[(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives; HIF prolyl 4-hydroxylase inhibitors as oral erythropoietin secretagogues.
作者： Yong Rae Hong , Hyun Tae Kim , Seung-Chul Lee , Seonggu Ro , Joong Myung Cho
DOI: 10.1016/J.BMCL.2013.08.067
关键词:
摘要: A new series of PHD (HIF prolyl 4-hydroxylase) inhibitors was designed based on the X-ray co-crystal structure FG-2216. Using a lead generation process, [(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives developed as potent PHD2 inhibitors. This class compounds also showed ability to stabilize HIF-α, stimulate EPO secretion in vitro studies, and increase hematocrit, red blood cell count, hemoglobin levels an animal efficacy study.
sci-hub.se 参考文章(17)
A Weidemann, R S Johnson, Biology of HIF-1alpha. Cell Death & Differentiation. ,vol. 15, pp. 621- 627 ,(2008) , 10.1038/CDD.2008.12
Matthew M. Hsieh, N. Seth Linde, Aisha Wynter, Mark Metzger, Carol Wong, Ingrid Langsetmo, Al Lin, Reginald Smith, Griffin P. Rodgers, Robert E. Donahue, Stephen J. Klaus, John F. Tisdale, HIF prolyl hydroxylase inhibition results in endogenous erythropoietin induction, erythrocytosis, and modest fetal hemoglobin expression in rhesus macaques. Blood. ,vol. 110, pp. 2140- 2147 ,(2007) , 10.1182/BLOOD-2007-02-073254
Sarah K. Harten, Margaret Ashcroft, Patrick H. Maxwell, Prolyl Hydroxylase Domain Inhibitors: A Route to HIF Activation and Neuroprotection Antioxidants & Redox Signaling. ,vol. 12, pp. 459- 480 ,(2010) , 10.1089/ARS.2009.2870
Peter Fraisl, Julián Aragonés, Peter Carmeliet, Inhibition of oxygen sensors as a therapeutic strategy for ischaemic and inflammatory disease Nature Reviews Drug Discovery. ,vol. 8, pp. 139- 152 ,(2009) , 10.1038/NRD2761
Robert Freeman, Maria Barone, Targeting Hypoxia-Inducible Factor (HIF) as a Therapeutic Strategy for CNS Disorders Current Drug Targets - Cns & Neurological Disorders. ,vol. 4, pp. 85- 92 ,(2005) , 10.2174/1568007053005154
Hyunju Cho, Hyunsung Park, Eun Gyeong Yang, A fluorescence polarization-based interaction assay for hypoxia-inducible factor prolyl hydroxylases Biochemical and Biophysical Research Communications. ,vol. 337, pp. 275- 280 ,(2005) , 10.1016/J.BBRC.2005.09.041
M. Ivan, T. Haberberger, D. C. Gervasi, K. S. Michelson, V. Gunzler, K. Kondo, H. Yang, I. Sorokina, R. C. Conaway, J. W. Conaway, W. G. Kaelin, Biochemical purification and pharmacological inhibition of a mammalian prolyl hydroxylase acting on hypoxia-inducible factor Proceedings of the National Academy of Sciences of the United States of America. ,vol. 99, pp. 13459- 13464 ,(2002) , 10.1073/PNAS.192342099
Gregg L. Semenza, HIF-1, O2, and the 3 PHDs: How Animal Cells Signal Hypoxia to the Nucleus Cell. ,vol. 107, pp. 1- 3 ,(2001) , 10.1016/S0092-8674(01)00518-9
Kai-Hsin Chang, Mary M Stevenson, Comparison of murine Epo ELISA and Epo bioassays in detecting serum Epo levels during anemia associated with malaria infection. Journal of Immunological Methods. ,vol. 262, pp. 129- 136 ,(2002) , 10.1016/S0022-1759(02)00012-1
KangAe Lee, Robert A. Roth, John J. LaPres, Hypoxia, drug therapy and toxicity Pharmacology & Therapeutics. ,vol. 113, pp. 229- 246 ,(2007) , 10.1016/J.PHARMTHERA.2006.08.001