wang YL
Syk inhibition and response prediction in diffuse large B-cell lymphoma. Blood. October 24, 2011.

Coffey G, DeGuzman F, Inagaki M, Pak Y, Delaney SM, Ives D, Betz A, Jia ZJ, Pandey A, Baker D, Hollenbach SJ, Phillips DR, Sinha U
Specific inhibition of Syk suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. Journal of  Pharmacology and Experimental Therapeutics. October 31, 2011.

Haberstock-Debic H, Andre P, Mills S, Phillips D, Conley P
A clopidogrel-insensitive pool of P2Y12 receptors is exposed upon platelet activation and contributes to thrombus formation: Inhibition of the newly exposed P2Y12 receptors by elinogrel, a direct acting, reversible P2Y12 antagonist. Journal of Pharmacology and Experimental Therapeutics. July 5, 2011.

Hughes CE, O’Callaghan CA, Sinha U, Pandey A, Watson SP
CLEC-2 signalling is critically dependent on Syk and the hemITAM acidic sequence. Presented at the 13th UK Platelet Group Meeting 2011.

Lu G, DeGuzman F, Karbarz MJ, Hollenbach SJ, Conley PB, Hutchaleelaha A, Sinha U
Reversal of rivaroxaban mediated anticoagulation in animal models by a recombinant antidote protein (r-Antidote, PRT064445). Presented at the European Society of Cardiology Congress 2011.

Pandey A
Discovery of PRT062607: A potent and selective Syk inhibitor for the treatment of inflammatory, B cell proliferative diseases and thrombosis. Presented at the 6th Annual Drug Discovery Chemistry Conference 2011.

Reilly M, Sinha U, Andre P,Taylor SM, Pak Y, DeGuzman F, Nanda N, Pandey A, Stolla M, Bergmeier W, McKenzie S
PRT060318, a novel Syk inhibitor, prevents heparin-induced thrombocytopenia in a transgenic mouse model. Blood. 2011;117(7):2241-2246.

Stefanini L, Boulaftali Y, Ouellette T, Holinstat M, Désiré L, Leblond B, Andre P. Conley PB, Bergmeier W
Role of the CalDAG-GEFI/Rap1 signaling module in ITAM-dependentplatelet activation. Presented at the International Society on Thrombosis and Haemotasis 2011.

Stefanini L, Boulaftali Y, Ouellette TD, Holinstat M, Désiré L, Leblond B, Andre P, Conley PB, Bergmeier W
Rap1-Rac1 Circuits Potentiate Platelet Activation. Arterioscler Thromb Vasc Biol. November 10, 2011.

Wang J, Christine Y, Joe L
Development and application of a multi-pH dissolution method to facilitate rational formulation design of a model weak acid compound. Presented at the American Association of Pharmaceutical Scientists Annual Meeting 2011.

Weir S, Ratcliffe M, Mollon P, Langham S
The economic and humanistic burden of acute coronary syndrome: A systematic review. Presented at the International Society for Pharmacoeconomics and Outcomes Research 16th Annual International Meeting 2011.

2010


Andre P, DeGuzman F, Mills S, Pak Y, Inagaki M, Pandey A, Hollenbach S, Phillips DR, Conley PB
Off-target effects at the vessel wall, in addition to inhibition of P2Y12, contribute to bleeding associated with clopidogrel and prasugrel. Presented at the American Heart Association’s Arteriosclerosis, Thrombosis and Vascular Biology 2010 Scientific Sessions.

Ben Addi A, Cammarata D, Conley PB, Boeynaems J-M, Robaye B
Role of the P2Y12 receptor in the modulation of murine dendritic cell function by ADP. J Immunol. 2010:185.

Cheng S, Zhang H, Shaknovich R, Song Z, Lu P, Pandey A, Sinha U, Coffey G, Wang YL
BCR signaling to PLC gamma and AKT predict NHL sensitivity to Syk inhibition. Presented at the American Society of Investigative Pathology Annual Meeting 2010.

Coffey G, Deguzman F, Inagaki M, Pak Y, Delaney S, Betz A, Jia ZJ, Xu Q, Bauer S, Song Y, Pandey A, Baker D, Hollenbach S, Phillips DR, Sinha U
Specific inhibition of Syk suppresses leukocyte immune function and alleviates inflammation in rodent models of rheumatoid arthritis. Presented at the American Society of Hematology Annual Meeting 2010.

Conley P
The platelet P2Y12 receptor: finding the balance between inhibition of thrombosis and hemostasis. Presented at the 5th Annual Platelet Colloquium (2010).

Connolly SJ, Ezekowitz MD, Gretler DD, Gorina E, Denney WS, Lauring B, Vosatka A, Mansoor G, Sinha U
Effects of the oral Factor Xa inhibitor betrixaban on pharmacodynamic markers in EXPLORE-Xa, a Phase 2 atrial fibrillation study. Presented at the European Society of Cardiology Congress 2010.

Delaney S, Sim D, Abe K, Nanda N, Siu G, DeGuzman F, Coffey G, Yan Y, Hollenbach S, Pandey A, Phillips DR, Sinha U, Owen W, Lowell C, Andre P
Targeting Syk as a key signaling pathway of platelet-mediated thrombo-inflammatory events. Presented at The 6th International Meeting: ADP 2010.

