2oqi

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{{STRUCTURE_2oqi| PDB=2oqi | SCENE= }}
{{STRUCTURE_2oqi| PDB=2oqi | SCENE= }}
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'''Human Dipeptidyl Peptidase IV (DPP4) with Piperidinone-constrained phenethylamine'''
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===Human Dipeptidyl Peptidase IV (DPP4) with Piperidinone-constrained phenethylamine===
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==Overview==
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Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of therapeutic agents for the treatment of type 2 diabetes. They exert their beneficial effects by increasing the levels of active glucagon-like peptide-1 and glucose-dependent insulinotropic peptide, which are two important incretins for glucose homeostasis. Starting from a high-throughput screening hit, we were able to identify a series of piperidinone- and piperidine-constrained phenethylamines as novel DPP4 inhibitors. Optimized compounds are potent, selective, and have good pharmacokinetic profiles.
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{{ABSTRACT_PUBMED_17367123}}
==About this Structure==
==About this Structure==
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[[Category: Inhibitor]]
[[Category: Inhibitor]]
[[Category: Serine-peptidase]]
[[Category: Serine-peptidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:27:31 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 07:33:39 2008''

Revision as of 04:33, 29 July 2008

Image:2oqi.png

Template:STRUCTURE 2oqi

Human Dipeptidyl Peptidase IV (DPP4) with Piperidinone-constrained phenethylamine

Template:ABSTRACT PUBMED 17367123

About this Structure

2OQI is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors., Pei Z, Li X, von Geldern TW, Longenecker K, Pireh D, Stewart KD, Backes BJ, Lai C, Lubben TH, Ballaron SJ, Beno DW, Kempf-Grote AJ, Sham HL, Trevillyan JM, J Med Chem. 2007 Apr 19;50(8):1983-7. Epub 2007 Mar 17. PMID:17367123

Page seeded by OCA on Tue Jul 29 07:33:39 2008

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