Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes. / Deacon, Carolyn F.

In: Peptides, Vol. 100, 02.2018, p. 150-157.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Deacon, CF 2018, 'Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes', Peptides, vol. 100, pp. 150-157. https://doi.org/10.1016/j.peptides.2017.10.011

APA

Deacon, C. F. (2018). Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes. Peptides, 100, 150-157. https://doi.org/10.1016/j.peptides.2017.10.011

Vancouver

Deacon CF. Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes. Peptides. 2018 Feb;100:150-157. https://doi.org/10.1016/j.peptides.2017.10.011

Author

Deacon, Carolyn F. / Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes. In: Peptides. 2018 ; Vol. 100. pp. 150-157.

Bibtex

@article{961422150b864ad7b8d9e4c8c762b4c2,
title = "Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes",
abstract = "Dipeptidyl peptidase-4 (DPP-4) inhibitors are now a widely used, safe and efficacious class of antidiabetic drugs, which were developed prospectively using a rational drug design approach based on a thorough understanding of the endocrinology and degradation of glucagon-like peptide-1 (GLP-1). GLP-1 is an intestinal hormone with potent insulinotropic and glucagonostatic effects and can normalise blood glucose levels in patients with type 2 diabetes, but the native peptide is not therapeutically useful because of its inherent metabolic instability. Using the GLP-1/DPP-4 system and type 2 diabetes as an example, this review summarises how knowledge of a peptide's biological effects coupled with an understanding of the pathways involved in its metabolic clearance can be exploited in a rational, step-by-step manner to develop a therapeutic agent, which is effective and well tolerated, and any side effects are minor and largely predictable. Other peptides with metabolic effects which can also be degraded by DPP-4 will be reviewed, and their potential role as additional mediators of the effects of DPP-4 inhibitors will be assessed.",
keywords = "Dipeptidyl peptidase.4, Glucagon-like peptide-1, Incretin, Peptide degradation, Therapy, Type 2 diabetes",
author = "Deacon, {Carolyn F}",
note = "Copyright {\circledC} 2017 Elsevier Inc. All rights reserved.",
year = "2018",
month = "2",
doi = "10.1016/j.peptides.2017.10.011",
language = "English",
volume = "100",
pages = "150--157",
journal = "Peptides",
issn = "0196-9781",
publisher = "Elsevier",

}

RIS

TY - JOUR

T1 - Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes

AU - Deacon, Carolyn F

N1 - Copyright © 2017 Elsevier Inc. All rights reserved.

PY - 2018/2

Y1 - 2018/2

N2 - Dipeptidyl peptidase-4 (DPP-4) inhibitors are now a widely used, safe and efficacious class of antidiabetic drugs, which were developed prospectively using a rational drug design approach based on a thorough understanding of the endocrinology and degradation of glucagon-like peptide-1 (GLP-1). GLP-1 is an intestinal hormone with potent insulinotropic and glucagonostatic effects and can normalise blood glucose levels in patients with type 2 diabetes, but the native peptide is not therapeutically useful because of its inherent metabolic instability. Using the GLP-1/DPP-4 system and type 2 diabetes as an example, this review summarises how knowledge of a peptide's biological effects coupled with an understanding of the pathways involved in its metabolic clearance can be exploited in a rational, step-by-step manner to develop a therapeutic agent, which is effective and well tolerated, and any side effects are minor and largely predictable. Other peptides with metabolic effects which can also be degraded by DPP-4 will be reviewed, and their potential role as additional mediators of the effects of DPP-4 inhibitors will be assessed.

AB - Dipeptidyl peptidase-4 (DPP-4) inhibitors are now a widely used, safe and efficacious class of antidiabetic drugs, which were developed prospectively using a rational drug design approach based on a thorough understanding of the endocrinology and degradation of glucagon-like peptide-1 (GLP-1). GLP-1 is an intestinal hormone with potent insulinotropic and glucagonostatic effects and can normalise blood glucose levels in patients with type 2 diabetes, but the native peptide is not therapeutically useful because of its inherent metabolic instability. Using the GLP-1/DPP-4 system and type 2 diabetes as an example, this review summarises how knowledge of a peptide's biological effects coupled with an understanding of the pathways involved in its metabolic clearance can be exploited in a rational, step-by-step manner to develop a therapeutic agent, which is effective and well tolerated, and any side effects are minor and largely predictable. Other peptides with metabolic effects which can also be degraded by DPP-4 will be reviewed, and their potential role as additional mediators of the effects of DPP-4 inhibitors will be assessed.

KW - Dipeptidyl peptidase.4

KW - Glucagon-like peptide-1

KW - Incretin

KW - Peptide degradation

KW - Therapy

KW - Type 2 diabetes

UR - http://www.scopus.com/inward/record.url?scp=85041483511&partnerID=8YFLogxK

U2 - 10.1016/j.peptides.2017.10.011

DO - 10.1016/j.peptides.2017.10.011

M3 - Journal article

VL - 100

SP - 150

EP - 157

JO - Peptides

JF - Peptides

SN - 0196-9781

ER -

ID: 189765215