Ezekowitz M, Diaz R, Dorian P, Hohnloser S, Cossu S, Vicari R, Teixeira J, Gorina E, Gretler D, Sinha U, Connolly SA
Randomized clinical trial of three doses of a long-acting oral Factor Xa inhibitor betrixaban, in patients with atrial fibrillation. Presented at the American College of Cardiology’s 59th Annual Scientific Session.

Gorina E, Connolly S, Diaz R, Dorian P, Ezekowitz M, Hohnloser SA
Phase 2 randomized, parallel group, dose-finding, multicenter, multinational study of the safety, tolerability and pilot efficacy of three blinded doses of the oral Factor Xa Inhibitor betrixaban compared with warfarin in AF. EXPLORE-Xa. Presented at the American College of Cardiology’s 59th Annual Scientific Session.

Höllenriegel J, Coffey G, Sinha U, Pandey A, Wierda WG, Keating MJ, Burger JA
Selective inhibitors of the spleen tyrosine kinase (Syk) block cell survival and migration in chronic lymphatic leukemia. Presented at the 15th Congress of the European Hematology Association.

Leonardi S, Rao SV, Harrington RA, Bhatt DL, Gibson M, Roe MT, Kochman J, Huber K, Zeymer U, Madan M, Gretler DD, McClure MW, Paynter GE, Thompson V, Welsh RC
Rationale and design of the randomized, double-blind trial testing Intravenous and Oral administration of elinogrel, a selective and reversible P2Y12,-receptor inhibitor vs. clopidogrel, to evaluate Tolerability and Efficacy. Am Heart J. 2010;160(1):65-72.

Lu G, DeGuzman FR, Hollenbach SJ, Luan P, Abe K, Siu G, Conley PB, Phillips DR, Sinha U
Reversal of low molecular weight heparin and fondaparinux anticoagulation by a recombinant antidote (r-antidote). Presented at the American Heart Association Scientific Sessions 2010.

Rao SV, Zeymer U, Thompson V, Huber K, Kochman J, McClure MW, Gretler DD, Bhatt DL, Gibson CM, Madan M, Berdan L, Paynter G, Leonardi S, Harrington RA, Welsh R
A Phase 2 study of the novel oral and intravenous P2Y12 inhibitor elinogrel: results of the INNOVATE-PCI randomized trial. Presented at the European Society of Cardiology Congress 2010.

Spurgeon SE, Fletcher LB, Tyner JW, Druker BJ, Pandey A. Sinha A, Loriaux MM
P505-15, a highly selective Syk inhibitor, shows significant activity in primary CLL cells and is synergistic with fludarabine at low concentrations. Presented at the American Society of Hematology Annual Meeting 2010.

Stephens G, Tauscher J, Andre P, Siegel FP, Phillips DR, Petrides PE
Sub-optimal inhibition of thrombus formation by aspirin (as measured by RTTP analysis) in primary.

2009


Andre P, Deguzman F, Mills S, Pak Y, Inagaki M, Pandey A, Phillips D, Conley P
Clopidogrel and prasugrel prolong primary hemostasis in the mouse beyond levels associated with P2Y12 inhibition. ISTH 2009.

Andre P, Inagaki M, Pak Y, Mills S, DeGuzman F, Pandey A, Hollenbach S, Phillips D, Conley P
Clopidogrel and Prasugrel prolong primary hemostasis in the mouse beyond levels associated with P2Y12 Inhibition. ISTH 2009.

Bauer S, Mehrotra M, Conley P, Jurek M, Hutchaleelaha A, Ye C, Hollenbach S, Scarborough R, Pandey A
Identification of non-sulfonylurea P2Y12 inhibitors as a follow-up series to PRT060128 (elinogrel).

ACS 2009 Abstract.

Berger JS, Roe MT, Gibson CM, Kilaru R, Green CL, Melton L, Blankenship JD, Metzger DC, Granger CB, Gretler DD, et al
Safety and feasibility of adjunctive antiplatelet therapy with intravenous elinogrel, a selective P2Y12-receptor inhibitor, before primary percutaneous intervention in patients with STelevation myocardial infarction: ERASE MI trial 2009 Am Heart J.

Conley P, Andre P, Stephens G, Haberstock-Debic H, Jurek M, Phillips D, Gretler D
ADP-Mediated Aggregation as a Pharmacodynamic Assay Underestimates the Antithrombotic Activity of Elinogrel, a Competitive, Reversible P2Y12 Inhibitor, Relative to Clopidogrel. ISTH 2009.

Conley P, Andre P, Stephens G, Haberstock-Debic H, Jurek M, Phillips D, Gretler D
ADP-mediated aggregation as a pharmacodynamic assay underestimates the antithrombotic activity of elinogrel, a competitive, reversible P2Y12 antagonist, relative to clopidogrel. ISTH 2009 Abstract.

Delaney S,Sim D, Abe K, Nanda N, Siu G, DeGuzman F, Coffey G, Yan Y, Hollenbach S, Pandey A, Phillips D, Sinha U,
Targeting Syk as a key signaling pathway of platelet-mediated thrombo-inflammatory events. Gordon Conf 2009 ppt Presentation.

Gurbel P, Bliden KP, Antonino MJ, Andre P, Stephens G, Gretler DD, Jurek MM, Hutchaleelaha A, Conley P, Tantry US
First in Patient Experience With a New, Direct Acting, Reversible P2Y12 Inhibitor, Elinogrel (PRT060128): Evaluation in Patients With High Platelet Reactivity During Clopidogrel Therapy. ESC 2009.

