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Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen.
Bukhtiyarova M, Cook EM, Hancock PJ, Hruza AW, Shaw AW, Adam GC, Barnard RJO, McKenna PM, Holloway MK, Bell IM, Carroll S, Cornella-Taracido I, Cox CD, Kutchukian PS, Powell DA, Strickland C, Trotter BW, Tudor M, Wolkenberg S, Li J, Tellers DM. Bukhtiyarova M, et al. Among authors: barnard rjo. ACS Med Chem Lett. 2020 Dec 23;12(1):99-106. doi: 10.1021/acsmedchemlett.0c00551. eCollection 2021 Jan 14. ACS Med Chem Lett. 2020. PMID: 33488970 Free PMC article.
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. Liu J, et al. Among authors: barnard rjo. ACS Med Chem Lett. 2020 Oct 13;11(12):2476-2483. doi: 10.1021/acsmedchemlett.0c00462. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335670 Free PMC article.
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
Beshore DC, Adam GC, Barnard RJO, Burlein C, Gallicchio SN, Holloway MK, Krosky D, Lemaire W, Myers RW, Patel S, Plotkin MA, Powell DA, Rada V, Cox CD, Coleman PJ, Klein DJ, Wolkenberg SE. Beshore DC, et al. Among authors: barnard rjo. ACS Med Chem Lett. 2021 Mar 7;12(4):540-547. doi: 10.1021/acsmedchemlett.1c00074. eCollection 2021 Apr 8. ACS Med Chem Lett. 2021. PMID: 33854701 Free PMC article.
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
Liu J, Kelly J, Yu W, Clausen D, Yu Y, Kim H, Duffy JL, Chung CC, Myers RW, Carroll S, Klein DJ, Fells J, Holloway MK, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski JA. Liu J, et al. Among authors: barnard rjo. ACS Med Chem Lett. 2020 Jun 22;11(7):1476-1483. doi: 10.1021/acsmedchemlett.0c00302. eCollection 2020 Jul 9. ACS Med Chem Lett. 2020. PMID: 32676157 Free PMC article.
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.
Yu W, Liu J, Clausen D, Yu Y, Duffy JL, Wang M, Xu S, Deng L, Suzuki T, Chung CC, Myers RW, Klein DJ, Fells JI, Holloway MK, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski J. Yu W, et al. Among authors: barnard rjo. J Med Chem. 2021 Apr 22;64(8):4709-4729. doi: 10.1021/acs.jmedchem.0c02150. Epub 2021 Apr 2. J Med Chem. 2021. PMID: 33797924
CHEMGENIE: integration of chemogenomics data for applications in chemical biology.
Kutchukian PS, Chang C, Fox SJ, Cook E, Barnard R, Tellers D, Wang H, Pertusi D, Glick M, Sheridan RP, Wallace IM, Wassermann AM. Kutchukian PS, et al. Drug Discov Today. 2018 Jan;23(1):151-160. doi: 10.1016/j.drudis.2017.09.004. Epub 2017 Sep 14. Drug Discov Today. 2018. PMID: 28917822 Review.
Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Yu W, Liu J, Yu Y, Zhang V, Clausen D, Kelly J, Wolkenberg S, Beshore D, Duffy JL, Chung CC, Myers RW, Klein DJ, Fells J, Holloway K, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski J. Yu W, et al. Among authors: barnard rjo. Bioorg Med Chem Lett. 2020 Jul 1;30(13):127197. doi: 10.1016/j.bmcl.2020.127197. Epub 2020 Apr 15. Bioorg Med Chem Lett. 2020. PMID: 32331932
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. Clausen DJ, et al. Among authors: barnard rjo. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127367. doi: 10.1016/j.bmcl.2020.127367. Epub 2020 Jun 26. Bioorg Med Chem Lett. 2020. PMID: 32738976
53 results