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-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage. European Journal of Medicinal Chemistry, 191. p. 112154. ISSN 0223-5234, DOI https://doi.org/10.1016/j.ejmech.2020.112154.
Full text not available from this repository.Abstract
Transforming growth factor-β (TGF-β) 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-β serine/threonine kinase receptors, TGF-β activates downstream signaling cascades involving both SMAD-dependent and -independent pathways. Aberrant TGF-β signaling is associated with a variety of diseases, such as fibrosis, cardiovascular disease and cancer. Hence, the TGF-β signaling pathway is recognized as a potential drug target. Various organic molecules have been designed and developed as TGF-β signaling pathway inhibitors and they function by either down-regulating the expression of TGF-β or by inhibiting the kinase activities of the TGF-β receptors. In this review, we discuss the current status of research regarding organic molecules as TGF-β 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. © 2020 Elsevier Masson SAS
| Item Type: | Article |
|---|---|
| Funders: | National Natural Science Foundation of China ( 81660588 , 81960623 , 81773582 , 81973383 , 8132100 , 81621064 ), Key R&D Program of Ningxia ( 2018BFG02004 ), Program for Leading Talents of Ningxia Province ( KJT2018004 ), National Mega-project for Innovative Drugs ( 2019ZX09721001 ), National Science & Technology Major Project “Key New Drug Creation and Manufacturing Program”, China ( 2019ZX09201001-003-007 ), CAMS Initiative Fund for Innovative Medicine ( 2016-I2M-3-014 ), Peking Union Medical College Youth Fund (PUMC) ( 33320140177 and 3332016139 ) |
| Uncontrolled Keywords: | TGF-β; TGF-β receptor; SMAD signaling pathway; Small-molecule inhibitor |
| Subjects: | R Medicine T Technology > TP Chemical technology |
| Divisions: | Faculty of Dentistry |
| Depositing User: | Ms. Juhaida Abd Rahim |
| Date Deposited: | 10 Jun 2020 01:08 |
| Last Modified: | 10 Jun 2020 01:08 |
| URI: | http://eprints.um.edu.my/id/eprint/24767 |
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