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The design of enzyme inhibitors is a pragmatic approach to drug design; being compatible with the identification and optimization of small molecules that have properties commensurate with oral administration, as well as acceptable drug metabolism, distribution and elimination characteristics. Glucagon\u2010like peptide\u00a01 (<jats:styled-content style=\"fixed-case\">GLP<\/jats:styled-content><jats:italic>\u2010<\/jats:italic>1), a hormone with a spectrum of favourable metabolic actions, including glucose\u2010dependent stimulation of insulin and inhibition of glucagon secretion, provided the endocrine basis from which the idea of using <jats:styled-content style=\"fixed-case\">DPP<\/jats:styled-content><jats:italic>\u2010<\/jats:italic>4 inhibitors as anti\u2010diabetic agents was developed. The origin of the <jats:styled-content style=\"fixed-case\">DPP<\/jats:styled-content><jats:italic>\u2010<\/jats:italic>4 inhibitor concept was inspired by the angiotensin\u2010converting enzyme inhibitor approach, which succeeded in establishing a class of extensively used therapeutic agents for the treatment of cardiovascular disorders.<\/jats:p>","DOI":"10.1111\/dme.13066","type":"journal-article","created":{"date-parts":[[2016,1,16]],"date-time":"2016-01-16T18:16:12Z","timestamp":1452968172000},"page":"718-722","update-policy":"http:\/\/dx.doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Drug development from the bench to the pharmacy: with special reference to dipeptidyl peptidase<i>\u2010<\/i>4 inhibitor development"],"prefix":"10.1111","volume":"33","author":[{"given":"R. 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