Target Information
Target General Infomation | |||||
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Target ID |
T10965
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Former ID |
TTDC00197
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Target Name |
P-selectin
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Gene Name |
SELP
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Synonyms |
CD62P; GMP-140; Granule membrane protein 140; LECAM3; Leukocyte-endothelial cell adhesion molecule 3; PADGEM; SELP
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Target Type |
Clinical Trial
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Disease | Asthma [ICD10: J45] | ||||
Allergy [ICD9: 995.3; ICD10: T78.4] | |||||
Atherosclerosis; Thrombosis [ICD9:414.0, 440, 437.6, 453, 671.5, 671.9; ICD10: I70, I80-I82] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Delayed graft function; Heart transplantation [ICD9: 996; ICD10: T86] | |||||
Hypertension [ICD9: 401; ICD10: I10-I16] | |||||
Vaso-occlusive crisis [ICD9: 282.62; ICD10: D57.00] | |||||
Function |
Ca(2+)-dependent receptor for myeloid cells that binds to carbohydrates on neutrophils and monocytes. Mediates the interaction of activated endothelial cells or platelets with leukocytes. The ligand recognized is sialyl-Lewis X. Mediates rapid rolling of leukocyte rolling over vascular surfaces during the initial steps in inflammation through interaction with PSGL1.
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BioChemical Class |
Selectin/LECAM
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Target Validation |
T10965
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UniProt ID | |||||
Sequence |
MANCQIAILYQRFQRVVFGISQLLCFSALISELTNQKEVAAWTYHYSTKAYSWNISRKYC
QNRYTDLVAIQNKNEIDYLNKVLPYYSSYYWIGIRKNNKTWTWVGTKKALTNEAENWADN EPNNKRNNEDCVEIYIKSPSAPGKWNDEHCLKKKHALCYTASCQDMSCSKQGECLETIGN YTCSCYPGFYGPECEYVRECGELELPQHVLMNCSHPLGNFSFNSQCSFHCTDGYQVNGPS KLECLASGIWTNKPPQCLAAQCPPLKIPERGNMTCLHSAKAFQHQSSCSFSCEEGFALVG PEVVQCTASGVWTAPAPVCKAVQCQHLEAPSEGTMDCVHPLTAFAYGSSCKFECQPGYRV RGLDMLRCIDSGHWSAPLPTCEAISCEPLESPVHGSMDCSPSLRAFQYDTNCSFRCAEGF MLRGADIVRCDNLGQWTAPAPVCQALQCQDLPVPNEARVNCSHPFGAFRYQSVCSFTCNE GLLLVGASVLQCLATGNWNSVPPECQAIPCTPLLSPQNGTMTCVQPLGSSSYKSTCQFIC DEGYSLSGPERLDCTRSGRWTDSPPMCEAIKCPELFAPEQGSLDCSDTRGEFNVGSTCHF SCDNGFKLEGPNNVECTTSGRWSATPPTCKGIASLPTPGLQCPALTTPGQGTMYCRHHPG TFGFNTTCYFGCNAGFTLIGDSTLSCRPSGQWTAVTPACRAVKCSELHVNKPIAMNCSNL WGNFSYGSICSFHCLEGQLLNGSAQTACQENGHWSTTVPTCQAGPLTIQEALTYFGGAVA STIGLIMGGTLLALLRKRFRQKDDGKCPLNPHSHLGTYGVFTNAAFDPSP |
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Structure |
1ESL; 1G1T; 1KJA; 4C16; 4CSY; 1FSB; 1G1Q; 1G1R; 1G1S; 1HES; 1KJD
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Drugs and Mode of Action | |||||
Drug(s) | GMI-1070 | Drug Info | Phase 3 | Asthma | [530945], [531721], [543059] |
CY-1503 | Drug Info | Phase 2/3 | Hypertension | [521727] | |
RPSGL-Ig | Drug Info | Phase 2 | Delayed graft function; Heart transplantation | [537129] | |
PSI-697 | Drug Info | Phase 1 | Atherosclerosis; Thrombosis | [521877] | |
SelG1 | Drug Info | Phase 1 | Vaso-occlusive crisis | [551678] | |
CDP-850 | Drug Info | Discontinued in Phase 2 | Cancer | [546284] | |
CY-1787 | Drug Info | Discontinued in Phase 1 | Allergy | [545569] | |
SMART anti-E/P selectin | Drug Info | Discontinued in Phase 1 | Asthma | [546436] | |
PURPUROGALLIN | Drug Info | Terminated | Discovery agent | [546235] | |
Inhibitor | 1na | Drug Info | [551393] | ||
2,3,4-trihydroxybenzoic acid | Drug Info | [528676] | |||
2-Methyl-2,4-Pentanediol | Drug Info | [551393] | |||
BAICALEIN | Drug Info | [528676] | |||
Efomycine M | Drug Info | [535688] | |||
Fucose | Drug Info | [551393] | |||
GALLICACID | Drug Info | [528676] | |||
