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Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage

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 cascad...

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Main Authors: Wang, Hao, Chen, Meiling, Sang, Xiaohong, You, Xuefu, Wang, Yucheng, Paterson, Ian Charles, Hong, Wei, Yang, Xinyi
Format: Article
Published: Elsevier 2020
Subjects:
R Medicine
TP Chemical technology
Online Access:http://eprints.um.edu.my/24767/
https://doi.org/10.1016/j.ejmech.2020.112154
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spelling my.um.eprints.247672020-06-10T01:08:20Z http://eprints.um.edu.my/24767/ Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage Wang, Hao Chen, Meiling Sang, Xiaohong You, Xuefu Wang, Yucheng Paterson, Ian Charles Hong, Wei Yang, Xinyi R Medicine TP Chemical technology 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 Elsevier 2020 Article PeerReviewed 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 https://doi.org/10.1016/j.ejmech.2020.112154 doi:10.1016/j.ejmech.2020.112154
institution Universiti Malaya
building UM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Malaya
content_source UM Research Repository
url_provider http://eprints.um.edu.my/
topic R Medicine
TP Chemical technology
spellingShingle R Medicine
TP Chemical technology
Wang, Hao
Chen, Meiling
Sang, Xiaohong
You, Xuefu
Wang, Yucheng
Paterson, Ian Charles
Hong, Wei
Yang, Xinyi
Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage
description 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
format Article
author Wang, Hao
Chen, Meiling
Sang, Xiaohong
You, Xuefu
Wang, Yucheng
Paterson, Ian Charles
Hong, Wei
Yang, Xinyi
author_facet Wang, Hao
Chen, Meiling
Sang, Xiaohong
You, Xuefu
Wang, Yucheng
Paterson, Ian Charles
Hong, Wei
Yang, Xinyi
author_sort Wang, Hao
title Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage
title_short Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage
title_full Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage
title_fullStr Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage
title_full_unstemmed Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage
title_sort development of small molecule inhibitors targeting tgf-β ligand and receptor: structures, mechanism, preclinical studies and clinical usage
publisher Elsevier
publishDate 2020
url http://eprints.um.edu.my/24767/
https://doi.org/10.1016/j.ejmech.2020.112154
_version_ 1674066725804441600
score 13.211869

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