Gurbel PA, Bliden KP, Antonino MJ, Conley PB, Andre P, Pakyz RE, Jurek MM, Shuldiner AR, Kanda B, Gretler DD, Stephens G, Tantry US
Elinogrel, A Novel Direct-acting P2Y12 Antagonist Overcomes High Platelet Reactivity in Patients on Dual Antiplatelet Therapy Independent of CYP 2C19*2 Genotype. TCT 2009.

Gurbel PA, Bliden KP, Antonino MJ, Stephens G, Gretler DD, Jurek MM, Pakyz RE, Shuldiner AR, Conley PB, Tantry US
The effect of elinogrel on high platelet reactivity during dual antiplatelet therapy and the relation to cyp 2c19*2 genotype: first experience in patients. J Thromb Haemost. 2009 Oct 11. PMID: 19817997.

Gurbel PA, Conley PB, Andre P, Stephens G, Gretler DD, Jurek MM, Bliden KP, Antonino MJ, Singla N, Suarez T, Tantry US,
Oral Dosing of PRT060128, a Novel Direct-acting, Reversible P2Y12 Antagonist Overcomes High Platelet Reactivity in Patients Non-responsive to Clopidogrel Therapy. N* 1728 ISTH 2009.

Gurbel PA, Bliden KP, Antonino MJ, Stephens G, Gretler DD, Jurek MM, Pakyz RE, Shuldiner AR, Conley PB, Tantry US
The effect of elinogrel on high platelet reactivity during dual antiplatelet therapy and the relation to cyp 2c19*2 genotype: first experience in patients. J Thromb Haemost. 2009 Oct 11. [Epub ahead of print] PMID: 19817997.

Haberstock-Debic H, Andre P, Delaney S, Mills S, Pak Y, Phillips D, Conley P
The clopidogrel-insensitive pool of P2Y12 receptors exposed upon platelet activation contributes to thrombus formation and can be blocked by elinogrel, a direct acting, reversible P2Y12 inhibitor. ESC 2009 Abstract.

Haberstock-Debic H, Andre P, Delaney SM,, Mills S, Pak Y, Phillips,D. R. ,Conley P. B. ,
A functional pool of P2Y12 receptors exposed upon platelet activation receptors activation persists in mice treated with high dose Clopidogrel, and can be blocked by Elinogrel, a direct acting, reversible P2YBY P2Y12 12 Inhibitor. ISTH 2009.

Haberstock-Debic H; P. Andre; S. Delaney, S. Mills, Y. Pak, D. Phillips; P. Conley:
A functional pool of P2Y12 receptors exposed upon platelet activation persists in mice treated with high dose clopidogrel, and can be blocked by elinogrel, a direct acting, reversible P2Y12 inhibitor. ISTH 2009 Abstract.

Haberstock-Debic H, Andre P, Delaney SM, Mills S, Pak Y, Phillips DR, Conley PB
The clopidogrel-insensitive pool of P2Y12 receptors exposed upon platelet activation contributes to thrombus formation and can be blocked by elinogrel, a direct acting, reversible P2Y12 inhibitor. ESC 2009.

Jia, Z; Bauer, S; Song, Y; Su, T; Sinha, U; Pandey, A; Hutchaleelaha, A; Lambing, J; Hollennbach, S; Scarborough, R
Discovery of N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide (betrixaban, MLN1021, PRT54021), a highly potent, selective, efficacious, and orally bioavailable direct factor Xa inhibitor. Bioorganic Med Chem Ltt 2009 19(8):2179-2185.

Jia, Z; Scarborough, R; Sinha, U
Design, Synthesis and Discovery of 1-(2-(6-Chloro-3-methylsulfonyl)-naphthyl)-1H-pyrazole-5-carboxylamides as Highly Potent Factor Xa Inhibitors. 2009 Chem Pharm Bull 57(9):1004-1007.

Lambing, J.L., Hutchaleelaha, A., Ye, C., Romanko, K., Gretler, D.D., Pandey, A.,
Determination of absolute bioavailabibilty of Betrixaban using therapeutic oral dosing and and an IV Microdose with analysis by accelerator mass spectromtrometry. ASCPT 2009 Abstract.

Lu, Genmin, Peng Luan, Stanley J Hollenbach, Keith Abe, Francis R DeGuzman, Gail Siu, Athiwat Hutchaleelaha, Mayuko Inagaki, Pamela B Conley, David R Phillips, Uma Sinha.
Reconstructed Recombinant Factor Xa as an Antidote to Reverse Anticoagulation by Factor Xa Inhibitors. ISTH 2009 abstract/oral presentation.

Lu G, P. Luan, S. J. Hollenbach, K. Abe, F. R. DeGuzman, G. Siu, A. Hutchaleelaha, M. Inagaki, P. B. Conley, D. R. Phillips, U. Sinha
Reconstructed Recombinant Factor Xa as an Antidote to Reverse Anticoagulation by Factor Xa Inhibitors. ISTH 2009 (powerpoint).

Paruchuri S, Tashimo H, Feng C, Maekawa A, Xing W, Jiang Y, Kanaoka Y, Conley P, Boyce JA
Leukotriene E4-induced pulmonary inflammation is mediated by the P2Y12 receptor. J Exp Med. 2009 Oct 26;206(11):2543-55. Epub 2009 Oct 12.

Smyth SS, Woulfe DS, Weitz JI, Gachet C, Conley PB, Goodman SG, Roe MT, Kuliopulos A, Moliterno DJ, French PA, Steinhubl SR, Becker
G-protein-coupled receptors as signaling targets for antiplatelet therapy. Arterioscler Thromb Vasc Biol. 2009 Apr;29(4):449-57. Epub 2008 Nov 20.

