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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: capener jl. 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.
Illumination of understudied ciliary kinases.
Flax RG, Rosston P, Rocha C, Anderson B, Capener JL, Durcan TM, Drewry DH, Prinos P, Axtman AD. Flax RG, et al. Among authors: capener jl. Front Mol Biosci. 2024 Mar 8;11:1352781. doi: 10.3389/fmolb.2024.1352781. eCollection 2024. Front Mol Biosci. 2024. PMID: 38523660 Free PMC article. Review.
A PKA inhibitor motif within SMOOTHENED controls Hedgehog signal transduction.
Happ JT, Arveseth CD, Bruystens J, Bertinetti D, Nelson IB, Olivieri C, Zhang J, Hedeen DS, Zhu JF, Capener JL, Bröckel JW, Vu L, King CC, Ruiz-Perez VL, Ge X, Veglia G, Herberg FW, Taylor SS, Myers BR. Happ JT, et al. Among authors: capener jl. Nat Struct Mol Biol. 2022 Oct;29(10):990-999. doi: 10.1038/s41594-022-00838-z. Epub 2022 Oct 6. Nat Struct Mol Biol. 2022. PMID: 36202993 Free PMC article.
Smoothened transduces Hedgehog signals via activity-dependent sequestration of PKA catalytic subunits.
Arveseth CD, Happ JT, Hedeen DS, Zhu JF, Capener JL, Klatt Shaw D, Deshpande I, Liang J, Xu J, Stubben SL, Nelson IB, Walker MF, Kawakami K, Inoue A, Krogan NJ, Grunwald DJ, Hüttenhain R, Manglik A, Myers BR. Arveseth CD, et al. Among authors: capener jl. PLoS Biol. 2021 Apr 22;19(4):e3001191. doi: 10.1371/journal.pbio.3001191. eCollection 2021 Apr. PLoS Biol. 2021. PMID: 33886552 Free PMC article.