Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes

SH Havale, M Pal - Bioorganic & medicinal chemistry, 2009 - Elsevier
Emerging as an epidemic of the 21st century type 2 diabetes has become a major health
problem throughout the globe. The number of deaths attributable to diabetes reflects the …

Aminoboronic acids and esters: from synthetic challenges to the discovery of unique classes of enzyme inhibitors

S Touchet, F Carreaux, B Carboni, A Bouillon… - Chemical Society …, 2011 - pubs.rsc.org
Although boronic acids have attracted considerable interest as versatile intermediates in
organic synthesis, their contributions in chemical biology and drug discovery programs have …

Targeting fibroblast activation protein inhibits tumor stromagenesis and growth in mice

AM Santos, J Jung, N Aziz, JL Kissil… - The Journal of clinical …, 2009 - Am Soc Clin Investig
Membrane-bound proteases have recently emerged as critical mediators of tumorigenesis,
angiogenesis, and metastasis. However, the mechanisms by which they regulate these …

Selective inhibitors of fibroblast activation protein (FAP) with a (4-quinolinoyl)-glycyl-2-cyanopyrrolidine scaffold

K Jansen, L Heirbaut, JD Cheng… - ACS medicinal …, 2013 - ACS Publications
Fibroblast activation protein (FAP) is a serine protease that is generally accepted to play an
important role in tumor growth and other diseases involving tissue remodeling. Currently …

Molecular recognition of fibroblast activation protein for diagnostic and therapeutic applications

A Šimková, P Bušek, A Šedo, J Konvalinka - Biochimica et Biophysica Acta …, 2020 - Elsevier
Fibroblast activation protein (FAP) is a non-classical serine protease expressed
predominantly in conditions accompanied by tissue remodeling, particularly cancer. Due to …

Selective inhibition of fibroblast activation protein protease based on dipeptide substrate specificity

CY Edosada, C Quan, C Wiesmann, T Tran… - Journal of Biological …, 2006 - ASBMB
Fibroblast activation protein (FAP) is a transmembrane serine peptidase that belongs to the
prolyl peptidase family. FAP has been implicated in cancer; however, its specific role …

DPP-IV inhibitor combined with a further antidiabetic agent, tablets comprising such formulations, their use and process for their preparation

T Friedl, M Braun, K Egusa, H Fujita… - US Patent …, 2015 - Google Patents
US9155705B2 - DPP-IV inhibitor combined with a further antidiabetic agent, tablets
comprising such formulations, their use and process for their preparation - Google Patents …

Imaging of fibroblast activation protein in cancer xenografts using novel (4-quinolinoyl)-glycyl-2-cyanopyrrolidine-based small molecules

SL Slania, D Das, A Lisok, Y Du, Z Jiang… - Journal of medicinal …, 2021 - ACS Publications
Fibroblast activation protein (FAP) has become a favored target for imaging and therapy of
malignancy. We have synthesized and characterized two new (4-quinolinoyl)-glycyl-2 …

Uses of DPP-IV inhibitors

K Dugi, F Himmelsbach, M Mark - US Patent 8,673,927, 2014 - Google Patents
The speci? cation describes the use of selected DPP IV inhibi tors for the treatment of
physiological functional disorders and for reducing the risk of the occurrence of such …

Inhibition of fibroblast activation protein and dipeptidylpeptidase 4 increases cartilage invasion by rheumatoid arthritis synovial fibroblasts

C Ospelt, JC Mertens, A Jüngel… - Arthritis & …, 2010 - Wiley Online Library
Objective Since fibroblasts in the synovium of patients with rheumatoid arthritis (RA) express
the serine proteases fibroblast activation protein (FAP) and dipeptidylpeptidase 4 (DPP …