Smyth SS, Woulfe DS, Weitz JI, Gachet C, Conley PB, Goodman SG, Roe MT, Kuliopulos A, Moliterno DJ, French PA, Steinhubl SR, Becker RC; 2008 Platelet Colloquium Participants
G-protein-coupled receptors as signaling targets for antiplatelet therapy. Arterioscler Thromb Vasc Biol. 2009 Apr;29(4):449-57. Epub 2008 Nov 20. Review. PMID: 19023091.

Turpie AGG, Bauer KA, Davidson BL, Fisher WD, Gent M, Huo MH, Sinha U, Gretler DD
A randomized Phase II evaluation of the oral factor Xa inhibitor betrixaban (PRT054021) against enoxaparin for the prevention of venous thromboembolic events after total knee replacement: the EXPERT trial. Thromb Haemost. 2009 Jan;101(1):68-76.

Zhang P, Bao L, Fan J, Jia ZJ, Sinha U, Wong PW, Park G, Hutchaleelaha A, Scarborough RM, Zhu BY,
Anthranilamide-based N,N-dialkylated benzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR. Bioorganic Med Chem Lett 2009 19(8): 2186-2189.

2008


Andre P, Conley P, Deguzman F, Pak Y, Inagaki M, Sinha U, Phillips DR
Combination of direct acting FXa inhibitor and P2Y12 antagonist at non-effective doses provides significant inhibition of arterial thrombosis. AHA 2008 Poster.

Andre P, Conley P, Deguzman F, Pak Y, Inagaki M, Sinha U, Phillips DR
Combination of direct acting FXa inhibitor and P2Y12 antagonist at non-effective doses provides significant inhibition of arterial thrombosis. AHA 2008 abstract.

Andre, Patrick, Pamela B. Conley, Francis Deguzman, Yvonne Pak, Mayuko Inagaki, Uma Sinha, David R. Phillips
Combination of non-effective doses of direct acting FXa inhibitor and P2Y12 antagonist provides significant inhibition of arterial thrombosis in vivo. AHA 2008 Abstract.

Coffey G, Luan P, Delaney S, Pandey A, Jia Z.J., Xu Q, Bauer S,Song Y, Conley P, Phillips D, Sinha U
Specific Inhibition of Syk is Sufficient to Disrupt Proliferation and Survival of Non-Hodgkin’s Lymphoma Cell Lines Without Concomitant Inhibition of JAK. ASH 2008 Abstract.

Coffey G, Luan P, Delaney S, Pandey A, Jia ZJ, Xu Q, Bauer S, Song Y, Conley P, Phillips D, Sinha U
Specific Inhibition of the Spleen Tyrosine Kinase is Sufficient to Disrupt Proliferation and Survival of Non-Hodgkin’s Lymphoma Cell Lines. ASH 2008 Abstract.

Deguzman, Francis, Patrick Andre, Yvonne Pak, Mayuko Inagaki, David R. Phillips, Stan Hollenbach, Pamela B. Conley
Clopidogrel and prasugrel impact primary hemostasis in the mouse beyond levels associated with P2Y12 gene-deficiency. AHA 2008 Abstract.

Delaney S, Sinha U, Nanda N, Yan Y, Pandey A, Hollenbach S, Owen W, Phillips D, Andre P
Specific Pharmacological Targeting of Syk Kinase Activity in Platelets: A Novel, Safe Anti-Thrombotic Strategy. ASH 2008 abstract.

Delaney S, Sinha U, Pandey A, Hollenbach S, Phillips D, Andre, P, Nanda N, Owen W
Specific Pharmacological Targeting of Syk Kinase Activity in Platelets: A Novel, Safe Anti-Thrombotic Strategy. ASH 2008 Abstract.

Gurbel PA, Conley PB, Andre P, Stephens G, Gretler DD, Jurek MM, Bliden KP, Antonino MJ, Singla A, Suarez T, Tantry US
Oral Dosing of PRT060128, a Novel Direct-acting, Reversible P2Y12 Antagonist Overcomes High Platelet Reactivity in Patients Non-responsive to Clopidogrel Therapy. AHA 2008 Abstract.

Hollenbach S, Coffey G, Deguzman F , Inagaki M, Pandey A, Jia ZJ, Xu Q, Bauer S, Baker D, Nanda N, Phillips D, Sinha U
Inhibition of syk activity is sufficient for inhibitory effect in animal models of autoimmune diseases. ASH 2008 Presentation.

Hollenbach, Stan, Greg Coffey, Francis DeGuzman, Mayuko Inagaki, Anjali Pandey, Zhaozhong J Jia, Qing Xu, Shawn Bauer, Dale Baker, Nisha Nanda, David Phillips, Uma Sinha
Inhibition of Syk kinase activity is sufficient for inhibitory effect in animal models of autoimmune diseases. ASH 2008 Abstract.

Hutchaleelaha A, Ye C, Lambing J, Pandey A, Romanko, K, Liu HD, Gretler D
Metabolism and Excretion of PRT060128, a New Competitive, Reversible P2Y12 Inhibitor in Healthy Human Subjects. AAPS 2008 poster.

Hutchaleelaha A, Ye C, Lambing J, Pandey A, Romanko, K, Liu HD, Gretler D, Desai M
Metabolism and Excretion of PRT060128, a New Direct-acting, Reversible P2Y12 Inhibitor in Healthy Volunteer. AAPS 2008 Asbtract.

