Peptidomimetics as Potent and Selective PTP1B Inhibitors

Dipam      Patel; Mukul      Jain; Shailesh   R.   Shah; Rajesh      Bahekar; Pradip      Jadav; Kiran      Shah; Amit      Joharapurkar; Mubeen      Shaikh; Kalapatapu   V.V.M.   Sairam

doi:10.2174/1573406411309050005

Abstract

A series of peptidomimetic containing bidentate pTyr mimetics (9a-w) are reported as potent and selective PTP1B inhibitors. Compounds (9p and 9q) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (in vitro), which confirms discovery of highly potent and selective PTP1B inhibitors.

Keywords: Tri-peptides, pTyr mimetics, PTP1B inhibitors, TCPTP, Type 2 diabetes, Metabolic disorders.

« Previous Next »

Rights & Permissions Print Cite

Medicinal Chemistry

Title:Peptidomimetics as Potent and Selective PTP1B Inhibitors

Volume: 9 Issue: 5

Author(s): Dipam Patel, Mukul Jain, Shailesh R. Shah, Rajesh Bahekar, Pradip Jadav, Kiran Shah, Amit Joharapurkar, Mubeen Shaikh and Kalapatapu V.V.M. Sairam

Affiliation:

Keywords: Tri-peptides, pTyr mimetics, PTP1B inhibitors, TCPTP, Type 2 diabetes, Metabolic disorders.

Abstract: A series of peptidomimetic containing bidentate pTyr mimetics (9a-w) are reported as potent and selective PTP1B inhibitors. Compounds (9p and 9q) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (in vitro), which confirms discovery of highly potent and selective PTP1B inhibitors.

Export Options

Export File:

RIS (for EndNote, Reference Manager, ProCite)

BibTeX

Text

Content:

Citation Only

Citation and Abstract

About this article

Cite this article as:

Patel Dipam, Jain Mukul, Shah R. Shailesh, Bahekar Rajesh, Jadav Pradip, Shah Kiran, Joharapurkar Amit, Shaikh Mubeen and Sairam V.V.M. Kalapatapu, Peptidomimetics as Potent and Selective PTP1B Inhibitors, Medicinal Chemistry 2013; 9 (5) . https://dx.doi.org/10.2174/1573406411309050005