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selectin P (CD62)

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 3103

Nomenclature: selectin P (CD62)

Family: CD molecules

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 830 1q24.2 SELP selectin P
Previous and Unofficial Names Click here for help
CD62P | GMP140 | granule membrane protein 140kD | PADGEM | pSEL | P-selectin
Database Links Click here for help
Alphafold P16109 (Hs)
ChEMBL Target CHEMBL5378 (Hs)
Ensembl Gene ENSG00000174175 (Hs)
Entrez Gene 6403 (Hs)
Human Protein Atlas ENSG00000174175 (Hs)
KEGG Gene hsa:6403 (Hs)
OMIM 173610 (Hs)
Pharos P16109 (Hs)
RefSeq Nucleotide NM_003005 (Hs)
RefSeq Protein NP_002996 (Hs)
UniProtKB P16109 (Hs)
Wikipedia SELP (Hs)

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
bimosiamose Small molecule or natural product Immunopharmacology Ligand Hs Binding 4.2 pIC50 5
⤷ pIC50 4.2 (IC50 7x10-5 M) [5]
Description: Inhibition of P-selectin binding in an HL-60 cellular assay.
rivipansel Small molecule or natural product Hs Binding 3.4 pIC50 2
⤷ pIC50 3.4 (IC50 4.23x10-4 M) [2]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
crizanlizumab Peptide Approved drug Hs Binding 8.2 pKd 7
⤷ pKd 8.2 (Kd 5.89x10-9 M) [7]
Description: Binding affinity determined by SPR.
inclacumab Peptide Immunopharmacology Ligand Hs Binding - - 3
⤷ [3]
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
selectin P ligand {Sp: Human} Peptide Ligand is endogenous in the given species Immunopharmacology Ligand Hs Binding 6.5 pKd 6
⤷ pKd 6.5 (Kd 3.2x10-7 M) [6]
Immunopharmacology Comments
Leukocytes use P-selectin/selectin P ligand binding to facilitate tethering and rolling on endothelial surfaces [6].
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Sickle cell anemia
Disease Ontology: DOID:10923
Role:  The P-selectin/P-selectin glycoprotein ligand 1 (PSGL-1) interaction is involved in cell adhesion, largely between leukocytes, platelets and vascular endothelial cells. In Sickle cell disease P-selectin/PSGL-1 complexes promote abnormal adhesion of sickled erythrocytes to activated endothelial cells which precipitates vascular occlusion and pain crises.
Drugs:  Crizanlizumab
Comments:  Crizanlizumab binds to P-selectin and blocks interaction with PSGL-1, as a mechanism to reduce the frequency of vaso-occlusive crises in patients with sickle cell disease.
References:  4
General Comments
Leukocytes use P-selectin/selectin P ligand binding to facilitate tethering and rolling on endothelial surfaces [6]. Aberrant P-selectin translocation to the surface of sickled erythrocytes causes veno-occlusion in the microvasculature of patients with sickle cell disease. The P-selectin/selectin P ligand interaction is functionally antagonised by the first-in-class, targeted sickle cell disease therapeutic (an anti-P-selectin monoclonal) [1,7].

References

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1. Ataga KI, Kutlar A, Kanter J, Liles D, Cancado R, Friedrisch J, Guthrie TH, Knight-Madden J, Alvarez OA, Gordeuk VR et al.. (2017) Crizanlizumab for the Prevention of Pain Crises in Sickle Cell Disease. N Engl J Med, 376 (5): 429-439. [PMID:27959701]

2. Chang J, Patton JT, Sarkar A, Ernst B, Magnani JL, Frenette PS. (2010) GMI-1070, a novel pan-selectin antagonist, reverses acute vascular occlusions in sickle cell mice. Blood, 116 (10): 1779-86. [PMID:20508165]

3. Graus Y, Himber J, Jansen-Molenaar M, Kling D, Kopetzky E, Parren P, Reber F, Steiner B, Stern A, Strein P et al.. (2005) Anti-p-selectin antibodies. Patent number: WO2005100402A1. Assignee: F.Hoffmann-La Roche Ag. Priority date: 05/04/2005. Publication date: 27/10/2005.

4. Kaur K, Kennedy K, Liles D. (2023) Crizanlizumab in sickle cell disease. Pain Manag, [Epub ahead of print]. [PMID:37850353]

5. Kogan TP, Dupré B, Bui H, McAbee KL, Kassir JM, Scott IL, Hu X, Vanderslice P, Beck PJ, Dixon RA. (1998) Novel synthetic inhibitors of selectin-mediated cell adhesion: synthesis of 1,6-bis[3-(3-carboxymethylphenyl)-4-(2-alpha-D- mannopyranosyloxy)phenyl]hexane (TBC1269). J Med Chem, 41 (7): 1099-111. [PMID:9544210]

6. Mehta P, Cummings RD, McEver RP. (1998) Affinity and kinetic analysis of P-selectin binding to P-selectin glycoprotein ligand-1. J Biol Chem, 273 (49): 32506-13. [PMID:9829984]

7. Rollins S, ALvarez R, Rother R, Kawar ZS, Mcever RP. (2012) Anti-p-selectin antibodies and methods of their use and identification. Patent number: WO2012088265A1. Assignee: Selexys Pharmaceuticals Corporation. Priority date: 21/12/2010. Publication date: 28/06/2012.

How to cite this page

CD molecules: selectin P (CD62). Last modified on 16/11/2023. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3103.