Hutchaleelaha A, Ye C, Pak Y, Pandey A, Lambing J
Tissue Distribution, Metabolism and Mass Balance of PRT060128, a New Direct-Acting, Reversible P2Y12 Inhibitor, in Preclinical Species. ISSX 2008 poster.

Hutchaleelaha, Athiwat , Christine Ye, Yvonne Pak, Anjali Pandey, Tod G Wehrman, Ronghua Wang, Mohammad Bashir, Joe Lambing
Tissue Distribution, Metabolism and Mass Balance of PRT060128, a New Direct-Acting, Reversible P2Y12 Inhibitor, in Preclinical Species. ISSX 2008 abstract.

Lambing, Joe, Athiwat Hutcheelaha, Christine Ye, Kevin Romanko, Dan Gretler
Determination of Absolute Bioavailability of Betrixaban using Therapeutic Oral Dosing and an IV Microdose with Analysis by Accelerator Mass Spectrometry. APA 2008 Abstract.

Lambing, Joe, Athiwat Hutcheelaha, Christine Ye, Kevin Romanko, Dan Gretler
Determination of Absolute Bioavailability of Betrixaban using Therapeutic Oral Dosing and an IV Microdose with Analysis by Accelerator Mass Spectrometry. APA 2008 Abstract.

Lu, Genmin, Francis R DeGuzman, Sanjay Lakhotia, Stanley J Hollenbach, David R Phillips, Uma Sinha
Recombinant Antidote for Reversal of Anticoagulation by Factor Xa Inhibitors. ASH 2008 Poster.

Lu, Genmin, Francis R Deguzman, Stanley J Hollenbach, David R Phillips, Uma Sinha
Recombinant Antidote for Reversal of Anticoagulation by Factor Xa Inhibitors. ASH 2008 Abstract.

Patrick Andre, Pamela B. Conley, Francis Deguzman, Yvonne Pak, Mayuko Inagaki, Uma Sinha, David R. Phillips.
Combination of direct acting FXa inhibitor and P2Y12 antagonist at non-effective doses provides significant inhibition of arterial thrombosis. AHA 2008 Poster.

Patrick Andre, Pamela B. Conley, Francis Deguzman, Yvonne Pak, Mayuko Inagaki, Uma Sinha, David R. Phillips.
Combination of direct acting FXa inhibitor and P2Y12 antagonist at non-effective doses provides significant inhibition of arterial thrombosis. AHA 2008 poster.

Ramani, C., Wang, J.,Kane, A., 1, Chow, K., Lambing, J.
Development of controlled release tablet formulations using hydrophillic polymer matrix systems. AAPS 2008 Abstract.

Reilly M, Sinha U, Pak Y, DeGuzman F, Nanda N, Pandey A, McKenzie S,
PRT060318, a novel Syk inhibitor, prevents heparin-induced thrombocytopenia in a transgenic mouse model. ASH 2008 Abstract.

Sinha U, Edwards ST, Wong PW, Delaney SM, Nanda N, Marzec UM, Pak Y, Hollenbach SJ, Hanson SR, Scarborough RM
Development of a new bioassay for predicting in vivo antithrombotic efficacy of direct factor Xa

inhibitors. ASH 2008 Abstract.

Suzanne Delaney, Uma Sinha, Nisha Nanda, Yibing Yan, Anjali Pandey, Stan Hollenbach, David Phillips and Patrick Andre
Specific Pharmacological Targeting of Syk Kinase Activity in Platelets: A Novel, Safe Anti-Thrombotic Strategy. ASH 2008 Presentation.

Wang J, Joe Lambing, Chandir Ramani, Anil Kane, Kwok Chow
Development of controlled release tablet formulations using hydrophillic polymer matrix systems. AAPS 2008 Poster.

Ye Y, Nieder M

On-Column Hydrolysis of a Sulfonylurea New Chemical Entity: Potential for Analytical Artifacts. ACS 2008 Abstract.

2007


Andre P, M Jurek, D Sim, F Deguzman, S Hollenbach, D.R. Phillips, P.B. Conley
PRT060128, a novel, direct-acting P2Y12 antagonist, confers superior antithrombotic activity over clopidogrel in a mouse thrombosis model. 2007 ISTH 2007 Abstract.

Gretler DD, Conley PB, Andre P, Jurek M, Pandey A, Romanko K, Leese PT, Hutchaleelaha A, Phillips DR
First In Human Experience With PRT060128, A New Direct-acting, Reversible, P2Y12 Inhibitor For IV And Oral Use. 2007 ACC 2007 Abstract.

Lieu HD, Conley PB, Andre P, Leese PT, Romanko K, Phillips DR, Jurek M, Meloni A, Hutchaleelaha A, Gretler DD
Initial intravenous experience with PRT060128 (PRT128), an orally available, direct-acting, and reversible P2Y12 Inhibitor. 2007 ISTH 2007 poster.

Lu G, Deguzman FR, Hollenbach SJ, Phillips DR, Sinha U
Antidote for Reversal of Anticoagulation by Factor Xa Inhibitors. 2007 ASH abstract.

Sim D, Conley PB, He M, Jurek M, Stephens G, Phillips DR, Finn AV, Gold HK, Andre P
Measurement of Thrombus stability predicts coronary events postpercutaneous coronary intervention (PCI). 2007 ISTH 2007 Poster.

