Target Information
Target General Information | Top | |||||
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Target ID |
T50688
(Former ID: TTDS00077)
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Target Name |
Glycoprotein IIb/IIIa receptor (GPIIb/IIIa)
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Synonyms |
Platelet membrane glycoprotein IIb; Platelet membrane glycoprotein IIIa; GP
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Gene Name |
ITGA2B; ITGB3
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 3 Target-related Diseases | + | ||||
1 | Acquired hypermelanosis [ICD-11: ED60] | |||||
2 | Angina pectoris [ICD-11: BA40] | |||||
3 | Myocardial infarction [ICD-11: BA41-BA43] | |||||
Function |
Integrin alpha-IIb/beta-3 is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. It recognizes the sequence R-G-D in a wide array of ligands. It recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha- IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial cell surface.
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UniProt ID | ||||||
Sequence |
MARALCPLQALWLLEWVLLLLGPCAAPPAWALNLDPVQLTFYAGPNGSQFGFSLDFHKDS
HGRVAIVVGAPRTLGPSQEETGGVFLCPWRAEGGQCPSLLFDLRDETRNVGSQTLQTFKA RQGLGASVVSWSDVIVACAPWQHWNVLEKTEEAEKTPVGSCFLAQPESGRRAEYSPCRGN TLSRIYVENDFSWDKRYCEAGFSSVVTQAGELVLGAPGGYYFLGLLAQAPVADIFSSYRP GILLWHVSSQSLSFDSSNPEYFDGYWGYSVAVGEFDGDLNTTEYVVGAPTWSWTLGAVEI LDSYYQRLHRLRGEQMASYFGHSVAVTDVNGDGRHDLLVGAPLYMESRADRKLAEVGRVY LFLQPRGPHALGAPSLLLTGTQLYGRFGSAIAPLGDLDRDGYNDIAVAAPYGGPSGRGQV LVFLGQSEGLRSRPSQVLDSPFPTGSAFGFSLRGAVDIDDNGYPDLIVGAYGANQVAVYR AQPVVKASVQLLVQDSLNPAVKSCVLPQTKTPVSCFNIQMCVGATGHNIPQKLSLNAELQ LDRQKPRQGRRVLLLGSQQAGTTLNLDLGGKHSPICHTTMAFLRDEADFRDKLSPIVLSL NVSLPPTEAGMAPAVVLHGDTHVQEQTRIVLDCGEDDVCVPQLQLTASVTGSPLLVGADN VLELQMDAANEGEGAYEAELAVHLPQGAHYMRALSNVEGFERLICNQKKENETRVVLCEL GNPMKKNAQIGIAMLVSVGNLEEAGESVSFQLQIRSKNSQNPNSKIVLLDVPVRAEAQVE LRGNSFPASLVVAAEEGEREQNSLDSWGPKVEHTYELHNNGPGTVNGLHLSIHLPGQSQP SDLLYILDIQPQGGLQCFPQPPVNPLKVDWGLPIPSPSPIHPAHHKRDRRQIFLPEPEQP SRLQDPVLVSCDSAPCTVVQCDLQEMARGQRAMVTVLAFLWLPSLYQRPLDQFVLQSHAW FNVSSLPYAVPPLSLPRGEAQVWTQLLRALEERAIPIWWVLVGVLGGLLLLTILVLAMWK VGFFKRNRPPLEEDDEEGE Click to Show/Hide
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HIT2.0 ID | T95XHB |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
1 | Abciximab | Drug Info | Approved | Angina pectoris | [2], [3] | |
2 | Eptifibatide | Drug Info | Approved | Acute cardiac ischemic events | [4], [5] | |
3 | Hydroquinone | Drug Info | Approved | Melasma | [6] | |
4 | Tirofiban | Drug Info | Approved | Acute coronary syndrome | [5], [7] | |
Clinical Trial Drug(s) | [+] 6 Clinical Trial Drugs | + | ||||
1 | DMP-444 | Drug Info | Phase 3 | Coronary artery disease | [8] | |
2 | 99mTc-rBitistatin | Drug Info | Phase 1/2 | Embolism | [9] | |
3 | AjvW2 | Drug Info | Phase 1 | Thrombosis | [10] | |
4 | Lefradafiban | Drug Info | Phase 1 | Angina pectoris | [11] | |
5 | RGD-891 | Drug Info | Phase 1 | Thrombosis | [12] | |
6 | SDZ-GPI-562 | Drug Info | Phase 1 | Thrombosis | [13] | |
Discontinued Drug(s) | [+] 28 Discontinued Drugs | + | ||||
1 | LAMIFIBAN | Drug Info | Discontinued in Phase 3 | Angina pectoris | [14] | |
2 | LOTRAFIBAN | Drug Info | Discontinued in Phase 3 | Cardiovascular disease | [15] | |
3 | ORBOFIBAN | Drug Info | Discontinued in Phase 3 | Angina pectoris | [16] | |
4 | SIBRAFIBAN | Drug Info | Discontinued in Phase 3 | Angina pectoris | [17] | |
5 | XEMILOFIBAN | Drug Info | Discontinued in Phase 3 | Peripheral vascular disease | [18] | |
6 | Cromafiban | Drug Info | Discontinued in Phase 2 | Coronary artery disease | [19] | |
