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Publikationer i urvalet

20 träffar

Bibliografisk träff 2024-04-03

Active site-directed probes targeting dipeptidyl peptidases 8 and 9.

Espadinha M, De Loose J, Corthaut S, Thys S, Van Rymenant Y, Verhulst E, Benramdane S, Filippi N, Augustyns K, Van Wielendaele P, Pintelon I, De Meester I, Van der Veken P.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2024.116389

Bibliografisk träff 2023-02-01

Optimized M24B Aminopeptidase Inhibitors for CARD8 Inflammasome Activation.

Chen Q, Wang A, Covelli DJ, Bhattacharjee A, Wang Q, Orth-He EL, Rao SD, Huang HC, Ball DP, Hsiao JC, Bachovchin DA.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.2c01535

Bibliografisk träff 2022-06-17

Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications.

Plescia J, Hédou D, Pousse ME, Labarre A, Dufresne C, Mittermaier A, Moitessier N.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114543

Bibliografisk träff 2022-04-18

Boron-Containing heterocycles as promising pharmacological agents.

Das BC, Adil Shareef M, Das S, Nandwana NK, Das Y, Saito M, Weiss LM.

Bioorg Med Chem · review; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2022.116748

Bibliografisk träff 2021-02-09

Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor.

Jung HJ, Nam EH, Park JY, Ghosh P, Kim IS.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2021.127846

Bibliografisk träff 2020-05-11

A cell-based fluorescent assay for FAP inhibitor discovery.

Zhang B, Liu F, Yang MF, Xu J, Wang Z, Zhang J, Wang R, Yang X.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2020.127253

Bibliografisk träff 2019-08-22

Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α.

Plescia J, De Cesco S, Patrascu MB, Kurian J, Di Trani J, Dufresne C, Wahba AS, Janmamode N, Mittermaier AK, Moitessier N.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.9b00642

Bibliografisk träff 2014-03-24

Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP).

Jansen K, Heirbaut L, Verkerk R, Cheng JD, Joossens J, Cos P, Maes L, Lambeir AM, De Meester I, Augustyns K, Van der Veken P.

J Med Chem · journal article · DOI 10.1021/jm500031w

Bibliografisk träff 2013-04-29

Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.

Poplawski SE, Lai JH, Li Y, Jin Z, Liu Y, Wu W, Wu Y, Zhou Y, Sudmeier JL, Sanford DG, Bachovchin WW.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/jm400351a

Bibliografisk träff 2013-03-18

Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold.

Jansen K, Heirbaut L, Cheng JD, Joossens J, Ryabtsova O, Cos P, Maes L, Lambeir AM, De Meester I, Augustyns K, Van der Veken P.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml300410d

Bibliografisk träff 2012-04-04

Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.

Ryabtsova O, Jansen K, Van Goethem S, Joossens J, Cheng JD, Lambeir AM, De Meester I, Augustyns K, Van der Veken P.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2012.03.107

Bibliografisk träff 2011-03-09

Pro-soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases.

Poplawski SE, Lai JH, Sanford DG, Sudmeier JL, Wu W, Bachovchin WW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm100972f

Bibliografisk träff 2008-09-11

Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety.

Connolly BA, Sanford DG, Chiluwal AK, Healey SE, Peters DE, Dimare MT, Wu W, Liu Y, Maw H, Zhou Y, Li Y, Jin Z, Sudmeier JL, Lai JH, Bachovchin WW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm800390n

Bibliografisk träff 2007-04-26

Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.

Lai JH, Wu W, Zhou Y, Maw HH, Liu Y, Milo LJ, Poplawski SE, Henry GD, Sudmeier JL, Sanford DG, Bachovchin WW.

J Med Chem · research support, non-u.s. gov't; journal article; research support, n.i.h., extramural · DOI 10.1021/jm061321+

Bibliografisk träff 2006-10-10

Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor.

Danilova O, Li B, Szardenings AK, Huber BT, Rosenblum JS.

Bioorg Med Chem Lett · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2006.10.012

Bibliografisk träff 2004-11-01

Ketopyrrolidines and ketoazetidines as potent dipeptidyl peptidase IV (DPP IV) inhibitors.

Ferraris D, Ko YS, Calvin D, Chiou T, Lautar S, Thomas B, Wozniak K, Rojas C, Kalish V, Belyakov S.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2004.08.057

Bibliografisk träff 2004-08-01

Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.

Weber AE.

J Med Chem · review; journal article · DOI 10.1021/jm030628v

Bibliografisk träff 2003-11-01

Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases.

Senten K, Van der Veken P, De Meester I, Lambeir AM, Scharpé S, Haemers A, Augustyns K.

J Med Chem · comparative study; research support, non-u.s. gov't; journal article · DOI 10.1021/jm0308803

Bibliografisk träff 2002-10-01

Development of potent and selective dipeptidyl peptidase II inhibitors.

Senten K, Van der Veken P, Bal G, De Meester I, Lambeir AM, Scharpé S, Bauvois B, Haemers A, Augustyns K.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/s0960-894x(02)00603-0

Bibliografisk träff 1996-05-01

Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides.

Coutts SJ, Kelly TA, Snow RJ, Kennedy CA, Barton RW, Adams J, Krolikowski DA, Freeman DM, Campbell SJ, Ksiazek JF, Bachovchin WW.

J Med Chem · journal article · DOI 10.1021/jm950732f