2oqi
From Proteopedia
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==Overview== | ==Overview== | ||
| - | Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of | + | 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. |
==About this Structure== | ==About this Structure== | ||
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==Reference== | ==Reference== | ||
| - | Discovery and | + | 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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17367123 17367123] |
[[Category: Dipeptidyl-peptidase IV]] | [[Category: Dipeptidyl-peptidase IV]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Backes, B | + | [[Category: Backes, B J.]] |
| - | [[Category: Ballaron, S | + | [[Category: Ballaron, S J.]] |
| - | [[Category: Beno, D | + | [[Category: Beno, D W.]] |
| - | [[Category: Geldern, T | + | [[Category: Geldern, T W.von.]] |
| - | [[Category: Kempf-Grote, A | + | [[Category: Kempf-Grote, A J.]] |
[[Category: Lai, C.]] | [[Category: Lai, C.]] | ||
[[Category: Li, X.]] | [[Category: Li, X.]] | ||
| - | [[Category: Longenecker, K | + | [[Category: Longenecker, K L.]] |
| - | [[Category: Lubben, T | + | [[Category: Lubben, T H.]] |
[[Category: Pei, Z.]] | [[Category: Pei, Z.]] | ||
[[Category: Pireh, D.]] | [[Category: Pireh, D.]] | ||
| - | [[Category: Sham, H | + | [[Category: Sham, H L.]] |
| - | [[Category: Stewart, K | + | [[Category: Stewart, K D.]] |
| - | [[Category: Trevillyan, J | + | [[Category: Trevillyan, J M.]] |
[[Category: GGO]] | [[Category: GGO]] | ||
[[Category: inhibitor]] | [[Category: inhibitor]] | ||
[[Category: serine-peptidase]] | [[Category: serine-peptidase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:21:24 2008'' |
Revision as of 16:21, 21 February 2008
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Human Dipeptidyl Peptidase IV (DPP4) with Piperidinone-constrained phenethylamine
Overview
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.
About this Structure
2OQI is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 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 Thu Feb 21 18:21:24 2008
Categories: Dipeptidyl-peptidase IV | Homo sapiens | Single protein | Backes, B J. | Ballaron, S J. | Beno, D W. | Geldern, T W.von. | Kempf-Grote, A J. | Lai, C. | Li, X. | Longenecker, K L. | Lubben, T H. | Pei, Z. | Pireh, D. | Sham, H L. | Stewart, K D. | Trevillyan, J M. | GGO | Inhibitor | Serine-peptidase
