Medicinal chemistry of non-peptidomimetic dipeptidyl peptidase IV (DPP IV) inhibitors for treatment of Type-2 diabetes mellitus: Insights on recent development

Germinated chickpea protein ficin hydrolysate and its peptides inhibited glucose uptake and affected the bitter receptor signaling pathway in vitro

“…The S1 region is primarily composed of hydrophobic amino acids, whereas the N-terminus contains hydrophilic residues. 32 A mixture of peptides is therefore more favorable than pure peptides in effectively inhibiting the action of DPP-IV, as more peptides are available to bind to the active sites of DPP-IV.…”

“…30 Molecular docking sites were determined using previously identified active sites of the respective markers. [32][33][34][35][36][37][38][39][40] Visualizations were prepared to identify docking patterns, specifically the different types of interactions and the strongest contributors to inhibition or activation of the specific marker. The energy of affinity with the active site was determined and visualized using Discovery Studio v4.1 (Waltham, MA, USA).…”

GLP-1 Analogs, SGLT-2, and DPP-4 Inhibitors: A Triad of Hope for Alzheimer’s Disease Therapy

“…Dipeptidyl peptidase-4 (DPP-4), also known as CD26, made its initial appearance in scientific literature in 1966 as an enzyme endowed with the capacity to cleave dipeptides from the N-terminus of substrates containing proline and, to some extent, alanine at the penultimate position. This is particularly relevant in substrates such as GLP-1 and GIP [185,186]. Structurally, DPP-4 takes the form of a type II transmembrane serine protease, comprising two identical 110 kDa subunits interconnected through non-covalent interactions [187,188].…”

Pharmaceutical Food Science: Search for Bio-Functional Molecules Obtained from Natural Resources to Prevent and Ameliorate Lifestyle Diseases

“…Gliptins, such as sitagliptin, vildagliptin, saxagliptin, and alogliptin, are the currently available DPP-4 inhibitors approved for T2DM. [47][48][49][50] We found that a methanol extract of "Everlasting Flower," the flowers of Helichrysum arenarium (L.) Moench (common names; dwarf everlasting and immortelle) was found to inhibit Toshio Morikawa blood glucose elevation in sucrose-loaded mice as well as the enzymatic activity against DPP-4 (IC 50 = 41.2 µg/mL). 51,52) During the MONOTORI study of the extract, [53][54][55] we obtained new compounds having unusual structures for natural products, e.g., everlastosides A ( 5) and B ( 6), megastigman glycosides having a γ-lactone linkage between C-5 and C-12, 54) and arenariumoside VI (7) and related analogs (arenariumosides V and VII), dimeric dihydrocalcone glycosides 51) (Fig.…”