Target Information

Target General Infomation
Target ID
T10965
Former ID
TTDC00197
Target Name
P-selectin
Gene Name
SELP
Synonyms
CD62P; GMP-140; Granule membrane protein 140; LECAM3; Leukocyte-endothelial cell adhesion molecule 3; PADGEM; SELP
Target Type
Clinical Trial
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.
BioChemical Class
Selectin/LECAM
Target Validation
T10965
UniProt ID
P16109
Sequence
MANCQIAILYQRFQRVVFGISQLLCFSALISELTNQKEVAAWTYHYSTKAYSWNISRKYC
QNRYTDLVAIQNKNEIDYLNKVLPYYSSYYWIGIRKNNKTWTWVGTKKALTNEAENWADN
EPNNKRNNEDCVEIYIKSPSAPGKWNDEHCLKKKHALCYTASCQDMSCSKQGECLETIGN
YTCSCYPGFYGPECEYVRECGELELPQHVLMNCSHPLGNFSFNSQCSFHCTDGYQVNGPS
KLECLASGIWTNKPPQCLAAQCPPLKIPERGNMTCLHSAKAFQHQSSCSFSCEEGFALVG
PEVVQCTASGVWTAPAPVCKAVQCQHLEAPSEGTMDCVHPLTAFAYGSSCKFECQPGYRV
RGLDMLRCIDSGHWSAPLPTCEAISCEPLESPVHGSMDCSPSLRAFQYDTNCSFRCAEGF
MLRGADIVRCDNLGQWTAPAPVCQALQCQDLPVPNEARVNCSHPFGAFRYQSVCSFTCNE
GLLLVGASVLQCLATGNWNSVPPECQAIPCTPLLSPQNGTMTCVQPLGSSSYKSTCQFIC
DEGYSLSGPERLDCTRSGRWTDSPPMCEAIKCPELFAPEQGSLDCSDTRGEFNVGSTCHF
SCDNGFKLEGPNNVECTTSGRWSATPPTCKGIASLPTPGLQCPALTTPGQGTMYCRHHPG
TFGFNTTCYFGCNAGFTLIGDSTLSCRPSGQWTAVTPACRAVKCSELHVNKPIAMNCSNL
WGNFSYGSICSFHCLEGQLLNGSAQTACQENGHWSTTVPTCQAGPLTIQEALTYFGGAVA
STIGLIMGGTLLALLRKRFRQKDDGKCPLNPHSHLGTYGVFTNAAFDPSP
Structure
1ESL; 1G1T; 1KJA; 4C16; 4CSY; 1FSB; 1G1Q; 1G1R; 1G1S; 1HES; 1KJD
Drugs and Mode of Action
Drug(s) GMI-1070 Drug Info Phase 3 Asthma [1], [2], [3]
CY-1503 Drug Info Phase 2/3 Hypertension [4]
RPSGL-Ig Drug Info Phase 2 Delayed graft function; Heart transplantation [5]
PSI-697 Drug Info Phase 1 Atherosclerosis; Thrombosis [6]
SelG1 Drug Info Phase 1 Vaso-occlusive crisis [7]
CDP-850 Drug Info Discontinued in Phase 2 Cancer [8]
CY-1787 Drug Info Discontinued in Phase 1 Allergy [9]
SMART anti-E/P selectin Drug Info Discontinued in Phase 1 Asthma [10]
PURPUROGALLIN Drug Info Terminated Discovery agent [11]
Inhibitor 1na Drug Info [12]
2,3,4-trihydroxybenzoic acid Drug Info [13]
2-Methyl-2,4-Pentanediol Drug Info [12]
BAICALEIN Drug Info [13]
Efomycine M Drug Info [14]
Fucose Drug Info [12]
GALLICACID Drug Info [13]
GMI-1070 Drug Info [1], [2], [15]
O-Sialic Acid Drug Info [16]
PSI-697 Drug Info [17]
PURPUROGALLIN Drug Info [13]
RPSGL-Ig Drug Info [18], [5]
Modulator CY-1503 Drug Info [19]
CY-1787 Drug Info [20]
SMART anti-E/P selectin Drug Info [21]
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 1GMI-1070, a novel pan-selectin antagonist, reverses acute vascular occlusions in sickle cell mice. Blood. 2010 Sep 9;116(10):1779-86.
REF 2Deal watch: Pfizer deal for selectin inhibitor highlights potential of glycomimetic drugs. Nat Rev Drug Discov. 2011 Dec 1;10(12):890.
REF 3(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 4ClinicalTrials.gov (NCT00226369) Cylexin for Reduction of Reperfusion Injury in Infant Heart Surgery. U.S. National Institutes of Health.
REF 5New developments in immunosuppressive therapy for heart transplantation. Expert Opin Emerg Drugs. 2009 Mar;14(1):1-21.
REF 6ClinicalTrials.gov (NCT00367692) Study Evaluating PSI-697 in Patients With Scleritis. U.S. National Institutes of Health.
REF 7Clinical pipeline report, company report or official report of Selexys Pharmaceuticals (2011).
REF 8Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007242)
REF 9Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003725)
REF 10Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008129)
REF 11Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007041)
REF 12How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 13J Med Chem. 2007 Mar 22;50(6):1101-15. Epub 2007 Feb 16.Rational design of novel, potent small molecule pan-selectin antagonists.
REF 14Interfering with leukocyte rolling--a promising therapeutic approach in inflammatory skin disorders? Trends Pharmacol Sci. 2003 Feb;24(2):49-52.
REF 15GMI-1070, a novel pan-selectin antagonist, reverses acute vascular occlusions in sickle cell mice. Blood. 2010 September 9; 116(10): 1779-1786.
REF 16The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 17Effect 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 18rPSGL-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 19Adjunctive selectin blockade successfully reduces infarct size beyond thrombolysis in the electrolytic canine coronary artery model. Circulation. 1995 Aug 1;92(3):492-9.
REF 20Administration of an antibody to E-selectin in patients with septic shock. Crit Care Med. 1996 Feb;24(2):229-33.
REF 21HuEP5C7 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.

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