1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors

High-throughput screening of the P&GP corporate repository against several protein tyrosine phosphatases identified the sulfamic acid moiety as potential phosphotyrosine mimetic. Incorporation of the sulfamic acid onto a 1,2,3,4-tetrahydroisoquinoline scaffold provided a promising starting point...

Full description

Saved in:

Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 16; no. 6; pp. 1574 - 1578
Main Authors:	Klopfenstein, Sean R., Evdokimov, Artem G., Colson, Anny-Odile, Fairweather, Neil T., Neuman, Jeffrey J., Maier, Matthew B., Gray, Jeffrey L., Gerwe, Gina S., Stake, George E., Howard, Brian W., Farmer, Julie A., Pokross, Matthew E., Downs, Thomas R., Kasibhatla, Bhavani, Peters, Kevin G.
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 15-03-2006 Elsevier
Subjects:	Binding Sites Binding, Competitive Biological and medical sciences Crystallography, X-Ray Diabetes Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology General and cellular metabolism. Vitamins HTS screening Humans Ligands Medical sciences Models, Molecular Molecular Mimicry Pharmacology. Drug treatments Phosphatase PTP1B Phosphotyrosine - metabolism Protein Binding Protein Tyrosine Phosphatase, Non-Receptor Type 1 Protein Tyrosine Phosphatases - antagonists & inhibitors Protein Tyrosine Phosphatases - chemistry Protein Tyrosine Phosphatases - metabolism src Homology Domains Structure-Activity Relationship Sulfamic acid Sulfonic Acids - chemical synthesis Sulfonic Acids - chemistry Sulfonic Acids - pharmacology Tetrahydroisoquinoline Tetrahydroisoquinolines - chemistry HTS screening Diabetes Phosphatase PTP1B Sulfamic acid Tetrahydroisoquinoline High throughput screening Isoquinoline derivatives Enzyme Nitrogen heterocycle Phosphoric monoester hydrolases Enzyme inhibitor Esterases Inhibitor enzyme complex Amidosulfates In vitro Modeling Structure activity relation Molecular model Bicyclic compound Hydrolases Amidosulfuric acid Aromatic compound Protein-tyrosine-phosphatase
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	High-throughput screening of the P&GP corporate repository against several protein tyrosine phosphatases identified the sulfamic acid moiety as potential phosphotyrosine mimetic. Incorporation of the sulfamic acid onto a 1,2,3,4-tetrahydroisoquinoline scaffold provided a promising starting point for PTP1B inhibitor design.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.12.051