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Heterogeneous effect of saxagliptin on glucose fluctuation and β-cell function in T1DM: a multicentre, randomised trial. [PDF]
Shi Y +20 more
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Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Letters, 2004Amides derived from fluorinated pyrrolidines and 4-substituted cyclohexylglycine analogues have been prepared and evaluated as inhibitors of dipeptidyl dipeptidase IV (DP-IV). Analogues which incorporated (S)-3-fluoropyrrolidine showed good selectivity for DP-IV over quiescent cell proline dipeptidase (QPP).
Charles G, Caldwell +13 more
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Recent patents of dipeptidyl peptidase IV inhibitors
Expert Opinion on Therapeutic Patents, 2011The serine exopeptidase DPP IV is a dual protein able to work as an enzyme and an interacting protein. The incretin molecules glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) are hydrolyzed by DPP IV into inactive forms, which are unable to promote insulin secretion.
Laura, Mendieta +2 more
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Azetidine-Based Inhibitors of Dipeptidyl Peptidase IV (DPP IV)
Current Topics in Medicinal Chemistry, 2007The structure-activity relationships of azetidine-based DPP IV inhibitors will be discussed in detail in the following review. The azetidine-based DPP IV inhibitors can be divided into three main subtypes, the 2-cyanoazetidines, 3-fluoroazetidines and 2-ketoazetidines.
Dana, Ferraris +8 more
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Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Letters, 2005Dipeptidyl peptidase IV (DPP4) is a multifunctional type II transmembrane serine peptidase which regulates various physiological processes, most notably plasma glucose homeostasis by cleaving peptide hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide.
Guohua, Zhao +11 more
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Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Letters, 2007The synthesis and structure-activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with beta-branched natural and unnatural amino acids, particularly adamantylglycines, linked to a (2S,3R)-2,3 ...
Ligaya M, Simpkins +21 more
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Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors
Bioorganic & Medicinal Chemistry Letters, 2009A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. The potency, selectivity, cross-species DMPK profiles, and in vivo efficacy of 34 is reported.
Scott D, Edmondson +15 more
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Sitagliptin, a Dipeptidyl Peptidase-IV Inhibitor, Improves Psoriasis
Dermatology, 2011A patient with a 17-year history of plaque psoriasis accompanied by type 2 diabetes mellitus discontinued cyclosporine and steroid ointment given for treatment of psoriasis because she was dissatisfied with the effects of the drugs. After sitagliptin, a dipeptidyl peptidase-IV (DPP-IV) inhibitor, was administered for control of blood glucose, psoriatic
Tatsuya, Nishioka +4 more
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A potent dipeptide inhibitor of dipeptidyl peptidase IV
Bioorganic & Medicinal Chemistry Letters, 1998A series of novel potent inhibitors of dipeptidyl peptidase IV (DPP-IV) has been developed. A brief structure-activity relationship of the inhibitors was investigated. The dipeptide TSL-225, tryptophyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, was identified with the critical structure for the inhibitory activity.
M, Yamada +5 more
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