GMI-1070 | Drug Info | [530945], [531721], [544142] | |||
O-Sialic Acid | Drug Info | [551374] | |||
PSI-697 | Drug Info | [532283] | |||
PURPUROGALLIN | Drug Info | [528676] | |||
RPSGL-Ig | Drug Info | [533194], [537129] | |||
Modulator | CY-1503 | Drug Info | [533630] | ||
CY-1787 | Drug Info | [534107] | |||
SMART anti-E/P selectin | Drug Info | [526458] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Cell adhesion molecules (CAMs) | ||||
Malaria | |||||
Staphylococcus aureus infection | |||||
Pathway Interaction Database | IL4-mediated signaling events | ||||
amb2 Integrin signaling | |||||
Reactome | Platelet degranulation | ||||
Cell surface interactions at the vascular wall | |||||
WikiPathways | Human Complement System | ||||
Spinal Cord Injury | |||||
Cell surface interactions at the vascular wall | |||||
References | |||||
Ref 521727 | ClinicalTrials.gov (NCT00226369) Cylexin for Reduction of Reperfusion Injury in Infant Heart Surgery. U.S. National Institutes of Health. | ||||
Ref 521877 | ClinicalTrials.gov (NCT00367692) Study Evaluating PSI-697 in Patients With Scleritis. U.S. National Institutes of Health. | ||||
Ref 530945 | GMI-1070, a novel pan-selectin antagonist, reverses acute vascular occlusions in sickle cell mice. Blood. 2010 Sep 9;116(10):1779-86. | ||||
Ref 531721 | Deal watch: Pfizer deal for selectin inhibitor highlights potential of glycomimetic drugs. Nat Rev Drug Discov. 2011 Dec 1;10(12):890. | ||||
Ref 537129 | New developments in immunosuppressive therapy for heart transplantation. Expert Opin Emerg Drugs. 2009 Mar;14(1):1-21. | ||||
Ref 543059 | (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: 8307). | ||||
Ref 545569 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003725) | ||||
Ref 546235 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007041) | ||||
Ref 546284 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007242) | ||||
Ref 526458 | HuEP5C7 as a humanized monoclonal anti-E/P-selectin neurovascular protective strategy in a blinded placebo-controlled trial of nonhuman primate stroke. Circ Res. 2002 Nov 15;91(10):907-14. | ||||
Ref 528676 | J Med Chem. 2007 Mar 22;50(6):1101-15. Epub 2007 Feb 16.Rational design of novel, potent small molecule pan-selectin antagonists. | ||||
Ref 530945 | GMI-1070, a novel pan-selectin antagonist, reverses acute vascular occlusions in sickle cell mice. Blood. 2010 Sep 9;116(10):1779-86. | ||||
Ref 531721 | Deal watch: Pfizer deal for selectin inhibitor highlights potential of glycomimetic drugs. Nat Rev Drug Discov. 2011 Dec 1;10(12):890. | ||||
Ref 532283 | Effect of PSI-697, a novel P-selectin inhibitor, on platelet-monocyte aggregate formation in humans. J Am Heart Assoc. 2013 Jan 28;2(1):e006007. | ||||
Ref 533194 | rPSGL-1-Ig, a recombinant PSGL-1-Ig fusion protein, ameliorates LPS-induced acute lung injury in mice by inhibiting neutrophil migration. Cell Mol Biol (Noisy-le-grand). 2015 Feb 28;61(1):1-6. | ||||
Ref 533630 | Adjunctive selectin blockade successfully reduces infarct size beyond thrombolysis in the electrolytic canine coronary artery model. Circulation. 1995 Aug 1;92(3):492-9. | ||||
Ref 534107 | Administration of an antibody to E-selectin in patients with septic shock. Crit Care Med. 1996 Feb;24(2):229-33. | ||||
Ref 535688 | Interfering with leukocyte rolling--a promising therapeutic approach in inflammatory skin disorders? Trends Pharmacol Sci. 2003 Feb;24(2):49-52. | ||||
Ref 537129 | New developments in immunosuppressive therapy for heart transplantation. Expert Opin Emerg Drugs. 2009 Mar;14(1):1-21. | ||||
Ref 544142 | GMI-1070, a novel pan-selectin antagonist, reverses acute vascular occlusions in sickle cell mice. Blood. 2010 September 9; 116(10): 1779-1786. |
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