| pubmed-article:16789735 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:16789735 | lifeskim:mentions | umls-concept:C0038760 | lld:lifeskim |
| pubmed-article:16789735 | lifeskim:mentions | umls-concept:C0070948 | lld:lifeskim |
| pubmed-article:16789735 | lifeskim:mentions | umls-concept:C0908145 | lld:lifeskim |
| pubmed-article:16789735 | lifeskim:mentions | umls-concept:C0332256 | lld:lifeskim |
| pubmed-article:16789735 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:16789735 | lifeskim:mentions | umls-concept:C0920591 | lld:lifeskim |
| pubmed-article:16789735 | lifeskim:mentions | umls-concept:C0053183 | lld:lifeskim |
| pubmed-article:16789735 | lifeskim:mentions | umls-concept:C1743045 | lld:lifeskim |
| pubmed-article:16789735 | pubmed:issue | 13 | lld:pubmed |
| pubmed-article:16789735 | pubmed:dateCreated | 2006-6-22 | lld:pubmed |
| pubmed-article:16789735 | pubmed:abstractText | Potent nonpeptidic benzimidazole sulfonamide inhibitors of protein tyrosine phosphatase 1B (PTP1B) were derived from the optimization of a tripeptide containing the novel (S)-isothiazolidinone ((S)-IZD) phosphotyrosine (pTyr) mimetic. An X-ray cocrystal structure of inhibitor 46/PTP1B at 1.8 A resolution demonstrated that the benzimidazole sulfonamides form a bidentate H bond to Asp48 as designed, although the aryl group of the sulfonamide unexpectedly interacts intramolecularly in a pi-stacking manner with the benzimidazole. The ortho substitution to the (S)-IZD on the aryl ring afforded low nanomolar enzyme inhibitors of PTP1B that also displayed low caco-2 permeability and cellular activity in an insulin receptor (IR) phosphorylation assay and an Akt phosphorylation assay. The design, synthesis, and SAR of this novel series of benzimidazole sulfonamide containing (S)-IZD inhibitors of PTP1B are presented herein. | lld:pubmed |
| pubmed-article:16789735 | pubmed:language | eng | lld:pubmed |
| pubmed-article:16789735 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16789735 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:16789735 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16789735 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16789735 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16789735 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16789735 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16789735 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:16789735 | pubmed:month | Jun | lld:pubmed |
| pubmed-article:16789735 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:16789735 | pubmed:author | pubmed-author:WynnRichardR | lld:pubmed |
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| pubmed-article:16789735 | pubmed:author | pubmed-author:WeiMinM | lld:pubmed |
| pubmed-article:16789735 | pubmed:author | pubmed-author:CombsAndrew... | lld:pubmed |
| pubmed-article:16789735 | pubmed:author | pubmed-author:SparksRichard... | lld:pubmed |
| pubmed-article:16789735 | pubmed:author | pubmed-author:ZhuWenyuW | lld:pubmed |
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| pubmed-article:16789735 | pubmed:author | pubmed-author:MetcalfBrianB | lld:pubmed |
| pubmed-article:16789735 | pubmed:author | pubmed-author:EllisDawnD | lld:pubmed |
| pubmed-article:16789735 | pubmed:author | pubmed-author:ReidBrian MBM | lld:pubmed |
| pubmed-article:16789735 | pubmed:author | pubmed-author:EmmThomasT | lld:pubmed |
| pubmed-article:16789735 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:16789735 | pubmed:day | 29 | lld:pubmed |
| pubmed-article:16789735 | pubmed:volume | 49 | lld:pubmed |
| pubmed-article:16789735 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:16789735 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:16789735 | pubmed:pagination | 3774-89 | lld:pubmed |
| pubmed-article:16789735 | pubmed:dateRevised | 2009-11-19 | lld:pubmed |
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| pubmed-article:16789735 | pubmed:year | 2006 | lld:pubmed |
| pubmed-article:16789735 | pubmed:articleTitle | Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic. | lld:pubmed |
| pubmed-article:16789735 | pubmed:affiliation | Incyte Corporation, Discovery Chemistry, Applied Technology, and Drug Metabolism, Experimental Station, Route 141 and Henry Clay Road, Wilmington, Delaware 19880, USA. acombs@incyte.com | lld:pubmed |
| pubmed-article:16789735 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:16789735 | lld:chembl |
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