关键词: Lck inhibitors Src family kinase lymphocyte-specific protein tyrosine kinase (Lck) molecular modelling structure-activity relationship (SAR)

Mesh : Dose-Response Relationship, Drug Drug Discovery Humans Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / antagonists & inhibitors metabolism Molecular Docking Simulation Protein Kinase Inhibitors / chemistry pharmacology Structure-Activity Relationship

来  源:   DOI:10.1080/14756366.2021.1937143   PDF(Sci-hub)   PDF(Pubmed)

Abstract:
Lymphocyte-specific protein tyrosine kinase (Lck), a non-receptor Src family kinase, has a vital role in various cellular processes such as cell cycle control, cell adhesion, motility, proliferation, and differentiation. Lck is reported as a key factor regulating the functions of T-cell including the initiation of TCR signalling, T-cell development, in addition to T-cell homeostasis. Alteration in expression and activity of Lck results in numerous disorders such as cancer, asthma, diabetes, rheumatoid arthritis, atherosclerosis, and neuronal diseases. Accordingly, Lck has emerged as a novel target against different diseases. Herein, we amass the research efforts in literature and pharmaceutical patents during the last decade to develop new Lck inhibitors. Additionally, structure-activity relationship studies (SAR) and docking models of these new inhibitors within the active site of Lck were demonstrated offering deep insights into their different binding modes in a step towards the identification of more potent, selective, and safe Lck inhibitors.
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