Integrins in GtoPdb v.2023.1

نویسندگان

چکیده

Integrins are unusual signalling proteins that function to signal both from the extracellular environment into cell, but also cytoplasm external of cell. The intracellular cascades associated with integrin activation focus on protein kinase activities, such as focal adhesion and Src. Based this association between signals activity, we have chosen include integrins in 'Catalytic receptors' section database until more stringent criteria NC-IUPHAR allows precise definition their classification.Integrins heterodimeric entities, composed α β subunits, each 1TM proteins, which bind components matrix or counter-receptors expressed other cells. One class contains an inserted domain (I) its subunit, if present (in α1, α2, α10, α11, αD, αE, αL, αM αX), I ligand binding site. All subunits possess a similar I-like domain, has capacity ligand, often recognising RGD motif. presence subunit precludes through subunit. provide link actin cytoskeleton (through typically short domains). several divalent cations, including Mg2+ ion is essential for binding. Other cation sites may regulate activity stabilise 3D structure. particular kinases, integrin-linked kinase. Cellular regulates affinity via inside-out can cellular outside-in signalling.Several drugs target clinical use including: (1) abciximab (αIIbβ3) term prevention coronary thrombosis, (2) vedolizumab (α4β7) reduce gastrointestinal inflammation, (3) natalizumab (α4β1) some cases severe multiple sclerosis.

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ژورنال

عنوان ژورنال: IUPHAR/BPS guide to pharmacology CITE

سال: 2023

ISSN: ['2633-1020']

DOI: https://doi.org/10.2218/gtopdb/f760/2023.1