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Page 1
Strategic Fluorination to Achieve a Potent, Selective, Metabolically Stable, and Orally Bioavailable Inhibitor of CSNK2.
Ong HW, Yang X, Smith JL, Taft-Benz S, Howell S, Dickmander RJ, Havener TM, Sanders MK, Brown JW, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM. Ong HW, et al. Among authors: havener tm. Molecules. 2024 Sep 2;29(17):4158. doi: 10.3390/molecules29174158. Molecules. 2024. PMID: 39275006 Free PMC article.
More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication.
Ong HW, Yang X, Smith JL, Dickmander RJ, Brown JW, Havener TM, Taft-Benz S, Howell S, Sanders MK, Capener JL, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM. Ong HW, et al. Among authors: havener tm. J Med Chem. 2024 Jul 25;67(14):12261-12313. doi: 10.1021/acs.jmedchem.4c00962. Epub 2024 Jul 3. J Med Chem. 2024. PMID: 38959455 Free PMC article.
Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial PfGSK3/PfPK6 with Activity against Blood Stage Parasites In Vitro.
Galal KA, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin ME, Merten E, Ong HW, Willis C, Abdelwaly A, Helal MA, Derbyshire ER, Zutshi R, Drewry DH. Galal KA, et al. Among authors: havener tm. J Med Chem. 2022 Oct 13;65(19):13172-13197. doi: 10.1021/acs.jmedchem.2c00996. Epub 2022 Sep 27. J Med Chem. 2022. PMID: 36166733 Free PMC article.
Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2.
Davis-Gilbert ZW, Krämer A, Dunford JE, Howell S, Senbabaoglu F, Wells CI, Bashore FM, Havener TM, Smith JL, Hossain MA, Oppermann U, Drewry DH, Axtman AD. Davis-Gilbert ZW, et al. Among authors: havener tm. ACS Med Chem Lett. 2023 Mar 14;14(4):432-441. doi: 10.1021/acsmedchemlett.2c00530. eCollection 2023 Apr 13. ACS Med Chem Lett. 2023. PMID: 37077385 Free PMC article.
Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore.
Ong HW, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin M, Galal KA, Willis C, Krämer A, Liu S, Knapp S, Derbyshire ER, Zutshi R, Drewry DH. Ong HW, et al. Among authors: havener tm. Eur J Med Chem. 2023 Mar 5;249:115043. doi: 10.1016/j.ejmech.2022.115043. Epub 2022 Dec 30. Eur J Med Chem. 2023. PMID: 36736152 Free PMC article.
Multi-omic profiling reveals the ataxia protein sacsin is required for integrin trafficking and synaptic organization.
Romano LEL, Aw WY, Hixson KM, Novoselova TV, Havener TM, Howell S, Taylor-Blake B, Hall CL, Xing L, Beri J, Nethisinghe S, Perna L, Hatimy A, Altadonna GC, Graves LM, Herring LE, Hickey AJ, Thalassinos K, Chapple JP, Wolter JM. Romano LEL, et al. Among authors: havener tm. Cell Rep. 2022 Nov 1;41(5):111580. doi: 10.1016/j.celrep.2022.111580. Cell Rep. 2022. PMID: 36323248 Free PMC article.
31 results