Target Information

Target General Infomation
Target ID
T72835
Former ID
TTDC00098
Target Name
E-selectin
Gene Name
SELE
Synonyms
CD62E; CD62E antigen; ELAM-1; Endothelial leukocyte adhesion molecule 1; LECAM2; Leukocyte-endothelial cell adhesion molecule 2; SELE
Target Type
Clinical Trial
Disease Asthma [ICD10: J45]
Acute myeloid leukemia [ICD9: 205; ICD10: C92.0]
Chronic obstructive pulmonary disease; Psoriatic disorder; Atopic dermatitis [ICD9:490-492, 494-496, 691.8, 692.9, 696; ICD10: J40-J44, J47, L20, L20-L30, L40]
Hypertension [ICD9: 401; ICD10: I10-I16]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Function
Cell-surface glycoprotein having a role in immunoadhesion. Mediates in the adhesion of blood neutrophils in cytokine-activated endothelium through interaction with PSGL1/SELPLG. May have a role in capillary morphogenesis.
BioChemical Class
Selectin/LECAM
Target Validation
T72835
UniProt ID
P16581
Sequence
MIASQFLSALTLVLLIKESGAWSYNTSTEAMTYDEASAYCQQRYTHLVAIQNKEEIEYLN
SILSYSPSYYWIGIRKVNNVWVWVGTQKPLTEEAKNWAPGEPNNRQKDEDCVEIYIKREK
DVGMWNDERCSKKKLALCYTAACTNTSCSGHGECVETINNYTCKCDPGFSGLKCEQIVNC
TALESPEHGSLVCSHPLGNFSYNSSCSISCDRGYLPSSMETMQCMSSGEWSAPIPACNVV
ECDAVTNPANGFVECFQNPGSFPWNTTCTFDCEEGFELMGAQSLQCTSSGNWDNEKPTCK
AVTCRAVRQPQNGSVRCSHSPAGEFTFKSSCNFTCEEGFMLQGPAQVECTTQGQWTQQIP
VCEAFQCTALSNPERGYMNCLPSASGSFRYGSSCEFSCEQGFVLKGSKRLQCGPTGEWDN
EKPTCEAVRCDAVHQPPKGLVRCAHSPIGEFTYKSSCAFSCEEGFELHGSTQLECTSQGQ
WTEEVPSCQVVKCSSLAVPGKINMSCSGEPVFGTVCKFACPEGWTLNGSAARTCGATGHW
SGLLPTCEAPTESNIPLVAGLSAAGLSLLTLAPFLLWLRKCLRKAKKFVPASSCQSLESD
GSYQKPSYIL
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]
Bimosiamose Drug Info Phase 2a Chronic obstructive pulmonary disease; Psoriatic disorder; Atopic dermatitis [5]
Bimosiamose Drug Info Phase 2 Asthma [5]
GMI-1271 Drug Info Phase 1 Acute myeloid leukemia [6]
SMART anti-E/P selectin Drug Info Discontinued in Phase 1 Asthma [7]
GI-270384X Drug Info Terminated Inflammatory bowel disease [8]
Inhibitor 1na Drug Info [9]
Bimosiamose Drug Info [10], [11], [12]
Efomycine M Drug Info [13]
Fucose Drug Info [9]
GMI-1070 Drug Info [1], [2], [14]
GMI-1271 Drug Info [15]
O-Sialic Acid Drug Info [16]
Modulator CY-1503 Drug Info [17]
GI-270384X Drug Info [8]
SMART anti-E/P selectin Drug Info [18]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Cell adhesion molecules (CAMs)
TNF signaling pathway
African trypanosomiasis
Malaria
NetPath Pathway IL5 Signaling Pathway
IL4 Signaling Pathway
TNFalpha Signaling Pathway
ID Signaling Pathway
Pathway Interaction Database Thromboxane A2 receptor signaling
Glucocorticoid receptor regulatory network
ATF-2 transcription factor network
Reactome Cell surface interactions at the vascular wall
WikiPathways Human Complement System
TNF alpha Signaling Pathway
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 5Emerging drugs for asthma. Expert Opin Emerg Drugs. 2008 Dec;13(4):643-53.
REF 6ClinicalTrials.gov (NCT02271113) Phase I Study to Assess Safety and Pharmacokinetics of GMI-1271 in Healthy Adult Subjects. U.S. National Institutes of Health.
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008129)
REF 8Inhibition of endothelial cell adhesion molecule expression improves colonic hyperalgaesia. Neurogastroenterol Motil. 2009 Feb;21(2):189-96.
REF 9How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 10Bimosiamose, an inhaled small-molecule pan-selectin antagonist, attenuates late asthmatic reactions following allergen challenge in mild asthmatics: a randomized, double-blind, placebo-controlled clinical cross-over-trial. Pulm Pharmacol Ther. 2006;19(4):233-41. Epub 2005 Sep 1.
REF 11The pharmacokinetics of subcutaneously injected Bimosiamose disodium in healthy male volunteers. Biopharm Drug Dispos. 2007 Dec;28(9):475-84.
REF 12Effects of the pan-selectin antagonist bimosiamose (TBC1269) in experimental human endotoxemia. Shock. 2008 Apr;29(4):475-82.
REF 13Interfering with leukocyte rolling--a promising therapeutic approach in inflammatory skin disorders? Trends Pharmacol Sci. 2003 Feb;24(2):49-52.
REF 14GMI-1070, a novel pan-selectin antagonist, reverses acute vascular occlusions in sickle cell mice. Blood. 2010 September 9; 116(10): 1779-1786.
REF 15Clinical pipeline report, company report or official report of glycomimetics.
REF 16The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 17Adjunctive selectin blockade successfully reduces infarct size beyond thrombolysis in the electrolytic canine coronary artery model. Circulation. 1995 Aug 1;92(3):492-9.
REF 18HuEP5C7 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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