7 | ELAROFIBAN | Drug Info | Discontinued in Phase 2 | Thrombosis | [20] | |
8 | FK-633 | Drug Info | Discontinued in Phase 2 | Artery stenosis | [21] | |
9 | Gantofiban | Drug Info | Discontinued in Phase 2 | Arteriosclerosis | [22] | |
10 | MK-852 | Drug Info | Discontinued in Phase 2 | Thrombosis | [23] | |
11 | SR-121787 | Drug Info | Discontinued in Phase 2 | Thrombosis | [24] | |
12 | YM-337 | Drug Info | Discontinued in Phase 2 | Angiogenesis disorder | [25] | |
13 | ZD-2486 | Drug Info | Discontinued in Phase 2 | Angina pectoris | [26] | |
14 | DMP-728 | Drug Info | Discontinued in Phase 1 | Thrombosis | [27] | |
15 | FR-158999 | Drug Info | Discontinued in Phase 1 | Thrombosis | [28] | |
16 | L-734217 | Drug Info | Discontinued in Phase 1 | Thrombosis | [29] | |
17 | ME-3277 | Drug Info | Discontinued in Phase 1 | Thrombosis | [30] | |
18 | SC-52012 | Drug Info | Discontinued in Phase 1 | Thrombosis | [31] | |
19 | TAK-029 | Drug Info | Discontinued in Phase 1 | Thrombosis | [32] | |
20 | TP-9201 | Drug Info | Discontinued in Phase 1 | Thrombosis | [33] | |
21 | BIBU-251 | Drug Info | Terminated | Thrombosis | [34] | |
22 | Fradafiban | Drug Info | Terminated | Thrombosis | [35] | |
23 | GR-144053 | Drug Info | Terminated | Thrombosis | [36], [37] | |
24 | GR-233548 | Drug Info | Terminated | Thrombosis | [38] | |
25 | L-703014 | Drug Info | Terminated | Thrombosis | [39] | |
26 | SB-208651 | Drug Info | Terminated | Thrombosis | [40] | |
27 | SC-49992 | Drug Info | Terminated | Arterial thrombosis | [41] | |
28 | SKF-106760 | Drug Info | Terminated | Thrombosis | [42] | |
Mode of Action | [+] 3 Modes of Action | + | ||||
Modulator | [+] 36 Modulator drugs | + | ||||
1 | Abciximab | Drug Info | [43] | |||
2 | Eptifibatide | Drug Info | [44] | |||
3 | Tirofiban | Drug Info | [43] | |||
4 | DMP-444 | Drug Info | [45] | |||
5 | 99mTc-rBitistatin | Drug Info | [46] | |||
6 | Lefradafiban | Drug Info | [48] | |||
7 | RGD-891 | Drug Info | [12] | |||
8 | SDZ-GPI-562 | Drug Info | [49] | |||
9 | LAMIFIBAN | Drug Info | [50] | |||
10 | LOTRAFIBAN | Drug Info | [51] | |||
11 | ORBOFIBAN | Drug Info | [52] | |||
12 | SIBRAFIBAN | Drug Info | [53] | |||
13 | XEMILOFIBAN | Drug Info | [54], [55] | |||
14 | Cromafiban | Drug Info | [56] | |||
15 | ELAROFIBAN | Drug Info | [57] | |||
16 | FK-633 | Drug Info | [58] | |||
17 | Gantofiban | Drug Info | [59] | |||
18 | MK-852 | Drug Info | [56] | |||
19 | SR-121787 | Drug Info | [60], [61] | |||
20 | YM-337 | Drug Info | [62] | |||
21 | ZD-2486 | Drug Info | [56] | |||
22 | DMP-728 | Drug Info | [63] | |||
23 | L-734217 | Drug Info | [65] | |||
24 | ME-3277 | Drug Info | [66] | |||
25 | SC-52012 | Drug Info | [67] | |||
26 | TAK-029 | Drug Info | [68] | |||
27 | TP-9201 | Drug Info | [69] | |||
28 | BIBU-251 | Drug Info | [70] | |||
29 | Fradafiban | Drug Info | [71] | |||
30 | GR-144053 | Drug Info | [72], [73] | |||
31 | GR-233548 | Drug Info | [43] | |||
32 | L-703014 | Drug Info | [74] | |||
33 | SB-208651 | Drug Info | [75], [76] | |||
34 | SC-49992 | Drug Info | [77] | |||
35 | SKF-106760 | Drug Info | [43] | |||
36 | RGD-039 | Drug Info | [12], [79] | |||
Antagonist | [+] 3 Antagonist drugs | + | ||||
1 | Hydroquinone | Drug Info | [1] | |||
2 | FR-158999 | Drug Info | [6], [64] | |||
3 | XV454 | Drug Info | [80] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | RGD | Drug Info | [78] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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Reactome | [+] 12 Reactome Pathways | + | ||||
1 | Platelet degranulation | |||||
2 | Elastic fibre formation | |||||
