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Inhibitors of dipeptidyl peptidase IV: a novel approach for the prevention and treatment of Type 2 diabetes?

Deacon, CF; Ahrén, Bo LU and Holst, JJ (2004) In Expert Opinion on Investigational Drugs 13(9). p.1091-1102
Abstract
Inhibitors of the enzyme dipeptidyl peptidase IV (DPP IV) are of increasing interest to both diabetologists and the pharmaceutical industry alike, as they may become established as the next member of the oral antidiabetic class of therapeutic agents, designed to lower blood glucose and, possibly, prevent the progressive impairment of glucose metabolism in patients with impaired glucose tolerance and Type 2 diabetes. DPP IV has become a focus of attention for drug design, as it has a pivotal role in the rapid degradation of at least two of the hormones released during food ingestion, a property that has warranted the design of inhibitor-based drugs. At the molecular level, DPP IV cleaves two amino acids from the N-terminus of the intact,... (More)
Inhibitors of the enzyme dipeptidyl peptidase IV (DPP IV) are of increasing interest to both diabetologists and the pharmaceutical industry alike, as they may become established as the next member of the oral antidiabetic class of therapeutic agents, designed to lower blood glucose and, possibly, prevent the progressive impairment of glucose metabolism in patients with impaired glucose tolerance and Type 2 diabetes. DPP IV has become a focus of attention for drug design, as it has a pivotal role in the rapid degradation of at least two of the hormones released during food ingestion, a property that has warranted the design of inhibitor-based drugs. At the molecular level, DPP IV cleaves two amino acids from the N-terminus of the intact, biologically active forms of both so-called incretin hormones, glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide (formerly known as gastric inhibitory polypeptide), resulting in truncated metabolites, which are largely inactive. Inhibition of the enzyme, therefore, is thought to increase levels of the active forms of both incretin hormones, culminating in an increase in insulin release after a meal, in a fully glucosedependant manner. DPP IV inhibitors combine several features of interest to the drug design process. They can be readily optimised for their target and be designed as low molecular weight, orally active entities compatible with once-daily administration. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
glucose-dependent insulinotropic polypeptide, glucagon-like peptide-1, enzyme inhibitor, dipeptidyl peptidase, enteroinsular axis, incretin, oral antidiabetic agent
in
Expert Opinion on Investigational Drugs
volume
13
issue
9
pages
1091 - 1102
publisher
Ashley Publications
external identifiers
  • wos:000223845700001
  • pmid:15330741
  • scopus:4544232468
ISSN
1744-7658
DOI
10.1517/13543784.13.9.1091
language
English
LU publication?
yes
id
c568dfbf-762b-43eb-b450-bab663729817 (old id 267484)
date added to LUP
2007-10-23 10:34:15
date last changed
2017-11-05 03:48:12
@article{c568dfbf-762b-43eb-b450-bab663729817,
  abstract     = {Inhibitors of the enzyme dipeptidyl peptidase IV (DPP IV) are of increasing interest to both diabetologists and the pharmaceutical industry alike, as they may become established as the next member of the oral antidiabetic class of therapeutic agents, designed to lower blood glucose and, possibly, prevent the progressive impairment of glucose metabolism in patients with impaired glucose tolerance and Type 2 diabetes. DPP IV has become a focus of attention for drug design, as it has a pivotal role in the rapid degradation of at least two of the hormones released during food ingestion, a property that has warranted the design of inhibitor-based drugs. At the molecular level, DPP IV cleaves two amino acids from the N-terminus of the intact, biologically active forms of both so-called incretin hormones, glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide (formerly known as gastric inhibitory polypeptide), resulting in truncated metabolites, which are largely inactive. Inhibition of the enzyme, therefore, is thought to increase levels of the active forms of both incretin hormones, culminating in an increase in insulin release after a meal, in a fully glucosedependant manner. DPP IV inhibitors combine several features of interest to the drug design process. They can be readily optimised for their target and be designed as low molecular weight, orally active entities compatible with once-daily administration.},
  author       = {Deacon, CF and Ahrén, Bo and Holst, JJ},
  issn         = {1744-7658},
  keyword      = {glucose-dependent insulinotropic polypeptide,glucagon-like peptide-1,enzyme inhibitor,dipeptidyl peptidase,enteroinsular axis,incretin,oral antidiabetic agent},
  language     = {eng},
  number       = {9},
  pages        = {1091--1102},
  publisher    = {Ashley Publications},
  series       = {Expert Opinion on Investigational Drugs},
  title        = {Inhibitors of dipeptidyl peptidase IV: a novel approach for the prevention and treatment of Type 2 diabetes?},
  url          = {http://dx.doi.org/10.1517/13543784.13.9.1091},
  volume       = {13},
  year         = {2004},
}