17β-Hydroxysteroid dehydrogenase type 13 also known as 17β-HSD type 13 is an enzyme that in humans is encoded by the HSD17B13 gene.[5][6]

17β-HSD13 is significantly up-regulated in the liver of patients with non-alcoholic fatty liver disease (NAFLD) and enhances lipogenesis.[7]

Inhibitors

In 2023 the first potent and selective HSD17B13 inhibitor, BI-3231, was reported.[8] The inhibitor meets the quality criteria of a 'Donated Chemical Probe' as defined by the Structural Genomics Consortium.[9]

References

  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000170509 – Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000034528 – Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ Zhu YS, Imperato-McGinley JL (9 November 2016). "4.02: Disorders of Sexual Development in Males: Molecular Genetics, Epigenetics, Gender Identity, and Cognition". In Lightman S (ed.). Hormones, Brain and Behavior. Vol. 4: Clinical Important Effects of Hormones on Brain and Behavior. Elsevier Science. p. 69. ISBN 978-0-12-803608-2.
  6. ^ Zanders ED (9 November 2015). "Enzymes, Part 2". Human Drug Targets: A Compendium for Pharmaceutical Discovery. John Wiley & Sons. pp. 257–. ISBN 978-1-118-84985-9.
  7. ^ Su W, Wang Y, Jia X, Wu W, Li L, Tian X, et al. (August 2014). "Comparative proteomic study reveals 17β-HSD13 as a pathogenic protein in nonalcoholic fatty liver disease". Proceedings of the National Academy of Sciences of the United States of America. 111 (31): 11437–11442. Bibcode:2014PNAS..11111437S. doi:10.1073/pnas.1410741111. PMC 4128098. PMID 25028495.
  8. ^ Thamm S, Willwacher MK, Aspnes GE, Bretschneider T, Brown NF, Buschbom-Helmke S, et al. (February 2023). "Discovery of a Novel Potent and Selective HSD17B13 Inhibitor, BI-3231, a Well-Characterized Chemical Probe Available for Open Science". Journal of Medicinal Chemistry. 66 (4): 2832–2850. doi:10.1021/acs.jmedchem.2c01884. PMC 9969402. PMID 36727857.
  9. ^ "Donated Chemical Probes". thesgc.org. Retrieved July 31, 2023.
Allikas: http://en.wikipedia.org/wiki/HSD17B13
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