3 | PECAM1 interactions | |||||
4 | Molecules associated with elastic fibres | |||||
5 | Integrin cell surface interactions | |||||
6 | Syndecan interactions | |||||
7 | ECM proteoglycans | |||||
8 | Integrin alphaIIb beta3 signaling | |||||
9 | GRB2:SOS provides linkage to MAPK signaling for Integrins | |||||
10 | p130Cas linkage to MAPK signaling for integrins | |||||
11 | VEGFA-VEGFR2 Pathway | |||||
12 | MAP2K and MAPK activation | |||||
WikiPathways | [+] 9 WikiPathways | + | ||||
1 | Focal Adhesion | |||||
2 | Hematopoietic Stem Cell Differentiation | |||||
3 | Human Complement System | |||||
4 | Extracellular matrix organization | |||||
5 | Arrhythmogenic Right Ventricular Cardiomyopathy | |||||
6 | Integrin-mediated Cell Adhesion | |||||
7 | L1CAM interactions | |||||
8 | Integrin cell surface interactions | |||||
9 | Integrin alphaIIb beta3 signaling |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Accutin, a new disintegrin, inhibits angiogenesis in vitro and in vivo by acting as integrin alphavbeta3 antagonist and inducing apoptosis. Blood. 1998 Nov 1;92(9):3268-76. | |||||
REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6584). | |||||
REF 3 | Advances in ischemic stroke treatment: neuroprotective and combination therapies. Expert Opin Emerg Drugs. 2007 Mar;12(1):97-112. | |||||
REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6585). | |||||
REF 5 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 6 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 7 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6586). | |||||
REF 8 | Evaluation of 99mTc-labeled cyclic RGD peptide with a PEG4 linker for thrombosis imaging: comparison with DMP444. Bioconjug Chem. 2011 Aug 17;22(8):1715-22. | |||||
REF 9 | ClinicalTrials.gov (NCT00808626) Phase II Investigation of 99mTc-rBitistatin for Imaging Venous Thrombosis. U.S. National Institutes of Health. | |||||
REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009728) | |||||
REF 11 | ClinicalTrials.gov (NCT02264106) Influence of Pantoprazole on the Pharmacokinetics of Fradafiban After Multiple Oral Doses of Lefradafiban Over 5 Days in Healthy Subjects. U.S. National Institutes ofHealth. | |||||
REF 12 | Pharmacokinetics, pharmacodynamics, and safety of a platelet GPIIb/IIIa antagonist, RGD891, following intravenous administration in healthy male volunteers. J Clin Pharmacol. 2000 Nov;40(11):1245-56. | |||||
REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005009) | |||||
REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003532) | |||||
REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004570) | |||||
REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007819) | |||||
REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006751) | |||||
REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004434) | |||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010404) | |||||
REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010575) | |||||
REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006561) | |||||
REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010688) | |||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001868) | |||||
REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009197) | |||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005765) | |||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006364) | |||||
REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003382) | |||||
REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011969) | |||||
REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006092) | |||||
REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007141) | |||||
REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003583) | |||||
REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005011) | |||||
REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001874) | |||||
REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004683) | |||||
REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005534) | |||||
REF 36 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6587). | |||||
REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004027) | |||||
REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010798) | |||||
REF 39 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004828) | |||||
REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004708) | |||||
REF 41 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001873) | |||||
REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003995) | |||||
REF 43 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 44 | Barbourin. A GPIIb-IIIa-specific integrin antagonist from the venom of Sistrurus m. barbouri. J Biol Chem. 1991 May 25;266(15):9359-62. | |||||
REF 45 | Evaluation of Tc-99m-labeled glycoprotein IIb/IIIa receptor antagonist DMP444 SPECT in patients with infective endocarditis. Clin Nucl Med. 2003 Jun;28(6):480-4. | |||||
REF 46 | Platelet binding and biodistribution of [99mTc]rBitistatin in animal species and humans. Nucl Med Biol. 2007 Oct;34(7):855-63. | |||||
REF 47 | Novel approaches to the treatment of thrombosis. Trends Pharmacol Sci. 2002 Jan;23(1):25-32. | |||||
REF 48 | Pharmacodynamics and safety of lefradafiban, an oral platelet glycoprotein IIb/IIIa receptor antagonist, in patients with stable coronary artery disease undergoing elective angioplasty. Heart. 2001 Apr;85(4):444-50. | |||||
REF 49 | Heparin-induced thrombocytopenia: the role of platelet activation and therapeutic implications. Semin Thromb Hemost. 1999;25 Suppl 1:67-75. | |||||
REF 50 | Lamifiban. Drugs. 1999 Feb;57(2):215-21; discussion 222-3. | |||||
REF 51 | Lotrafiban: an oral platelet glycoprotein IIb/IIIa blocker.Expert Opin Investig Drugs.2000 Nov;9(11):2673-87. | |||||
REF 52 | Orbofiban: an orally active GPIIb/IIIa platelet receptor antagonist. Med Res Rev. 2001 May;21(3):211-26. | |||||
REF 53 | Pharmacokinetics and pharmacodynamics of sibrafiban, an orally administered GP IIb/IIIa antagonist, following coadministration of aspirin and heparin. J Clin Pharmacol. 2000 May;40(5):488-95. | |||||
REF 54 | Glycoprotein IIb/IIIa receptor number and occupancy during chronic administration of an oral antagonist. J Pharmacol Exp Ther. 2000 Nov;295(2):670-6. | |||||
REF 55 | Acute thrombocytopenia in patients treated with the oral glycoprotein IIb/IIIa inhibitors xemilofiban and orbofiban: evidence for an immune etiology. Thromb Haemost. 2002 Dec;88(6):892-7. | |||||
REF 56 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
REF 57 | 1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists. Bioorg Med Chem Lett. 2001 Oct 8;11(19):2619-22. | |||||
REF 58 | Efficacy of FK633, an ultra-short acting glycoprotein IIb/IIIa antagonist on platelet preservation during and after cardiopulmonary bypass. Eur J Cardiothorac Surg. 2004 Aug;26(2):289-93. | |||||
REF 59 | Enantioseparation of gantofiban precursors on chiral stationary phases of the poly-(N-acryloyl amino acid derivative)-type. J Pharm Biomed Anal. 2002 Jan 15;27(3-4):627-37. | |||||
REF 60 | Prevention of thrombosis and enhancement of thrombolysis in rabbits by SR 121787, a glycoprotein II/III antagonist. J Pharmacol Exp Ther. 1998 Aug;286(2):670-5. | |||||
