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Peptidomimetics as Potent and Selective PTP1B Inhibitors

[ Vol. 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   Pages 660 - 671 ( 12 )

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.

Affiliation:

Zydus Research Centre, Sarkhej-Bavla, N.H. 8A Moraiya, Ahmedabad-382210, India.



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