التفاصيل البيبلوغرافية
العنوان:
Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors
المؤلفون:
E. Michael August , Lana Louise Smith Keenan , Jun Li , S. Mariana Margarit , Alexander Heim-Riether , Hans-Dieter Junker , Kathleen Haverty , Neil A. Farrow , Brandon Collins , Bennett T. Farmer , Thomas Neumann , Shuang Liang , John R. Proudfoot , Renate Sekul , Qiang Zhang , Donghong Amy Gao , Steven John Taylor , Zhaoming Xiong , Neil Moss , Melissa Hill-Drzewi
المصدر:
Bioorganic & Medicinal Chemistry Letters . 19:5321-5324
بيانات النشر:
Elsevier BV, 2009.
سنة النشر:
2009
مصطلحات موضوعية:
Models, Molecular , Matrix metalloproteinase inhibitor , medicine.drug_class , Stereochemistry , Clinical Biochemistry , Pharmaceutical Science , Carboxamide , Matrix Metalloproteinase Inhibitors , Biochemistry , Structure-Activity Relationship , Catalytic Domain , Matrix Metalloproteinase 13 , Drug Discovery , medicine , Potency , Structure–activity relationship , Protease Inhibitors , Molecular Biology , Chelating Agents , chemistry.chemical_classification , biology , Organic Chemistry , Active site , Enzyme , chemistry , Enzyme inhibitor , biology.protein , Molecular Medicine , Selectivity , Protein Binding
الوصف:
Discovery and optimization of potency and selectivity of a non-Zn-chelating MMP-13 inhibitor with the aid of protein co-crystal structural information is reported. This inhibitor was observed to have a binding mode distinct from previously published MMP-13 inhibitors. Potency and selectivity were improved by extending the hit structure out from the active site into the S1' pocket.
تدمد:
0960-894X
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a91cc7f3c887b95e837900c788a1ecfd https://doi.org/10.1016/j.bmcl.2009.07.151
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....a91cc7f3c887b95e837900c788a1ecfd
قاعدة البيانات:
OpenAIRE
