Literature DB >> 20740228

A fluopol-ABPP HTS assay to identify PAD inhibitors.

Bryan Knuckley1, Justin E Jones, Daniel A Bachovchin, Jessica Slack, Corey P Causey, Steven J Brown, Hugh Rosen, Benjamin F Cravatt, Paul R Thompson.   

Abstract

Protein Arginine Deiminase (PAD) activity is dysregulated in numerous diseases, e.g., Rheumatoid Arthritis. Herein we describe the development of a fluorescence polarization-Activity Based Protein Profiling (fluopol-ABPP) based high throughput screening assay that can be used to identify PAD-selective inhibitors. Using this assay, streptonigrin was identified as a potent, selective, and irreversible PAD4 inactivator.

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Year:  2010        PMID： 20740228      PMCID： PMC2943038          DOI： 10.1039/c0cc02634d

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN： 1359-7345            Impact factor:   6.222


  25 in total

1.  Preliminary observations on the use of streptonigrin as an antitumor agent in human beings.

Authors:  W L WILSON; C LABRA; E BARRIST
Journal:  Antibiot Chemother (Northfield)       Date:  1961-03

2.  The effects of streptonigrin on experimental tumors.

Authors:  J J OLESON; L A CALDERELLA; K J MJOS; A R REITH; R S THIE; I TOPLIN
Journal:  Antibiot Chemother (Northfield)       Date:  1961-03

3.  Transplantable human tumors in experimental chemotherapy: effects of streptonigrin on HS No. 1 and HEp No. 3 in the rat.

Authors:  M N TELLER; S F WAGSHUL; G W WOOLLEY
Journal:  Antibiot Chemother (Northfield)       Date:  1961-03

4.  A fluoroacetamidine-based inactivator of protein arginine deiminase 4: design, synthesis, and in vitro and in vivo evaluation.

Authors:  Yuan Luo; Bryan Knuckley; Young-Ho Lee; Michael R Stallcup; Paul R Thompson
Journal:  J Am Chem Soc       Date:  2006-02-01       Impact factor: 15.419

5.  Substrate specificity and kinetic studies of PADs 1, 3, and 4 identify potent and selective inhibitors of protein arginine deiminase 3.

Authors:  Bryan Knuckley; Corey P Causey; Justin E Jones; Monica Bhatia; Christina J Dreyton; Tanesha C Osborne; Hidenari Takahara; Paul R Thompson
Journal:  Biochemistry       Date:  2010-06-15       Impact factor: 3.162

6.  A colorimetric 96-well microtiter plate assay for the determination of enzymatically formed citrulline.

Authors:  M Knipp; M Vasák
Journal:  Anal Biochem       Date:  2000-11-15       Impact factor: 3.365

7.  Inhibitors and inactivators of protein arginine deiminase 4: functional and structural characterization.

Authors:  Yuan Luo; Kyouhei Arita; Monica Bhatia; Bryan Knuckley; Young-Ho Lee; Michael R Stallcup; Mamoru Sato; Paul R Thompson
Journal:  Biochemistry       Date:  2006-10-03       Impact factor: 3.162

8.  Activity-based protein profiling reagents for protein arginine deiminase 4 (PAD4): synthesis and in vitro evaluation of a fluorescently labeled probe.

Authors:  Yuan Luo; Bryan Knuckley; Monica Bhatia; Perry J Pellechia; Paul R Thompson
Journal:  J Am Chem Soc       Date:  2006-11-15       Impact factor: 15.419

9.  Kinetic characterization of protein arginine deiminase 4: a transcriptional corepressor implicated in the onset and progression of rheumatoid arthritis.

