Small Molecule "Silmitasertib" Repurposed as Inhibitor of Transforming Growth Factor Beta 1 for the Development of Therapeutics for Oral Submucous Fibrosis

被引：5

作者：

Boreak, Nezar ^{[1
]}

机构：

[1] Jazan Univ, Dept Restorat Dent Sci, Coll Dent, Jazan, Saudi Arabia

来源：

BIOMED RESEARCH INTERNATIONAL | 2021年 / 2021卷

关键词：

SWISS-PDBVIEWER; PATHOGENESIS; INDIA; MODEL;

D O I：

10.1155/2021/6631848

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Oral submucous fibrosis (OSMF) is considered a premalignant condition characterized by aggressive fibrosis of the submucosal tissues of the oral cavity reflecting its malignant transformation potential. Activation of transforming growth factor beta (TGF-beta) signaling has been reported to lead increased collagen production and fibrosis. Recently, significant upregulation of TGF-beta 1 has been reported in OSMF as compared to normal tissues. Therefore, inhibition of the TGF-beta 1 may pave for the development of therapeutics of OSMF. Based on the structure-assisted drug designing, we found "silmitasertib" as potent inhibitor of TGF-beta 1. We suggest that this molecule can be validated and implemented for the treatment of OSMF.

引用

页数：8

共 28 条

[1] Areca nut in pathogenesis of oral submucous fibrosis: Revisited
Angadi P.V.
Rao S.S.
[J]. Oral and Maxillofacial Surgery, 2011, 15 (1) : 1 - 9
[2] Burden of Smoked and Smokeless Tobacco Consumption in India - Results from the Global adult Tobacco Survey India (GATS-India)-2009-2010
Bhawna, Gupta
[J]. ASIAN PACIFIC JOURNAL OF CANCER PREVENTION, 2013, 14 (05) : 3323 - 3329
[3] SWISS-MODEL and the Swiss-PdbViewer: An environment for comparative protein modeling
Guex, N
Peitsch, MC
[J]. ELECTROPHORESIS, 1997, 18 (15) : 2714 - 2723
[4] Automated comparative protein structure modeling with SWISS-MODEL and Swiss-PdbViewer: A historical perspective
Guex, Nicolas
Peitsch, Manuel C.
Schwede, Torsten
[J]. ELECTROPHORESIS, 2009, 30 : S162 - S173
[5] Role of oxidative stress and antioxidants in aetiopathogenesis and management of oral submucous fibrosis
Gupta S.
Reddyand M.V.R.
Harinath B.C.
[J]. Indian Journal of Clinical Biochemistry, 2004, 19 (1) : 138 - 141
[6] Immunolocalization of cytokines and growth factors in oral submucous fibrosis
Haque, MF
Harris, M
Meghji, S
Barrett, AW
[J]. CYTOKINE, 1998, 10 (09) : 713 - 719
[7] Hazarey VK, 2007, J ORAL PATHOL MED, V36, P12
[8] Oral submucous fibrosis in India: Are we progressing??
Hebbar, P. B.
Sheshaprasad, R.
Gurudath, S.
Pai, A.
Sujatha, D.
[J]. INDIAN JOURNAL OF CANCER, 2014, 51 (03) : 222 - 226
[9] ChemBioOffice Ultra 2010 Suite
Kerwin, Sean M.
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2010, 132 (07) : 2466 - 2467
[10] Activation of TGF-β Pathway by Areca Nut Constituents: A Possible Cause of Oral Submucous Fibrosis
Khan, Imran
Kumar, Neeraj
Pant, Ila
Narra, Sivakrishna
Kondaiah, Paturu
[J]. PLOS ONE, 2012, 7 (12):

← 1 2 3 →