Sim D, Sinha U, Mann KG, Phillips DR, Andre P
Antagonism of intrinsic pathway inhibits tissue factor (TF)-Initiated coagulation in a platelet dependent whole body flow assay. 2007 ISTH 2007 Poster.

Stephens G, Gao D, Phillips DR, Andre P
Differential effects of anti-platelet drugs on Thrombus formation and Thrombus stability. 2007 ISTH 2007 Abstract.

Stephens G, Gao D, Phillips DR, Andre P
Real time thrombosis profiler: a novel assay to measure differential effects of anti-platelet drugs on thrombus initiation, propagation and stability. 2007 ESC 2007 poster.

Turpie AGG, Gent M, Bauer K, Davidson BL, Fisher WD, Huo M, Borrow K, Frame VB, Michalsky C, Gretler DD, Romanko K, Sinha U
Evaluation of the Factor Xa (fXa) Inhibitor, PRT054021 (PRT021), against Enoxaparin in a Randomised Trial for the Prevention of Venous Thromboembolic Events after Total Knee Replacement (EXPERT). 2007 ISTH 2007 Poster.

Wang J, Nieder M, Zhou Y, et al
Optimization of a lyophilization cycle to eliminate mannitol-related vial breakage. 2007 AAPS 2007 Poster.

Ye Y, Ye C, Nieder M
HPLC Method Development for a New Oral Factor Xa Inhibitor, A Potential Chronic Anticoagulant. 2007 ACS 2007 poster.

2006


Abe K, Siu G, Edwards ST, Lin PH, Zhu BY, Marzec UM, Hanson SR, Pak Y, Hollenbach S, Sinha U
Antithrombotic potency of an oral direct factor Xa inhibitor PRT54021. 2006 ASH Abstract.

Abe K, Siu G, Pak Y, Hollenbach S
Utilization of Telemetrized Dogs to Assess Hemodynamic Changes in a Drug Interaction Study

with Verapamil and PRT054021. 2006 Poster Presentation, Safety Pharmacology Society Mtg, 9/24/06.

Abe K, Siu G, Pak Y, Hollenbach S, Sinha U
Animal Models of Thrombosis Help Predict the Human Therapeutic Concentration of PRT054021, a Potent Oral Factor Xa Inhibitor. 2006 ASH 2006 Poster.

Andre P, Luedemann H-C, He M, Golnaz S, Munnelly K, Muir C, Phillips DR
Modeling the kinetics of arterial thrombosis. 2006 Biomedical Engineering Society abstract 9/29-10/1/06.

Conley P. , Jurek M., Stephens G. , He M. , Finn A., Gold H., Romanko K., Gretler D., Phillips D., Andre P.
A novel pharmacodynamic perfusion chamber assay reveals superior and unique antithrombotic activities of a direct-acting P2Y12 antagonist, PRT128, relative to clopidogrel. 2006 ASH 2006 Abstract.

Delaney S, Arfsten A, Halfon S, Siu G, Malinowski J, Zhang P, Bauer S, Jia Z, Zhu BY, Park
G, Hollenbach S, Sinha U
Inhibition of prothrombinase and not soluble factor Xa (fXa) predicts efficacy of fXa inhibitors in an in vivo model of deep vein thrombosis. 2006 ASH 2006 Abstract.

Delaney S, Arfsten A, Halfon S, Siu G, Malinowski J, Zhang P, Bauer S, Jia Z, Zhu B-Y, Park
G, Hollenbach S, Sinha U.
Inhibition of prothrombinase and not soluble factor Xa (fXa) predicts efficacy of fXa inhibitors in an in vivo model of deep vein thrombosis. 2006 ASH 2006 Poster Presentation.

Nanda N, Phillips DR
Novel targets for antithrombotic drug discovery. 2006 Blood Cells Mol Dis. 2006 Mar-Apr;36(2):228-31. Epub 2006 Feb 13.

Nurden AT, Phillips DR, George JN.
Platelet membrane glycoproteins: historical perspectives. 2006 J Thromb Haemost. 2006 Jan;4(1):3-9.

Sinha U, Delaney SM, Nanda N, Pak Y, Hollenbach SJ, Scarborough RM
Antithrombotic activity of PRT54021, a potent oral direct factor Xa inhibitor, can be monitored using a novel prothrombinase inhibition bioassay. 2006 ASH 2006 Poster Presentation.

Stephens G, Phillips DR, Andre P
Endogenous platelet mediators of thrombus stability. 2006 ATVB 2006 Abstract.

Zhu BY, Jia ZJ, Zhang P, Su T, Huang W, Goldman E, Tumas D, Kadambi V, Eddy P, Sinha U, Scarborough RM, Song Y.
Inhibitory effect of carboxylic acid group on hERG binding. 2006 Bioorg Med Chem Lett. 2006 Nov 1;16(21):5507-12. Epub 2006 Aug 22.

2005


Hardy AR, Conley PB, Luo J, Benovic JL, Poole AW, Mundell SJ
P2Y1 and P2Y12 receptors for ADP desensitize by distinct kinase-dependent mechanisms. 2005 Blood. 2005 May 1;105(9):3552-60. Epub 2005 Jan 21.

Hezi-Yamit A, Wong PW, Bien-Ly N, Komuves LG, Prasad KS, Phillips DR, Sinha U
Synergistic induction of tissue factor by coagulation factor Xa and TNF: evidence for involvement of negative regulatory signaling cascades. 2005 Proc Natl Acad Sci U S A. 2005 Aug 23;102(34):12077-82. Epub 2005 Aug 16.

