2nt7: Difference between revisions

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[[Image:2nt7.gif|left|200px]]
{{Seed}}
[[Image:2nt7.png|left|200px]]


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{{STRUCTURE_2nt7|  PDB=2nt7  |  SCENE=  }}  
{{STRUCTURE_2nt7|  PDB=2nt7  |  SCENE=  }}  


'''Crystal structure of PTP1B-inhibitor complex'''
===Crystal structure of PTP1B-inhibitor complex===




==Overview==
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The following account describes our systematic effort to replace one of the carboxylate groups of our diacid thiophene PTP1B inhibitors. Active hits were validated using enzymatic assays before pursuing efforts to improve the potency. Only when the C2 carboxylic acid was replaced with another ionizable functional group was reversible and competitive inhibition retained. Use of a tetrazole ring or 1,2,5-thiadiazolidine-3-one-1,1-dioxide as a carboxylate mimetic led to the discovery of two unique starting series that showed improved permeability (PAMPA) and potency of the order of 300nM. The SAR from these efforts underscores some of the major challenges in developing small molecule inhibitors for PTP1B.
The line below this paragraph, {{ABSTRACT_PUBMED_17336064}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 17336064 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17336064}}


==About this Structure==
==About this Structure==
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[[Category: Protein-inhibitor complex]]
[[Category: Protein-inhibitor complex]]
[[Category: Ptp1b]]
[[Category: Ptp1b]]
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