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Volumn 22, Issue 3, 2012, Pages 1464-1468

Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes

Author keywords

DPP 4 inhibitor; Type 2 diabetes

Indexed keywords

ANTIDIABETIC AGENT; DIPEPTIDYL PEPTIDASE; DIPEPTIDYL PEPTIDASE IV INHIBITOR;

EID: 84856210285     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.11.054     Document Type: Article
Times cited : (65)

References (25)
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    • note
    • Compounds were tested for their inhibitory potency against human DPP-4. Human DPP-4 (amino acids 39-766) with a C-terminal step-tag was expressed using the baculovirus system and purified to >80%, and stored in a 25 mM Tris buffer, pH 9, containing 300 mM NaCl at -80 °C. The substrate was kept at 5 mM stock solution in DMSO at -20 °C and the assay buffer for the DPP-4 reaction was 25 nM Tris/HCl, pH 7.5, containing 140 mM NaCl, 10 mM KCl and 0.05% (w/v) CHAPS.
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    • This observed boost in affinity moving from piperazine to aminopiperidine has been rationalised in terms of an additional hydrogen bonding ability and lower energy conformation
    • This observed boost in affinity moving from piperazine to aminopiperidine has been rationalised in terms of an additional hydrogen bonding ability and lower energy conformation: M. Engel, T. Hoffmann, S. Manhart, U. Heiser, S. Chambre, R. Huber, H.-U. Demuth, and W. Bode J. Mol. Biol. 356 2006 768
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* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.