Structural Aspects of LIMK Regulation and Pharmacology

Author:

Chatterjee DeepORCID,Preuss Franziska,Dederer Verena,Knapp StefanORCID,Mathea Sebastian

Abstract

Malfunction of the actin cytoskeleton is linked to numerous human diseases including neurological disorders and cancer. LIMK1 (LIM domain kinase 1) and its paralogue LIMK2 are two closely related kinases that control actin cytoskeleton dynamics. Consequently, they are potential therapeutic targets for the treatment of such diseases. In the present review, we describe the LIMK conformational space and its dependence on ligand binding. Furthermore, we explain the unique catalytic mechanism of the kinase, shedding light on substrate recognition and how LIMK activity is regulated. The structural features are evaluated for implications on the drug discovery process. Finally, potential future directions for targeting LIMKs pharmacologically, also beyond just inhibiting the kinase domain, are discussed.

Publisher

MDPI AG

Subject

General Medicine

Cited by 13 articles. 订阅此论文施引文献 订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献

1. Decoding the tumour-modulatory roles of LIMK2;Life Sciences;2024-06

2. The Role of LIM Kinase 1 in Memory Processes;Neuroscience and Behavioral Physiology;2024-06

3. Tetrahydropyridine LIMK inhibitors: Structure activity studies and biological characterization;European Journal of Medicinal Chemistry;2024-05

4. Engineering memory with an extrinsically disordered kinase;Science Advances;2023-11-17

5. Role of LIM-Kinase 1 in Memory Processes;Успехи физиологических наук;2023-10-01

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