Wang, Hao and Chen, Meiling and Sang, Xiaohong and You, Xuefu and Wang, Yucheng and Paterson, Ian Charles and Hong, Wei and Yang, Xinyi (2020) Development of small molecule inhibitors targeting TGF-beta ligand and receptor: Structures, mechanism, preclinical studies and clinical usage. European Journal of Medicinal Chemistry, 191. ISSN 0223-5234, DOI https://doi.org/10.1016/j.ejmech.2020.112154.
Full text not available from this repository.Abstract
Transforming growth factor-beta (TGF-beta) is a member of a superfamily of pleiotropic proteins that regulate multiple cellular processes such as growth, development and differentiation. Following binding to type I and II TGF-beta serine/threonine kinase receptors, TGF-beta activates downstream signaling cascades involving both SMAD-dependent and -independent pathways. Aberrant TGF-beta signaling is associated with a variety of diseases, such as fibrosis, cardiovascular disease and cancer. Hence, the TGF-beta signaling pathway is recognized as a potential drug target. Various organic molecules have been designed and developed as TGF-beta signaling pathway inhibitors and they function by either down-regulating the expression of TGF-beta or by inhibiting the kinase activities of the TGF-beta receptors. In this review, we discuss the current status of research regarding organic molecules as TGF-beta inhibitors, focusing on the biological functions and the binding poses of compounds that are in the market or in the clinical or pre-clinical phases of development. (c) 2020 Elsevier Masson SAS. All rights reserved.
| Item Type: | Article |
|---|---|
| Funders: | National Natural Science Foundation of China (NSFC) [81660588] |
| Uncontrolled Keywords: | TGF-beta; TGF-beta receptor; SMAD signaling pathway; Small-molecule inhibitor |
| Subjects: | R Medicine |
| Divisions: | Faculty of Dentistry |
| Depositing User: | Ms Zaharah Ramly |
| Date Deposited: | 04 Oct 2023 06:46 |
| Last Modified: | 04 Oct 2023 06:46 |
| URI: | http://eprints.um.edu.my/id/eprint/36800 |
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