Synthesis and biological evaluation of novel 2,3-pyrazole ring-substituted-4,4-dimethyl lithocholic acid derivatives as selective protein tyrosine phosphatase 1B (PTP1B) inhibitors with cellular efficacy-Reference-Cited by-同舟云学术

Synthesis and biological evaluation of novel 2,3-pyrazole ring-substituted-4,4-dimethyl lithocholic acid derivatives as selective protein tyrosine phosphatase 1B (PTP1B) inhibitors with cellular efficacy

Published:2015 Issue:129 Volume:5 Page:106551-106560
ISSN:2046-2069
Container-title:RSC Advances
language:en
Short-container-title:RSC Adv.

Author:

Mao Shi-Wei¹²³⁴⁵,Shuai Lin⁶⁷⁸⁹⁵,He Hai-Bing¹⁰¹¹¹²⁵,Pan Na¹²³⁴⁵,Gao Li-Xin⁶⁷⁸⁹⁵,Yu Li-Fang¹²³⁴⁵,Li Jia⁶⁷⁸⁹⁵,Li Jing-Ya⁶⁷⁸⁹⁵,Yang Fan¹²³⁴⁵

Affiliation:

1. MTDD

2. School of Chemistry and Molecular Engineering

3. East China Normal University

4. Shanghai 200062

5. China

6. National Center for Drug Screening

7. Shanghai Institute of Materia Medica

8. Chinese Academy of Science

9. Shanghai 201203

10. Chemistry and Chemical Engineering

11. Nantong University

12. Jiangsu 226019

Abstract

Fourteen 2,3-pyrazole ring-substituted 4,4-dimethyl lithocholic acid derivatives were designed and synthesized as novel PTP1B inhibitors with good potency, selectivity as well as cell permeability.

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemical Engineering,General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2015/RA/C5RA20238H

Reference20 articles.

1. Insulin signalling and the regulation of glucose and lipid metabolism

2. Protein-Tyrosine Phosphatase 1B Complexes with the Insulin Receptor in Vivo and Is Tyrosine-phosphorylated in the Presence of Insulin

3. Tyrosine Dephosphorylation and Deactivation of Insulin Receptor Substrate-1 by Protein-tyrosine Phosphatase 1B

4. Alterations in skeletal muscle protein-tyrosine phosphatase activity and expression in insulin-resistant human obesity and diabetes.

5. Increased abundance of specific skeletal muscle protein-tyrosine phosphatases in a genetic model of insulin-resistant obesity and diabetes mellitus

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