Molecular and Cellular Mechanisms of HIF Prolyl Hydroxylase inhibitors in Clinical Trials

Molecular and Cellular Mechanisms of HIF Prolyl Hydroxylase inhibitors in Clinical Trials

Inhibition of the human 2-oxoglutarate (2OG) dependent hypoxia inducible factor (HIF) prolyl hydroxylases (human PHD1-3) causes upregulation of HIF, thus promoting erythropoiesis and is therefore of therapeutic interest. We describe cellular, biophysical, and biochemical studies comparing four PHD i...

Full description

Bibliographic Details
Main Authors:	Yeh, TL, Leissing, TM, Abboud, M, Thinnes, CC, Atasoylu, O, Holt-Martyn, JP, Zhang, D, Tumber, A, Lippl, K, Lohans, CT, Leung, IKH, Morcrette, H, Kawamura, A, Flashman, E, Lu, X, Ratcliffe, P, Chowdhury, R, Pugh, C, Schofield, C
Format:	Journal article
Published:	Royal Society of Chemistry 2017

Similar Items

Structure–activity relationship and crystallographic studies on 4-hydroxypyrimidine HIF prolyl hydroxylase domain inhibitors
by: Holt-Martyn, JP, et al.
Published: (2019)

Tuning the transcriptional response to hypoxia by inhibiting HIF prolyl- and asparaginyl-hydroxylases
by: Chan, M, et al.
Published: (2016)

Lack of activity of recombinant HIF prolyl hydroxylases (PHDs) on reported non-HIF substrates
by: Cockman, M, et al.
Published: (2019)

2-oxoglutarate analogue inhibitors of HIF prolyl hydroxylase.
by: Mole, D, et al.
Published: (2003)

Inhibition of a viral prolyl hydroxylase
by: Langley, G, et al.
Published: (2019)

Regulation of HIF: prolyl hydroxylases.
by: Stolze, I, et al.
Published: (2006)

Lack of activity of recombinant HIF prolyl hydroxylases (PHDs) on reported non-HIF substrates
by: Matthew E Cockman, et al.
Published: (2019-09-01)

Potent and selective triazole-based inhibitors of the hypoxia-inducible factor prolyl-hydroxylases with activity in the murine brain
by: Chan, MC, et al.
Published: (2015)

Analogues of dealanylalahopcin are inhibitors of human HIF prolyl hydroxylases.
by: Schlemminger, I, et al.
Published: (2003)

The use of dioxygen by HIF prolyl hydroxylase (PHD1).
by: McNeill, L, et al.
Published: (2002)

Biochemical and biophysical analyses of hypoxia sensing prolyl hydroxylases from Dictyostelium discoideum and Toxoplasma gondii
by: Liu, T, et al.
Published: (2020)

Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors
by: Holt-Martyn, J, et al.
Published: (2019)

Selective inhibitors of a human prolyl hydroxylase (OGFOD1) involved in ribosomal decoding
by: Thinnes, C, et al.
Published: (2018)

Exploring the substrate selectivity of oxygen sensing prolyl hydroxylases
by: Lippl, K, et al.
Published: (2015)

Structural basis for oxygen degradation domain selectivity of the HIF prolyl hydroxylases
by: Chowdhury, R, et al.
Published: (2016)

Structural, biochemical and inhibition studies on hypoxia-inducible factor (HIF) prolyl hydroxylases
by: Lippl, K
Published: (2018)

Determination and comparison of specific activity of the HIF-prolyl hydroxylases.
by: Tuckerman, JR, et al.
Published: (2004)

Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases.
by: Chowdhury, R, et al.
Published: (2013)

Structural basis for oxygen degradation domain selectivity of the HIF prolyl hydroxylases
by: Rasheduzzaman Chowdhury, et al.
Published: (2016-08-01)

Investigating the dependence of the hypoxia-inducible factor hydroxylases (factor inhibiting HIF and prolyl hydroxylase domain 2) on ascorbate and other reducing agents.
by: Flashman, E, et al.
Published: (2010)

A fluorescent benzo[g]isoquinoline-based HIF prolyl hydroxylase inhibitor for cellular imaging
by: Mayer, M, et al.
Published: (2018)

Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain.
by: Mun Chiang Chan, et al.
Published: (2015-01-01)

Studies on the substrate selectivity of the hypoxia-inducible factor prolyl hydroxylase 2 catalytic domain
by: Abboud, M, et al.
Published: (2018)

HIF prolyl and asparaginyl hydroxylases in the biological response to intracellular O(2) levels.
by: Masson, N, et al.
Published: (2003)

The HIF prolyl hydroxylase PHD3 is a potential substrate of the TRiC chaperonin.
by: Masson, N, et al.
Published: (2004)

Pharmacological targeting of the HIF hydroxylases - A new field in medicine development.
by: Chan, M, et al.
Published: (2016)

Dual-action inhibitors of HIF prolyl hydroxylases that induce binding of a second iron ion.
by: Yeoh, K, et al.
Published: (2013)

Signalling hypoxia by HIF hydroxylases.
by: Schofield, C, et al.
Published: (2005)

Oxygen sensing by HIF hydroxylases.
by: Schofield, C, et al.
Published: (2004)

BIOL 56-ESI-MS studies on prolyl hydroxylase domain 2
by: Mecinovic, J, et al.
Published: (2008)

Characterization of different isoforms of the HIF prolyl hydroxylase PHD1 generated by alternative initiation.
by: Tian, Y, et al.
Published: (2006)

HIF prolyl hydroxylases in the rat; organ distribution and changes in expression following hypoxia and coronary artery ligation.
by: Willam, C, et al.
Published: (2006)

Structural basis of prolyl hydroxylase domain inhibition by Molidustat
by: Figg, WD, et al.
Published: (2021)

2-oxoglutarate regulates binding of hydroxylated hypoxia-inducible factor to prolyl hydroxylase domain 2
by: Abboud, M, et al.
Published: (2018)

Born to sense: biophysical analyses of the oxygen sensing prolyl hydroxylase from the simplest animal Trichoplax adhaerens
by: Lippl, K, et al.
Published: (2018)

Inhibition of HIF-prolyl hydroxylases improves healing of intestinal anastomoses
by: Moritz J. Strowitzki, et al.
Published: (2021-04-01)

The Prolyl Hydroxylase Inhibitor BIQ/FG-2216 Stabilises HIF-1 alpha and Upregulates VEGF in vitro: A Potential Strategy For Difficult CTO Lesions in Patients.
by: Barnett, G, et al.
Published: (2013)

Novel and selective small molecule inhibitors and activators for the prolyl hydroxylase domain enzyme
by: Holt-Martyn, J
Published: (2018)

Use of mass spectrometry to probe the nucleophilicity of cysteinyl residues of prolyl hydroxylase domain 2.
by: Mecinović, J, et al.
Published: (2009)

HIF prolyl hydroxylase inhibition prior to transient focal cerebral ischaemia is neuroprotective in mice.
by: Chen, R, et al.
Published: (2014)