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Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.

Clausen DJ, Liu J, Yu W, Duffy JL, Chung CC, Myers RW, Klein DJ, Fells J, Holloway K, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski J
Bioorg Med Chem Lett 30 127367 (2020)
Cited: 10 times
EuropePMC logo PMID: 32738976

Abstract

The synthesis and SAR development of a trisubstituted imidazole HDAC inhibitor is described. The compounds were synthesized with high diastereocontrol by leveraging Ellman sulfinyl imine chemistry. Structural elucidation provided insight into binding mode and supported design rational. Pharmacokinetic properties of lead compounds were determined.

Reviews - 6xec mentioned but not cited (1)

  1. Characterization of host substrates of SARS-CoV-2 main protease. Melano I, Lo YC, Su WC. Front Microbiol 14 1251705 (2023)

Articles - 6xec mentioned but not cited (2)

  1. Mechanism of assembly, activation and lysine selection by the SIN3B histone deacetylase complex. Wan MSM, Muhammad R, Koliopoulos MG, Roumeliotis TI, Choudhary JS, Alfieri C. Nat Commun 14 2556 (2023)
  2. Structural mass spectrometry decodes domain interaction and dynamics of the full-length Human Histone Deacetylase 2. Soloviev Z, Bullock JMA, James JMB, Sauerwein AC, Nettleship JE, Owens RJ, Hansen DF, Topf M, Thalassinos K. Biochim Biophys Acta Proteins Proteom 1870 140759 (2022)


Reviews citing this publication (3)

  1. Non-Hydroxamate Zinc-Binding Groups as Warheads for Histone Deacetylases. Frühauf A, Meyer-Almes FJ. Molecules 26 5151 (2021)
  2. Isoform-Selective Versus Nonselective Histone Deacetylase Inhibitors in HIV Latency Reversal. Boateng AT, Abaidoo-Myles A, Bonney EY, Kyei GB. AIDS Res Hum Retroviruses 38 615-621 (2022)
  3. Significance of Five-Membered Heterocycles in Human Histone Deacetylase Inhibitors. Frühauf A, Behringer M, Meyer-Almes FJ. Molecules 28 5686 (2023)

Articles citing this publication (4)

  1. Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group. Liu J, Yu Y, Kelly J, Sha D, Alhassan AB, Yu W, Maletic MM, Duffy JL, Klein DJ, Holloway MK, Carroll S, Howell BJ, Barnard RJO, Wolkenberg S, Kozlowski JA. ACS Med Chem Lett 11 2476-2483 (2020)
  2. Synthesis of HDAC Inhibitor Libraries via Microscale Workflow. Dykstra KD, Streckfuss E, Liu M, Liu J, Yu Y, Wang M, Kozlowski JA, Myers RW, Buevich AV, Maletic MM, Vachal P, Krska SW. ACS Med Chem Lett 12 337-342 (2021)
  3. A histone deacetylase network regulates epigenetic reprogramming and viral silencing in HIV-infected cells. Peterson JJ, Lewis CA, Burgos SD, Manickam A, Xu Y, Rowley AA, Clutton G, Richardson B, Zou F, Simon JM, Margolis DM, Goonetilleke N, Browne EP. Cell Chem Biol 30 1617-1633.e9 (2023)
  4. Enantioselective Bioreduction of Medicinally Relevant Nitrogen-Heteroaromatic Ketones. Bai WJ, Estrada MA, Gartman JA, Judd AS. ACS Med Chem Lett 14 846-852 (2023)


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