Structure‐Activity Relationship and Crystallographic Studies on 4‐Hydroxypyrimidine HIF Prolyl Hydroxylase Domain Inhibitors
Abstract: The 2‐oxoglutarate‐dependent hypoxia inducible factor prolyl hydroxylases (PHDs) are targets for treatment of a variety of diseases including anaemia. One PHD inhibitor is approved for use for the treatment of renal anaemia and others are in late stage clinical trials. The number of reported templates for PHD inhibition is limited. We report structure–activity relationship and crystallographic studies on a promising class of 4‐hydroxypyrimidine‐containing PHD inhibitors.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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Structure‐Activity Relationship and Crystallographic Studies on 4‐Hydroxypyrimidine HIF Prolyl Hydroxylase Domain Inhibitors ; volume:15 ; number:3 ; year:2020 ; pages:270-273 ; extent:4
ChemMedChem ; 15, Heft 3 (2020), 270-273 (gesamt 4)
- Creator
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Holt‐Martyn, James P.
Chowdhury, Rasheduzzaman
Tumber, Anthony
Yeh, Tzu‐Lan
Abboud, Martine I.
Lippl, Kerstin
Lohans, Christopher T.
Langley, Gareth W.
Figg, William
McDonough, Michael A.
Pugh, Christopher W.
Ratcliffe, Peter J.
Schofield, Christopher
- DOI
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10.1002/cmdc.201900557
- URN
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urn:nbn:de:101:1-2022062511155766166738
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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15.08.2025, 7:25 AM CEST
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Associated
- Holt‐Martyn, James P.
- Chowdhury, Rasheduzzaman
- Tumber, Anthony
- Yeh, Tzu‐Lan
- Abboud, Martine I.
- Lippl, Kerstin
- Lohans, Christopher T.
- Langley, Gareth W.
- Figg, William
- McDonough, Michael A.
- Pugh, Christopher W.
- Ratcliffe, Peter J.
- Schofield, Christopher
Other Objects (12)
Crystallographic and Selectivity Studies on the Approved HIF Prolyl Hydroxylase Inhibitors Desidustat and Enarodustat
Rolle der HIF-Prolyl Hydroxylase Enzyme in der akuten Pankreatitis
Bedeutung des HIF-Prolyl-Hydroxylase 1 (PHS1) Enzyms bei der Leberregeneration
Novel Dioxygenases, HIF-α Specific Prolyl-hydroxylase and Asparanginyl-hydroxylase: O2 Switch for Cell Survival
HIF prolyl hydroxylase inhibition protects skeletal muscle from eccentric contraction-induced injury
Impact of HIF prolyl hydroxylase inhibitors in heart failure patients with renal anemia
The role ofm HIF-prolyl hydroxylase 2 (PHD2) and erythropoietin in the hematopoietic system
Correction to: HIF prolyl hydroxylase inhibition protects skeletal muscle from eccentric contraction induced injury
Collagen prolyl 4-hydroxylase 1 is essential for HIF-1α stabilization and TNBC chemoresistance
Relevance of Prolyl HIF Hydroxylase 2 (PHD2) during embryo development and wound healing in mice
No benefit of HIF prolyl hydroxylase inhibition for hypertensive renal damage in renovascular hypertensive rats
The impact of neuronal HIF prolyl 4-hydroxylase 2 inactivation on ischemic stroke recovery in mice
Crystallographic and Selectivity Studies on the Approved HIF Prolyl Hydroxylase Inhibitors Desidustat and Enarodustat
Rolle der HIF-Prolyl Hydroxylase Enzyme in der akuten Pankreatitis
Bedeutung des HIF-Prolyl-Hydroxylase 1 (PHS1) Enzyms bei der Leberregeneration
Novel Dioxygenases, HIF-α Specific Prolyl-hydroxylase and Asparanginyl-hydroxylase: O2 Switch for Cell Survival
HIF prolyl hydroxylase inhibition protects skeletal muscle from eccentric contraction-induced injury
Impact of HIF prolyl hydroxylase inhibitors in heart failure patients with renal anemia
The role ofm HIF-prolyl hydroxylase 2 (PHD2) and erythropoietin in the hematopoietic system
Correction to: HIF prolyl hydroxylase inhibition protects skeletal muscle from eccentric contraction induced injury
Collagen prolyl 4-hydroxylase 1 is essential for HIF-1α stabilization and TNBC chemoresistance
Relevance of Prolyl HIF Hydroxylase 2 (PHD2) during embryo development and wound healing in mice
No benefit of HIF prolyl hydroxylase inhibition for hypertensive renal damage in renovascular hypertensive rats
The impact of neuronal HIF prolyl 4-hydroxylase 2 inactivation on ischemic stroke recovery in mice
Crystallographic and Selectivity Studies on the Approved HIF Prolyl Hydroxylase Inhibitors Desidustat and Enarodustat
Rolle der HIF-Prolyl Hydroxylase Enzyme in der akuten Pankreatitis
Bedeutung des HIF-Prolyl-Hydroxylase 1 (PHS1) Enzyms bei der Leberregeneration
Novel Dioxygenases, HIF-α Specific Prolyl-hydroxylase and Asparanginyl-hydroxylase: O2 Switch for Cell Survival
HIF prolyl hydroxylase inhibition protects skeletal muscle from eccentric contraction-induced injury
Impact of HIF prolyl hydroxylase inhibitors in heart failure patients with renal anemia
The role ofm HIF-prolyl hydroxylase 2 (PHD2) and erythropoietin in the hematopoietic system
Correction to: HIF prolyl hydroxylase inhibition protects skeletal muscle from eccentric contraction induced injury
Collagen prolyl 4-hydroxylase 1 is essential for HIF-1α stabilization and TNBC chemoresistance
Relevance of Prolyl HIF Hydroxylase 2 (PHD2) during embryo development and wound healing in mice
No benefit of HIF prolyl hydroxylase inhibition for hypertensive renal damage in renovascular hypertensive rats