Literature DB >> 19364117

Application of a proteolysis/mass spectrometry method for investigating the effects of inhibitors on hydroxylase structure.

Christopher J Stubbs1, Christoph Loenarz, Jasmin Mecinović, Kar Kheng Yeoh, Nicola Hindley, Benoît M Liénard, Frank Sobott, Christopher J Schofield, Emily Flashman.   

Abstract

Limited proteolysis coupled to matrix-assisted laser desorption/ionization (MALDI) mass spectrometric analyses can be used to screen for compounds that alter protein structure by monitoring stabilizing/destabilizing effects with respect to the rate and nature of proteolysis. When applied to prolyl hydroxylase 2, a key enzyme involved in human oxygen sensing, the method efficiently revealed differential effects on proteolytic stability for structurally similar compounds and for different substrates.

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Year:  2009        PMID： 19364117     DOI： 10.1021/jm900285r

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  17 in total

1.  Screening chelating inhibitors of HIF-prolyl hydroxylase domain 2 (PHD2) and factor inhibiting HIF (FIH).

Authors:  Shannon C Flagg; Cristina B Martin; Cornelius Y Taabazuing; Breanne E Holmes; Michael J Knapp
Journal:  J Inorg Biochem       Date:  2012-03-17       Impact factor: 4.155

2.  Pre- and post-conditional inhibition of prolyl-4-hydroxylase domain enzymes protects the heart from an ischemic insult.

Authors:  Melanie Vogler; Anke Zieseniss; Amke R Hesse; Elif Levent; Malte Tiburcy; Eva Heinze; Nicolai Burzlaff; Gunnar Schley; Kai Uwe Eckardt; Carsten Willam; Dörthe M Katschinski
Journal:  Pflugers Arch       Date:  2015-01-13       Impact factor: 3.657

3.  A photoreactive small-molecule probe for 2-oxoglutarate oxygenases.

Authors:  Akane Kawamura; Alexander Wolf; Dante Rotili; Mikael Altun; Roman Fischer; Ivanhoe K H Leung; Mukram M Mackeen; Ya-Min Tian; Peter J Ratcliffe; Antonello Mai; Benedikt M Kessler; Christopher J Schofield
Journal:  Chem Biol       Date:  2011-05-27

4.  Protein Flexibility of the α-Ketoglutarate-Dependent Oxygenase Factor-Inhibiting HIF-1: Implications for Substrate Binding, Catalysis, and Regulation.

Authors:  Cristina B Martin; Vanessa D Chaplin; Stephen J Eyles; Michael J Knapp
Journal:  Biochemistry       Date:  2019-09-20       Impact factor: 3.162

5.  The metabolite α-ketoglutarate extends lifespan by inhibiting ATP synthase and TOR.

Authors:  Randall M Chin; Xudong Fu; Melody Y Pai; Laurent Vergnes; Heejun Hwang; Gang Deng; Simon Diep; Brett Lomenick; Vijaykumar S Meli; Gabriela C Monsalve; Eileen Hu; Stephen A Whelan; Jennifer X Wang; Gwanghyun Jung; Gregory M Solis; Farbod Fazlollahi; Chitrada Kaweeteerawat; Austin Quach; Mahta Nili; Abby S Krall; Hilary A Godwin; Helena R Chang; Kym F Faull; Feng Guo; Meisheng Jiang; Sunia A Trauger; Alan Saghatelian; Daniel Braas; Heather R Christofk; Catherine F Clarke; Michael A Teitell; Michael Petrascheck; Karen Reue; Michael E Jung; Alison R Frand; Jing Huang
Journal:  Nature       Date:  2014-05-14       Impact factor: 49.962

6.  Prolyl-hydroxylase inhibitor activating hypoxia-inducible transcription factors reduce levels of transplant arteriosclerosis in a murine aortic allograft model.

Authors:  Christian Heim; Wanja Bernhardt; Sabina Jalilova; Zhendi Wang; Benjamin Motsch; Martina Ramsperger-Gleixner; Nicolai Burzlaff; Michael Weyand; Kai-Uwe Eckardt; Stephan M Ensminger
Journal:  Interact Cardiovasc Thorac Surg       Date:  2016-01-27

7.  Substrate preference of the HIF-prolyl hydroxylase-2 (PHD2) and substrate-induced conformational change.

Authors:  Serap Pektas; Michael J Knapp
Journal:  J Inorg Biochem       Date:  2013-05-21       Impact factor: 4.155

8.  Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors.

Authors:  Ivanhoe K H Leung; Marina Demetriades; Adam P Hardy; Clarisse Lejeune; Tristan J Smart; Andrea Szöllössi; Akane Kawamura; Christopher J Schofield; Timothy D W Claridge
Journal:  J Med Chem       Date:  2013-01-04       Impact factor: 7.446

9.  Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors.

Authors:  Oliver N F King; Xuan Shirley Li; Masaaki Sakurai; Akane Kawamura; Nathan R Rose; Stanley S Ng; Amy M Quinn; Ganesha Rai; Bryan T Mott; Paul Beswick; Robert J Klose; Udo Oppermann; Ajit Jadhav; Tom D Heightman; David J Maloney; Christopher J Schofield; Anton Simeonov
Journal:  PLoS One       Date:  2010-11-23       Impact factor: 3.240

10.  Dual-action inhibitors of HIF prolyl hydroxylases that induce binding of a second iron ion.

Authors:  Kar Kheng Yeoh; Mun Chiang Chan; Armin Thalhammer; Marina Demetriades; Rasheduzzaman Chowdhury; Ya-Min Tian; Ineke Stolze; Luke A McNeill; Myung Kyu Lee; Esther C Y Woon; Mukram M Mackeen; Akane Kawamura; Peter J Ratcliffe; Jasmin Mecinović; Christopher J Schofield
Journal:  Org Biomol Chem       Date:  2012-11-15       Impact factor: 3.876
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