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integrin, alpha L subunit (antigen CD11A (p180), lymphocyte function-associated antigen 1; alpha polypeptide)

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 2451

Nomenclature: integrin, alpha L subunit (antigen CD11A (p180), lymphocyte function-associated antigen 1; alpha polypeptide)

Family: Integrins

Contents:

Quaternary Structure: Complexes
integrin αLβ2
Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1170 16p11.2 ITGAL integrin subunit alpha L
Mouse 1 1163 7 69.44 cM Itgal integrin alpha L
Rat - 1160 1q36 Itgal integrin subunit alpha L
Previous and Unofficial Names Click here for help
CD11 antigen-like family member A | CD11A | Integrin alpha-L | LFA-1 | Ly-15 | Ly-21 | Lymphocyte antigen 15 | integrin, alpha L
Database Links Click here for help
Alphafold P20701 (Hs), P24063 (Mm)
ChEMBL Target CHEMBL1803 (Hs), CHEMBL1075188 (Mm)
DrugBank Target P20701 (Hs)
Ensembl Gene ENSG00000005844 (Hs), ENSMUSG00000030830 (Mm), ENSRNOG00000017980 (Rn)
Entrez Gene 3683 (Hs), 16408 (Mm), 308995 (Rn)
Human Protein Atlas ENSG00000005844 (Hs)
KEGG Gene hsa:3683 (Hs), mmu:16408 (Mm), rno:308995 (Rn)
OMIM 153370 (Hs)
Pharos P20701 (Hs)
RefSeq Nucleotide NM_002209 (Hs), NM_001114380 (Hs), NM_001253872 (Mm), NM_008400 (Mm), NM_001253874 (Mm), NM_001253873 (Mm), NM_001033998 (Rn)
RefSeq Protein NP_002200 (Hs), NP_001107852 (Hs), NP_001240801 (Mm), NP_001240802 (Mm), NP_001240803 (Mm), NP_032426 (Mm), NP_001029170 (Rn)
UniProtKB P20701 (Hs), P24063 (Mm)
Wikipedia ITGAL (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
BI-1950 Small molecule or natural product Immunopharmacology Ligand Hs Binding 8.1 pKd 1
⤷ pKd 8.1 (Kd 9x10-9 M) [1]
Description: Inhibition of LFA-1 binding to ICAM-1 in vitro.
BIRT 377 Small molecule or natural product Immunopharmacology Ligand Hs Binding 7.6 pKd 4
⤷ pKd 7.6 (Kd 2.58x10-8 M) [4]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
lifitegrast Small molecule or natural product Approved drug Primary target of this compound Immunopharmacology Ligand Hs Inhibition - - 2,7
⤷ [2,7]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
efalizumab Peptide Approved drug Primary target of this compound Immunopharmacology Ligand Hs Binding 11.4 pKd 3
⤷ pKd 11.4 (Kd 4x10-12 M) [3]
Description: Binding of humanized MHM24 to human CD11a on Jurkat cells.
rovelizumab Peptide Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Binding - - 5-6
⤷ [5-6]
Immunopharmacology Comments
ITGAL associates with the beta 2 chain (ITGB2) integrin and CD18 to form the lymphocyte function-associated antigen-1 (LFA-1) complex. LFA-1 is crucial for leukocyte intercellular adhesion and costimulatory signaling in the immune system. Ligands for LFA-1 are the intercellular adhesion molecules (ICAMs) 1-3. ITGAL is the target of the withdrawn psoriasis monoclonal antibody drug efalizumab.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  T cell (activation)
Immuno Process:  Immune regulation
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling

References

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1. Boehringer Ingelheim. LFA-1 (lymphocyte function-associated antigen-1) antagonist | BI-1950. Accessed on 28/11/2017. Modified on 28/11/2017. opnme.com, https://www.opnme.com/molecules/lfa-1-bi-1950

2. Breitenstein W, Huerzeler M, Kelly T, Mancuso R, Schneider G, Weitz-Schmidt G. (2015) Small molecule lfa-1 inhibitors. Patent number: WO2015189265. Assignee: Allocyte Pharmaceuticals Ag. Priority date: 12/06/2014. Publication date: 17/12/2015.

3. Jardieu PM, Presta LG. (2004) Method of treatment using humanized anti-CD11a antibodies. Patent number: US6703018. Assignee: Genentech, Inc.. Priority date: 27/11/1996. Publication date: 19/03/2004.

4. Kelly TA, Jeanfavre DD, McNeil DW, Woska Jr JR, Reilly PL, Mainolfi EA, Kishimoto KM, Nabozny GH, Zinter R, Bormann BJ et al.. (1999) Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion. J Immunol, 163 (10): 5173-7. [PMID:10553036]

5. Liles WC, Dale DC, Price TH, Gaviria JM, Turner T, Saoud J, Frumkin LR. (2000) Inhibition of in vivo neutrophil transmigration by a novel humanized anti-CD11/CD18 monoclonal antibody. Cytokines Cell Mol Ther, 6 (3): 121-6. [PMID:11140880]

6. Yenari MA, Kunis D, Sun GH, Onley D, Watson L, Turner S, Whitaker S, Steinberg GK. (1998) Hu23F2G, an antibody recognizing the leukocyte CD11/CD18 integrin, reduces injury in a rabbit model of transient focal cerebral ischemia. Exp Neurol, 153 (2): 223-33. [PMID:9784282]

7. Zhong M, Gadek TR, Bui M, Shen W, Burnier J, Barr KJ, Hanan EJ, Oslob JD, Yu CH, Zhu J et al.. (2012) Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye. ACS Med Chem Lett, 3 (3): 203-6. [PMID:24900456]

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