Authors:  Patricia L Kearney; Monica Bhatia; Nelroy G Jones; Luo Yuan; Mary C Glascock; Kristen L Catchings; Michiyuki Yamada; Paul R Thompson
Journal:  Biochemistry       Date:  2005-08-09       Impact factor: 3.162

10.  Protein arginine deiminase 4: evidence for a reverse protonation mechanism.

Authors:  Bryan Knuckley; Monica Bhatia; Paul R Thompson
Journal:  Biochemistry       Date:  2007-05-12       Impact factor: 3.162
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  30 in total

Review 1.  The pharmacological landscape and therapeutic potential of serine hydrolases.

Authors:  Daniel A Bachovchin; Benjamin F Cravatt
Journal:  Nat Rev Drug Discov       Date:  2012-01-03       Impact factor: 84.694

2.  Activity-based protein profiling of protein arginine methyltransferase 1.

Authors:  Obiamaka Obianyo; Corey P Causey; Justin E Jones; Paul R Thompson
Journal:  ACS Chem Biol       Date:  2011-08-23       Impact factor: 5.100

3.  Expression of peptidylarginine deiminase 4 in an alkali injury model of retinal gliosis.

Authors:  John W Wizeman; Royce Mohan
Journal:  Biochem Biophys Res Commun       Date:  2017-04-08       Impact factor: 3.575

Review 4.  Chemical biology of protein arginine modifications in epigenetic regulation.

Authors:  Jakob Fuhrmann; Kathleen W Clancy; Paul R Thompson
Journal:  Chem Rev       Date:  2015-05-13       Impact factor: 60.622

Review 5.  Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.

Authors:  Stuart L Schreiber; Joanne D Kotz; Min Li; Jeffrey Aubé; Christopher P Austin; John C Reed; Hugh Rosen; E Lucile White; Larry A Sklar; Craig W Lindsley; Benjamin R Alexander; Joshua A Bittker; Paul A Clemons; Andrea de Souza; Michael A Foley; Michelle Palmer; Alykhan F Shamji; Mathias J Wawer; Owen McManus; Meng Wu; Beiyan Zou; Haibo Yu; Jennifer E Golden; Frank J Schoenen; Anton Simeonov; Ajit Jadhav; Michael R Jackson; Anthony B Pinkerton; Thomas D Y Chung; Patrick R Griffin; Benjamin F Cravatt; Peter S Hodder; William R Roush; Edward Roberts; Dong-Hoon Chung; Colleen B Jonsson; James W Noah; William E Severson; Subramaniam Ananthan; Bruce Edwards; Tudor I Oprea; P Jeffrey Conn; Corey R Hopkins; Michael R Wood; Shaun R Stauffer; Kyle A Emmitte
Journal:  Cell       Date:  2015-06-04       Impact factor: 41.582

6.  Fluorescence polarization assays in high-throughput screening and drug discovery: a review.

Authors:  Matthew D Hall; Adam Yasgar; Tyler Peryea; John C Braisted; Ajit Jadhav; Anton Simeonov; Nathan P Coussens
Journal:  Methods Appl Fluoresc       Date:  2016-04-28       Impact factor: 3.009

Review 7.  Chemical approaches to study metabolic networks.

Authors:  Daniel Medina-Cleghorn; Daniel K Nomura
Journal:  Pflugers Arch       Date:  2013-01-08       Impact factor: 3.657

Review 8.  Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11.

Authors:  David F Tough; Huw D Lewis; Inmaculada Rioja; Matthew J Lindon; Rab K Prinjha
Journal:  Br J Pharmacol       Date:  2014-11       Impact factor: 8.739

Review 9.  Exploring metabolic pathways and regulation through functional chemoproteomic and metabolomic platforms.

Authors:  Daniel Medina-Cleghorn; Daniel K Nomura
Journal:  Chem Biol       Date:  2014-09-18

10.  Monitoring of protein arginine deiminase activity by using fluorescence quenching: multicolor visualization of citrullination.

Authors:  Qunzhao Wang; Melanie A Priestman; David S Lawrence
Journal:  Angew Chem Int Ed Engl       Date:  2013-01-21       Impact factor: 15.336
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