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AKR1C3 is an enzyme that makes potent male hormones and that some cancers carry in large amounts. Rather than blocking it, prodrugs use it as a key: they stay inactive until AKR1C3 inside a tumour cell converts them into a DNA-damaging drug.
AKR1C3 (chromosome 10p15.1) is a cytosolic aldo-keto reductase that reduces ketosteroids, producing potent androgens such as testosterone (UniProt P42330). A 2019 Clinical Cancer Research study described OBI-3424 as a highly selective prodrug that AKR1C3 converts to a potent DNA-alkylating agent, found AKR1C3 expression much higher in T-lineage than B-lineage acute lymphoblastic leukaemia, and reported prolonged event-free survival in all nine leukaemia xenografts tested (Evans et al., doi:10.1158/1078-0432.CCR-19-0551). In OnCo, AST-3424 (OBI-3424) and AST-001 come from Ascentawits' AKR1C3-activated prodrug platform, designed to kill tumour cells that overexpress the enzyme.
In plain words · AKR1C3 is an enzyme that makes potent male hormones and that some cancers carry in large amounts. Rather than blocking it, prodrugs use it as a key: they stay inactive until AKR1C3 inside a tumour cell converts them into a DNA-damaging drug.
AKR1C3 is an enzyme that makes potent male hormones and that some cancers carry in large amounts. Rather than blocking it, prodrugs use it as a key: they stay inactive until AKR1C3 inside a tumour cell converts them into a DNA-damaging drug.
NADPH-dependent reductase with broad ketosteroid substrate specificity (UniProt P42330); in these medicines it is the activating enzyme, not the thing inhibited.
1 product aims at AKR1C3: antibody-drug conjugates. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
NADPH-dependent reductase with broad ketosteroid substrate specificity (UniProt P42330); in these medicines it is the activating enzyme, not the thing inhibited.
AST-001 is an experimental small molecule AKR1C3-activated prodrug from Ascentawits Pharmaceuticals, in phase 1 trials for pancreatic cancer and advanced solid tumours.
Query for this target: (TITLE:"AKR1C3" OR ABSTRACT:"AKR1C3" OR TITLE:"aldo-keto reductase family 1 member C3" OR ABSTRACT:"aldo-keto reductase family 1 member C3" OR TITLE:"HSD17B5" OR ABSTRACT:"HSD17B5") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about AKR1C3, not a curated reading list.
Shares AST-001, Pancreatic ductal adenocarcinoma.
Shares AST-001, AST-3424, Hepatocellular carcinoma, Pancreatic ductal adenocarcinoma.
Shares AST-3424, Hepatocellular carcinoma.
Shares AST-3424, Hepatocellular carcinoma.
Shares AST-3424, Acute lymphoblastic leukaemia.
Shares AST-3424, Pancreatic ductal adenocarcinoma.
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