当前位置： SCI文献检索 > JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY期刊下所有文献 > New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011-2021) focussing on structure-activity relationship (SAR) and docking insights.

New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011-2021) focussing on structure-activity relationship (SAR) and docking insights.

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.

journal_name

J Enzyme Inhib Med Chem

journal_title

Journal of enzyme inhibition and medicinal chemistry

authors

Elkamhawy A,Ali EMH,Lee K

doi

10.1080/14756366.2021.1937143

keywords:

["Lck inhibitors","Src family kinase","lymphocyte-specific protein tyrosine kinase (Lck)","molecular modelling","structure-activity relationship (SAR)"]

subject

Has Abstract

pub_date

2021-12-01 00:00:00

pages

1574-1602

issue

1

eissn

1475-6366

issn

1475-6374

journal_volume

36

pub_type

杂志文章

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