Target Information
Target General Infomation | |||||
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Target ID |
T72835
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Former ID |
TTDC00098
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Target Name |
E-selectin
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Gene Name |
SELE
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Synonyms |
CD62E; CD62E antigen; ELAM-1; Endothelial leukocyte adhesion molecule 1; LECAM2; Leukocyte-endothelial cell adhesion molecule 2; SELE
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Target Type |
Clinical Trial
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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.
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BioChemical Class |
Selectin/LECAM
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Target Validation |
T72835
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UniProt ID | |||||
Sequence |
MIASQFLSALTLVLLIKESGAWSYNTSTEAMTYDEASAYCQQRYTHLVAIQNKEEIEYLN
SILSYSPSYYWIGIRKVNNVWVWVGTQKPLTEEAKNWAPGEPNNRQKDEDCVEIYIKREK DVGMWNDERCSKKKLALCYTAACTNTSCSGHGECVETINNYTCKCDPGFSGLKCEQIVNC TALESPEHGSLVCSHPLGNFSYNSSCSISCDRGYLPSSMETMQCMSSGEWSAPIPACNVV ECDAVTNPANGFVECFQNPGSFPWNTTCTFDCEEGFELMGAQSLQCTSSGNWDNEKPTCK AVTCRAVRQPQNGSVRCSHSPAGEFTFKSSCNFTCEEGFMLQGPAQVECTTQGQWTQQIP VCEAFQCTALSNPERGYMNCLPSASGSFRYGSSCEFSCEQGFVLKGSKRLQCGPTGEWDN EKPTCEAVRCDAVHQPPKGLVRCAHSPIGEFTYKSSCAFSCEEGFELHGSTQLECTSQGQ WTEEVPSCQVVKCSSLAVPGKINMSCSGEPVFGTVCKFACPEGWTLNGSAARTCGATGHW SGLLPTCEAPTESNIPLVAGLSAAGLSLLTLAPFLLWLRKCLRKAKKFVPASSCQSLESD GSYQKPSYIL |
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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] | |
Bimosiamose | Drug Info | Phase 2a | Chronic obstructive pulmonary disease; Psoriatic disorder; Atopic dermatitis | [536958] | |
Bimosiamose | Drug Info | Phase 2 | Asthma | [536958] | |
GMI-1271 | Drug Info | Phase 1 | Acute myeloid leukemia | [524962] | |
SMART anti-E/P selectin | Drug Info | Discontinued in Phase 1 | Asthma | [546436] | |
GI-270384X | Drug Info | Terminated | Inflammatory bowel disease | [529903] | |
Inhibitor | 1na | Drug Info | [551393] | ||
Bimosiamose | Drug Info | [536136], [536502], [536763] | |||
Efomycine M | Drug Info | [535688] | |||
Fucose | Drug Info | [551393] | |||
GMI-1070 | Drug Info | [530945], [531721], [544142] | |||
GMI-1271 | Drug Info | [550826] | |||
O-Sialic Acid | Drug Info | [551374] | |||
Modulator | CY-1503 | Drug Info | [533630] | ||
GI-270384X | Drug Info | [529903] | |||
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) | ||||
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 521727 | ClinicalTrials.gov (NCT00226369) Cylexin for Reduction of Reperfusion Injury in Infant Heart Surgery. U.S. National Institutes of Health. | ||||
Ref 524962 | ClinicalTrials.gov (NCT02271113) Phase I Study to Assess Safety and Pharmacokinetics of GMI-1271 in Healthy Adult Subjects. U.S. National Institutes of Health. | ||||
Ref 529903 | Inhibition of endothelial cell adhesion molecule expression improves colonic hyperalgaesia. Neurogastroenterol Motil. 2009 Feb;21(2):189-96. | ||||
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 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 529903 | Inhibition of endothelial cell adhesion molecule expression improves colonic hyperalgaesia. Neurogastroenterol Motil. 2009 Feb;21(2):189-96. | ||||
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 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 535688 | Interfering with leukocyte rolling--a promising therapeutic approach in inflammatory skin disorders? Trends Pharmacol Sci. 2003 Feb;24(2):49-52. | ||||
Ref 536136 | Bimosiamose, 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 536502 | The pharmacokinetics of subcutaneously injected Bimosiamose disodium in healthy male volunteers. Biopharm Drug Dispos. 2007 Dec;28(9):475-84. | ||||
Ref 536763 | Effects of the pan-selectin antagonist bimosiamose (TBC1269) in experimental human endotoxemia. Shock. 2008 Apr;29(4):475-82. |
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