Nanda N, Andre P, Bao M, Clauser K, Deguzman F, Howie D, Conley PB, Terhorst C, Phillips DR
Platelet aggregation induces platelet aggregate stability via SLAM family receptor signaling. 2005 Blood. 2005 Nov 1;106(9):3028-34. Epub 2005 Jul 21.

Nanda N, Bao M, Lin H, Clauser K, Komuves L, Quertermous T, Conley PB, Phillips DR, Hart MJ
Platelet endothelial aggregation receptor 1 (PEAR1), a novel epidermal growth factor repeatcontaining 
transmembrane receptor, participates in platelet contact-induced activation. 2005 J Biol Chem. 2005 Jul 1;280(26):24680-9. Epub 2005 Apr 25.

Phillips D, Conley P, Sinha U et al
Therapeutic approaches in arterial thrombosis. 2005 J Thromb Haemost; 2005 3: 1577-89.

Stephens G, Jurek M, He M, Deguzman F, Escobar E, Phillips DR, Conley PB, Andre P
Role of platelets in restenosis studied by examining the effect of P2Y12 genetic targeting on intimal hyperplasia following vascular injury. 2005 AHA 05 abstract.

Stephens G, Yan Y, Jandrot-Perrus M, Villeval JL, Clemetson KJ, Phillips DR
Platelet activation induces metalloproteinase-dependent GP VI cleavage to down-regulate platelet reactivity to collagen. Blood. 2005 Jan 1;105(1):186-91. Epub 2004 Aug 31.

Wang Y, Sakuma M, Chen Z, Ustinov V, Shi C, Croce K, Zago AC, Lopez J, Andre P, Plow E, Simon DI
Leukocyte engagement of platelet glycoprotein Ibalpha via the integrin Mac-1 is critical for the biological response to vascular injury. 2005 Circulation. 2005 Nov 8;112(19):2993-3000. Epub 2005 Oct 31.

Yan Y, Phillips DR
Aspirin response and failure in diabetic patients with cardiovascular disease. 2005 Curr Opin Pharmacol. 2005 Apr;5(2):190-7. Review.

2004


Andre P.
P-selectin in haemostasis. 2004 Br J Haematol. 2004 Aug;126(3):298-306. Review.

Bauer SM, Goldman EA, Huang W, Su T, Wang L, Woolfrey J, Wu Y, Zuckett JF, Arfsten A, Huang B, Kothule J, Lin J, May B, Sinha U, Wong PW, Hutchaleelaha A, Scarborough RM, Zhu BY
Parallel synthesis and structure-activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors. 2004 Bioorg Med Chem Lett. 2004 Aug 2;14(15):4045-50.

Heath JA, Mehrotra MM, Chi S, Yu J-C, Hutchaleelaha A, Hollenbach SJ, Giese NA, Scarborough RM, Pandey A
Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor. Bioorg Med Chem Letters 14 (2004) 4867-4872.

Iwatsubo K, Minamisawa S, Tsunematsu T, Nakagome M, Toya Y, Tomlinson JE, Umemura S, Scarborough RM, Levy DE, Ishikawa Y.
Direct inhibition of type 5 adenylyl cyclase prevents myocardial apoptosis without functional deterioration.

2004 J Biol Chem. 2004 Sep 24;279(39):40938-45. Epub 2004 Jul 15.

Jia ZJ, Su T, Zuckett JF, Wu Y, Goldman EA, Li W, Zhang P, Clizbe LA, Song Y, Bauer SM, Huang W, Woolfrey J, Sinha U, Arfsten AE, Hutchaleelaha A, Hollenbach SJ, Lambing JL, Scarborough RM, Zhu BY
N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors. 2004 Bioorg Med Chem Lett. 2004 May 3;14(9):2073-8.

Jia ZJ, Wu Y, Huang W, Zhang P, Clizbe LA, Goldman EA, Sinha U, Arfsten AE, Edwards ST, Alphonso M, Hutchaleelaha A, Scarborough RM, Zhu BY
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.

2004 Bioorg Med Chem Lett. 2004 Mar 8;14(5):1221-7.

Jia ZJ, Wu Y, Huang W, Zhang P, Song Y, Woolfrey J, Sinha U, Arfsten AE, Edwards ST, Hutchaleelaha A, Hollennbach SJ, Lambing JL, Scarborough RM, Zhu BY
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors. 2004 Bioorg Med Chem Lett. 2004 Mar 8;14(5):1229-34.

Welt FG, Rogers SD, Zhang X, Ehlers R, Chen Z, Nannizzi-Alaimo L, Phillips DR, Simon DI
GPIIb-IIIa inhibition with eptifibatide lowers levels of soluble CD40L and RANTES after percutaneous cornonary intervention. 2004 Catheter Cardiovasc Interv 2004 61:185-9.

Zhang P, Bao L, Zuckett JF, Goldman EA, Jia ZJ, Arfsten A, Edwards S, Sinha U, Hutchaleelaha A, Park G, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs. 2004 Bioorg Med Chem Lett. 2004 Feb 23;14(4):983-7.

Zhang P, Bao L, Zuckett JF, Jia ZJ, Woolfrey J, Arfsten A, Edwards S, Sinha U, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity. 2004 Bioorg Med Chem Lett. 2004 Feb 23;14(4):989-93.

