Literature DB >> 26713111

Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors.

Yonghua Lei1, Tianhan Hu1, Xingsen Wu1, Yue Wu1, Qichao Bao1, Lianshan Zhang2, Hua Xia1, Haopeng Sun1, Qidong You1, Xiaojin Zhang3.   

Abstract

Prolyl hydroxylase domain 2 (PHD2) enzyme, a Fe(II) and 2-oxoglutarate (2-OG) dependent oxygenase, mediates key physiological responses to hypoxia by modulating the levels of hypoxia inducible factor 1-α (HIF1α). PHD2 has been shown to have the therapeutic potentials for conditions including anemia and ischemic disease. Currently, many activity-based assays have been developed for identifying PHD2 inhibitors. Here we report an affinity-based fluorescence polarization method using FITC-labeled HIF1α (556-574) peptide as a probe for quantitative and site-specific screening of small molecule PHD2 inhibitors.

Entities:  

Keywords:  FITC-labeled probe; PHD2; affinity-based; fluorescence polarization assay

Year:  2015        PMID： 26713111      PMCID： PMC4677366          DOI： 10.1021/acsmedchemlett.5b00394

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  23 in total

1.  A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays.

Authors: 
Journal:  J Biomol Screen       Date:  1999

2.  Structure-based design, synthesis, and SAR evaluation of a new series of 8-hydroxyquinolines as HIF-1alpha prolyl hydroxylase inhibitors.

Authors:  Namal C Warshakoon; Shengde Wu; Angelique Boyer; Richard Kawamoto; Justin Sheville; Sean Renock; Kevin Xu; Matthew Pokross; Songtao Zhou; Carol Winter; Richard Walter; Marlene Mekel; Artem G Evdokimov
Journal:  Bioorg Med Chem Lett       Date:  2006-08-22       Impact factor: 2.823

3.  1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.

Authors:  Petr Vachal; Shouwu Miao; Joan M Pierce; Deodial Guiadeen; Vincent J Colandrea; Matthew J Wyvratt; Scott P Salowe; Lisa M Sonatore; James A Milligan; Richard Hajdu; Anantha Gollapudi; Carol A Keohane; Russell B Lingham; Suzanne M Mandala; Julie A DeMartino; Xinchun Tong; Michael Wolff; Dietrich Steinhuebel; Gerard R Kieczykowski; Fred J Fleitz; Kevin Chapman; John Athanasopoulos; Gregory Adam; Can D Akyuz; Dhirendra K Jena; Jeffrey W Lusen; Juncai Meng; Benjamin D Stein; Lei Xia; Edward C Sherer; Jeffrey J Hale
Journal:  J Med Chem       Date:  2012-02-27       Impact factor: 7.446

4.  A fluorescence polarization-based interaction assay for hypoxia-inducible factor prolyl hydroxylases.

Authors:  Hyunju Cho; Hyunsung Park; Eun Gyeong Yang
Journal:  Biochem Biophys Res Commun       Date:  2005-11-11       Impact factor: 3.575

Review 5.  HIF prolyl hydroxylase inhibitors for anemia.

Authors:  Eugene Muchnik; Joshua Kaplan
Journal:  Expert Opin Investig Drugs       Date:  2011-03-16       Impact factor: 6.206

Review 6.  The human oxygen sensing machinery and its manipulation.

Authors:  Rasheduzzaman Chowdhury; Adam Hardy; Christopher J Schofield
Journal:  Chem Soc Rev       Date:  2008-05-27       Impact factor: 54.564

7.  Dynamic combinatorial chemistry employing boronic acids/boronate esters leads to potent oxygenase inhibitors.

Authors:  Marina Demetriades; Ivanhoe K H Leung; Rasheduzzaman Chowdhury; Mun Chiang Chan; Michael A McDonough; Kar Kheng Yeoh; Ya-Min Tian; Timothy D W Claridge; Peter J Ratcliffe; Esther C Y Woon; Christopher J Schofield
Journal:  Angew Chem Int Ed Engl       Date:  2012-05-25       Impact factor: 15.336

8.  Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases.

Authors:  Rasheduzzaman Chowdhury; José Ignacio Candela-Lena; Mun Chiang Chan; David Jeremy Greenald; Kar Kheng Yeoh; Ya-Min Tian; Michael A McDonough; Anthony Tumber; Nathan R Rose; Ana Conejo-Garcia; Marina Demetriades; Sinnakaruppan Mathavan; Akane Kawamura; Myung Kyu Lee; Freek van Eeden; Christopher W Pugh; Peter J Ratcliffe; Christopher J Schofield
Journal:  ACS Chem Biol       Date:  2013-06-12       Impact factor: 5.100

9.  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

10.  Mimicking hypoxia to treat anemia: HIF-stabilizer BAY 85-3934 (Molidustat) stimulates erythropoietin production without hypertensive effects.

Authors:  Ingo Flamme; Felix Oehme; Peter Ellinghaus; Mario Jeske; Jörg Keldenich; Uwe Thuss
Journal:  PLoS One       Date:  2014-11-13       Impact factor: 3.240
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  4 in total

1.  Discovery of Fluorescence Polarization Probe for the ELISA-Based Antagonist Screening of α1-Adrenergic Receptors.

Authors:  Zhao Ma; Zhenzhen Liu; Tianyu Jiang; Tianchao Zhang; Huateng Zhang; Lupei Du; Minyong Li
Journal:  ACS Med Chem Lett       Date:  2016-08-26       Impact factor: 4.345

2.  Competitive and noncompetitive immunoassays for the detection of benzothiostrobin using magnetic nanoparticles and fluorescein isothiocyanate-labeled peptides.

Authors:  He Chen; Qian Yang; Yuan Ding; Natalia Vasylieva; Candace S Bever; Xiude Hua; Minghua Wang; Bruce D Hammock
Journal:  Anal Bioanal Chem       Date:  2018-11-26       Impact factor: 4.142

3.  Fluorescent "Turn off-on" Small-Molecule-Monitoring Nanoplatform Based on Dendrimer-like Peptides as Competitors.

Authors:  He Chen; Yuan Ding; Qian Yang; Bogdan Barnych; Gualberto González-Sapienza; Bruce D Hammock; Minghua Wang; Xiude Hua
Journal:  ACS Appl Mater Interfaces       Date:  2019-08-30       Impact factor: 9.229

4.  Endothelial HIF-2α contributes to severe pulmonary hypertension due to endothelial-to-mesenchymal transition.

Authors:  Haiyang Tang; Aleksandra Babicheva; Kimberly M McDermott; Yali Gu; Ramon J Ayon; Shanshan Song; Ziyi Wang; Akash Gupta; Tong Zhou; Xutong Sun; Swetaleena Dash; Zilu Wang; Angela Balistrieri; Qiuyu Zheng; Arlette G Cordery; Ankit A Desai; Franz Rischard; Zain Khalpey; Jian Wang; Stephen M Black; Joe G N Garcia; Ayako Makino; Jason X-J Yuan
Journal:  Am J Physiol Lung Cell Mol Physiol       Date:  2017-10-26       Impact factor: 5.464
  4 in total

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