Structure-based design of protein tyrosine phosphatase-1B inhibitors

Emma Black; Jason Breed; Alexander L Breeze; Kevin Embrey; Robert Garcia; Thomas W Gero; Linda Godfrey; Peter W Kenny; Andrew D Morley; Claire A Minshull; Andrew D Pannifer; Jon Read; Amanda Rees; Daniel J Russell; Dorin Toader; Julie Tucker

doi:10.1016/j.bmcl.2005.03.068

Structure-based design of protein tyrosine phosphatase-1B inhibitors

Bioorg Med Chem Lett. 2005 May 16;15(10):2503-7. doi: 10.1016/j.bmcl.2005.03.068.

Authors

Emma Black¹, Jason Breed, Alexander L Breeze, Kevin Embrey, Robert Garcia, Thomas W Gero, Linda Godfrey, Peter W Kenny, Andrew D Morley, Claire A Minshull, Andrew D Pannifer, Jon Read, Amanda Rees, Daniel J Russell, Dorin Toader, Julie Tucker

Affiliation

¹ AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.

PMID: 15863305
DOI: 10.1016/j.bmcl.2005.03.068

Abstract

Using structure-based design, a new class of inhibitors of protein tyrosine phosphatase-1B (PTP1B) has been identified, which incorporate the 1,2,5-thiadiazolidin-3-one-1,1-dioxide template.

MeSH terms

Crystallography, X-Ray
Drug Design
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Ligands
Magnetic Resonance Spectroscopy
Molecular Conformation
Protein Tyrosine Phosphatase, Non-Receptor Type 1
Protein Tyrosine Phosphatases / antagonists & inhibitors*
Structure-Activity Relationship
Thiadiazines / chemistry*
Thiadiazines / pharmacology*

Substances

Enzyme Inhibitors
Ligands
Thiadiazines
Protein Tyrosine Phosphatase, Non-Receptor Type 1
Protein Tyrosine Phosphatases