PMID- 26713111
OWN - NLM
STAT- PubMed-not-MEDLINE
DCOM- 20151229
LR  - 20200930
IS  - 1948-5875 (Print)
IS  - 1948-5875 (Electronic)
IS  - 1948-5875 (Linking)
VI  - 6
IP  - 12
DP  - 2015 Dec 10
TI  - Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of 
      Prolyl Hydroxylase 2 Inhibitors.
PG  - 1236-40
LID - 10.1021/acsmedchemlett.5b00394 [doi]
AB  - 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-alpha (HIF1alpha). 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 HIF1alpha (556-574) peptide as a probe for 
      quantitative and site-specific screening of small molecule PHD2 inhibitors.
FAU - Lei, Yonghua
AU  - Lei Y
AD  - Jiangsu Key Laboratory of Drug Design and Optimization, and State Key Laboratory 
      of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.
FAU - Hu, Tianhan
AU  - Hu T
AD  - Jiangsu Key Laboratory of Drug Design and Optimization, and State Key Laboratory 
      of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.
FAU - Wu, Xingsen
AU  - Wu X
AD  - Jiangsu Key Laboratory of Drug Design and Optimization, and State Key Laboratory 
      of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.
FAU - Wu, Yue
AU  - Wu Y
AD  - Jiangsu Key Laboratory of Drug Design and Optimization, and State Key Laboratory 
      of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.
FAU - Bao, Qichao
AU  - Bao Q
AD  - Jiangsu Key Laboratory of Drug Design and Optimization, and State Key Laboratory 
      of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.
FAU - Zhang, Lianshan
AU  - Zhang L
AD  - National Engineering and Research Center for Target Drugs , Lianyungang 222000, 
      China.
FAU - Xia, Hua
AU  - Xia H
AD  - Jiangsu Key Laboratory of Drug Design and Optimization, and State Key Laboratory 
      of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.
FAU - Sun, Haopeng
AU  - Sun H
AD  - Jiangsu Key Laboratory of Drug Design and Optimization, and State Key Laboratory 
      of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.
FAU - You, Qidong
AU  - You Q
AD  - Jiangsu Key Laboratory of Drug Design and Optimization, and State Key Laboratory 
      of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China.
FAU - Zhang, Xiaojin
AU  - Zhang X
AD  - Jiangsu Key Laboratory of Drug Design and Optimization, and State Key Laboratory 
      of Natural Medicines, China Pharmaceutical University , Nanjing 210009, China ; 
      Department of Organic Chemistry, School of Science, China Pharmaceutical 
      University , Nanjing 210009, China.
LA  - eng
PT  - Journal Article
DEP - 20151109
PL  - United States
TA  - ACS Med Chem Lett
JT  - ACS medicinal chemistry letters
JID - 101521073
PMC - PMC4677366
OTO - NOTNLM
OT  - FITC-labeled probe
OT  - PHD2
OT  - affinity-based
OT  - fluorescence polarization assay
COIS- The authors declare no competing financial interest.
EDAT- 2015/12/30 06:00
MHDA- 2015/12/30 06:01
PMCR- 2016/12/10
CRDT- 2015/12/30 06:00
PHST- 2015/10/07 00:00 [received]
PHST- 2015/11/09 00:00 [accepted]
PHST- 2015/12/30 06:00 [entrez]
PHST- 2015/12/30 06:00 [pubmed]
PHST- 2015/12/30 06:01 [medline]
PHST- 2016/12/10 00:00 [pmc-release]
AID - 10.1021/acsmedchemlett.5b00394 [doi]
PST - epublish
SO  - ACS Med Chem Lett. 2015 Nov 9;6(12):1236-40. doi: 10.1021/acsmedchemlett.5b00394. 
      eCollection 2015 Dec 10.