2003


Andre P, Delaney SM, LaRocca T, Vincent D, DeGuzman F, Jurek M, Koller B, Phillips DR, Conley PB
P2Y12 regulates platelet adhesion/activation, thrombus growth, and thrombus stability in injured arteries. 2003 J Clin. Invest. 112:398-406 (2003).

Andre P, Delaney SM, LaRocca T, Vincent D, DeGuzman F, Jurek M, Koller B, Phillips DR, Conley PB
P2Y12 regulates platelet adhesion/activation, thrombus growth, and thrombus stability in injured arteries. 2003 J Clin. Invest. 2003 112:398-406.

Andre P, LaRocca T, Delaney SM, Lin PH, Vincent D, Sinha U, Conley PB, Phillips DR
Anticoagulants (Thrombin Inhibitors) and Aspirin Synergize With P2Y12 Receptor Antagonism in Thrombosis

2003 Circulation. 2003. 108:2697-2703.

Cattaneo M, Zighetti ML, Lombardi R, Marinex C, Lecchi A, Conley P, Ware J, Ruggeri ZM
Molecular bases of defective signal transduction in the platelet P2Y12 receptor of a patient with congenital bleeding 2003 PNAS 2003;100(4);1978.

Conley PB, Delaney SM
Scientific and therapeutic insights into the role of the platelet P2Y12 receptor in thrombosis. 2003 Curr Opin Hematol. 2003 Sep;10(5):333-8. Review.

Delaney S, Jurek M, Manganello J, Vincent D, Conley P
The platelet ADP receptor P2Y12 is a critical player on the pathway of alpha-Iib-beta-3 activation by multiple agonists. 2003 ISTH 2003 Abstract.

Huang W, Naughton MA, Yang H, Su T, Dam S, Wong PW, Arfsten A, Edwards S, Sinha U, Hollenbach S, Scarborough RM, Zhu BY
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors. 2003 Bioorg Med Chem Lett. 2003 Feb 24;13(4):723-8.

Huang W, Zhang P, Zuckett JF, Wang L, Woolfrey J, Song Y, Jia ZJ, Clizbe LA, Su T, Tran K, Huang B, Wong P, Sinha U, Park G, Reed A, Malinowski J, Hollenbach SJ, Scarborough RM, Zhu BY
Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors. 2003 Bioorg Med Chem Lett. 2003 Feb 10;13(3):561-6.

Nannizzi-Alaimo L, Alves VL, Phillips DR
Inhibitory effects of Glycoprotein Iib/IIIa antagonits and aspirin on the release of soluble CD40 ligand during platelet stimulation. 2003 Circ 2003 107:1123-1128.

Scarborough RM
Protease-activated receptor-2 antagonists and agonists. 2003 Curr Med Chem Cardiovasc Hematol Agents. 2003 Mar;1(1):73-82. Review.

Sinha U, Lin PH, Edwards ST, Wong PW, Zhu B, Scarborough RM, Su T, Jia ZJ, Song Y, Zhang P, Clizbe L, Park G, Reed A, Hollenbach SJ, Malinowski J, Arfsten AE
Inhibition of purified factor Xa amidolytic activity may not be predictive of inhibition of in vivo thrombosis: implications for identification of therapeutically active inhibitors. 2003 Arterioscler Thromb Vasc Biol. 2003 Jun 1;23(6):1098-104. Epub 2003 May 15.

Song Y, Clizbe L, Bhakta C, Teng W, Wong P, Huang B, Tran K, Sinha U, Park G, Reed A, Scarborough RM, Zhu BY
Design and synthesis of factor Xa inhibitors and their prodrugs. 2003 Bioorg Med Chem Lett. 2003 Jan 20;13(2):297-300.

Su T, Yang H, Volkots D, Woolfrey J, Dam S, Wong P, Sinha U, Scarborough RM, Zhu BY
Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors. 2003 Bioorg Med Chem Lett. 2003 Feb 24;13(4):729-32.

2002


Larson MK, Chen H, Kahn ML, Taylor AM, Fabre JE, Mortensen RM, Conley PB, Parise LV
Identification of P2Y12-dependent and -independent mechanisms of glycoprotein VI-mediated Rap1 activation in platelets. 2002 Blood. 2003 Feb 15;101(4):1409-15. Epub 2002 Oct 17.

Nannizzi-Alaimo L, Rubenstein MH, Alves VL, Leong GY, Phillips DR, Gold HK
Cardiopulmonary bypass induces the release of soluble CD40L. 2002 Circ 2002 105:2849-2854.

2001


Scarborough RM, Laibelman AM, Clizbe LA, Fretto LJ, Conley PB, Reynolds EE, Sedlock DM, Jantzen H.
Novel tricyclic benzothiazolo[2,3-c]thiadiazine antagonists of the platelet ADP receptor (P2Y(12)). 2001 Bioorg Med Chem Lett. 2001 Jul 23;11(14):1805-8.

Su T, Wu Y, Doughan B, Kane-Maguire K, Marlowe CK, Kanter JP, Woolfrey J, Huang B, Wong P, Sinha U, Park G, Malinowski J, Hollenbach S, Scarborough RM, Zhu BY
Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors. 2001 Bioorg Med Chem Lett 2001 Sep3;11(17):2279-82.

2000


Sinha U, Ku P, Malinowski J, Zhu BY, Scarborough RM, Marlowe CK, Wong PW, Lin PH, Hollenbach SJ
Antithrombotic and hemostatic capacity of factor Xa versus thrombin inhibitors in models of venous and arteriovenous thrombosis. 2000 Eur J Pharmacol 395 2000.51-59.