REF 61 | The antithrombotic efficacy of the GP IIb/IIIa antagonist SR121787 is potentiated by antithrombin-dependent factor Xa inhibition without an increas... J Cardiovasc Pharmacol. 1999 Apr;33(4):573-9. | |||||
REF 62 | Pharmacodynamic characterization of the interaction between the glycoprotein IIb/IIIa inhibitor YM337 and unfractionated heparin and aspirin in hum... Br J Clin Pharmacol. 2003 Sep;56(3):321-6. | |||||
REF 63 | Antiplatelet and antithrombotic efficacy of DMP 728, a novel platelet GPIIb/IIIa receptor antagonist. Circulation. 1994 Jan;89(1):3-12. | |||||
REF 64 | QSAR study of the peptidic fibrinogen inhibitors FK633, FR158999 and related derivatives, using a novel and useful hydrophobic descriptor (logPmw). Bioorganic & Medicinal Chemistry Letters Volume 8, Issue 18, 22 September 1998, Pages 2483-2488. | |||||
REF 65 | Nonpeptide glycoprotein IIb/IIIa inhibitors. 8. Antiplatelet activity and oral antithrombotic efficacy of L-734,217. J Pharmacol Exp Ther. 1996 Jul;278(1):62-73. | |||||
REF 66 | ME3277, a GPIIb/IIIa antagonist reduces cerebral infarction without enhancing intracranial hemorrhage in photothrombotic occlusion of rabbit middle cerebral artery. J Cereb Blood Flow Metab. 2000 Jun;20(6):988-97. | |||||
REF 67 | Characterization of Binding of an RGD Mimetic, [(3)H]-SC-52012, to Platelet GPIIb/IIIa. Platelets. 1995;6(5):288-95. | |||||
REF 68 | Platelet protective effect of TAK-029, a novel glycoprotein IIb/IIIa antagonist: an in vitro study. Artif Organs. 1998 Apr;22(4):348-52. | |||||
REF 69 | TP-9201, a glycoprotein IIb/IIIa platelet receptor antagonist, prevents rethrombosis after successful arterial thrombolysis in the dog. Stroke. 1997 Sep;28(9):1789-96. | |||||
REF 70 | CN patent application no. 101312747, Anticoagulant antithrombotic dual inhibitors comprising a biotin label. | |||||
REF 71 | Profound and sustained inhibition of platelet aggregation by Fradafiban, a nonpeptide platelet glycoprotein IIb/IIIa antagonist, and its orally active prodrug, Lefradafiban, in men. Circulation. 1997Aug 19;96(4):1130-8. | |||||
REF 72 | GR144053, a fibrinogen receptor antagonist, enhances the suppression of neointima formation by losartan, an angiotensin II receptor antagonist, in ... Br J Pharmacol. 1997 Nov;122(6):1099-104. | |||||
REF 73 | Effect of GR144053, a fibrinogen-receptor antagonist, on thrombus formation and vascular patency after thrombolysis by tPA in the injured carotid a... J Cardiovasc Pharmacol. 1998 Aug;32(2):191-7. | |||||
REF 74 | Pharmacokinetics and pharmacodynamics of L-703,014, a potent fibrinogen receptor antagonist, after intravenous and oral administration in the dog. Pharm Res. 1994 Mar;11(3):426-31. | |||||
REF 75 | Design of a potent and orally active nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Bioorg Med Chem. 1994 Sep;2(9):897-908. | |||||
REF 76 | Chemical approaches to improve the oral bioavailability of peptidergic molecules.J Pharm Pharmacol.1996 Feb;48(2):119-35. | |||||
REF 77 | SC-49992--a potent and specific inhibitor of platelet aggregation. Thromb Res. 1994 Jun 1;74(5):523-35. | |||||
REF 78 | AlphaIIbbeta3 and its antagonism at the new millennium. Thromb Haemost. 2001 Jul;86(1):34-40. | |||||
REF 79 | Pharmacokinetics and concentration-effect analysis of intravenous RGD891, a platelet GPIIb/IIIa antagonist, using mixed-effects modeling (NONMEM). J Clin Pharmacol. 2000 Oct;40(10):1129-40. | |||||
REF 80 | Inhibition of tumor cell-induced platelet aggregation and lung metastasis by the oral GpIIb/IIIa antagonist XV454. Thromb Haemost. 2003 Sep;90(3):549-54. |
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