PAIN-less identification and evaluation of small molecule inhibitors against protein tyrosine phosphatase 1B-Reference-Cited by-同舟云学术

PAIN-less identification and evaluation of small molecule inhibitors against protein tyrosine phosphatase 1B

Published:2017 Issue:6 Volume:8 Page:1220-1224
ISSN:2040-2503
Container-title:MedChemComm
language:en
Short-container-title:Med. Chem. Commun.

Author:

Nasiri Hamid R.¹²³^ORCID,Mracek Philipp¹²³,Grimm Steffen K.¹²³,Gastaldello Janine¹²³,Kolodzik Adrian¹²³,Ullmann Dirk¹²³

Affiliation:

1. Evotec AG

2. D-22419 Hamburg

3. Germany

Abstract

A miniaturized assay was set up to test a set of natural products against protein tyrosine phosphatase 1B (PTP1B). By using several read-out and counter assays, berberine and palmatine were identified as PAINS (pan-assay interference compounds) and α-TOS as a novel inhibitor of PTP1B.

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2017/MD/C7MD00126F

Reference35 articles.

1. Prospects for Inhibitors of Protein Tyrosine Phosphatase 1B as Antidiabetic Drugs

2. Increased Insulin Sensitivity and Obesity Resistance in Mice Lacking the Protein Tyrosine Phosphatase-1B Gene

3. Increased Energy Expenditure, Decreased Adiposity, and Tissue-Specific Insulin Sensitivity in Protein-Tyrosine Phosphatase 1B-Deficient Mice

4. Recent Advances in the Discovery of Competitive Protein Tyrosine Phosphatase 1B Inhibitors for the Treatment of Diabetes, Obesity, and Cancer

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