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Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.
Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA; NIH Molecular Libraries Project Team. Schreiber SL, et al. Among authors: jackson mr. Cell. 2015 Jun 4;161(6):1252-65. doi: 10.1016/j.cell.2015.05.023. Cell. 2015. PMID: 26046436 Free PMC article. Review.
Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor.
Pinkerton AB, Sergienko E, Bravo Y, Dahl R, Ma CT, Sun Q, Jackson MR, Cosford NDP, Millán JL. Pinkerton AB, et al. Among authors: jackson mr. Bioorg Med Chem Lett. 2018 Jan 1;28(1):31-34. doi: 10.1016/j.bmcl.2017.11.024. Epub 2017 Nov 11. Bioorg Med Chem Lett. 2018. PMID: 29174347 Free PMC article.
Identification and characterization of small molecule inhibitors of the ubiquitin ligases Siah1/2 in melanoma and prostate cancer cells.
Feng Y, Sessions EH, Zhang F, Ban F, Placencio-Hickok V, Ma CT, Zeng FY, Pass I, Terry DB, Cadwell G, Bankston LA, Liddington RC, Chung TDY, Pinkerton AB, Sergienko E, Gleave M, Bhowmick NA, Jackson MR, Cherkasov A, Ronai ZA. Feng Y, et al. Among authors: jackson mr. Cancer Lett. 2019 May 1;449:145-162. doi: 10.1016/j.canlet.2019.02.012. Epub 2019 Feb 14. Cancer Lett. 2019. PMID: 30771432 Free PMC article.
Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.
Pinkerton AB, Peddibhotla S, Yamamoto F, Slosky LM, Bai Y, Maloney P, Hershberger P, Hedrick MP, Falter B, Ardecky RJ, Smith LH, Chung TDY, Jackson MR, Caron MG, Barak LS. Pinkerton AB, et al. Among authors: jackson mr. J Med Chem. 2019 Sep 12;62(17):8357-8363. doi: 10.1021/acs.jmedchem.9b00340. Epub 2019 Aug 20. J Med Chem. 2019. PMID: 31390201 Free PMC article.
Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators.
Pinkerton AB, Sessions EH, Hershberger P, Maloney PR, Peddibhotla S, Hopf M, Sergienko E, Ma CT, Smith LH, Jackson MR, Tanaka J, Tsuji T, Akiu M, Cohen SE, Nakamura T, Gardell SJ. Pinkerton AB, et al. Among authors: jackson mr. Bioorg Med Chem Lett. 2021 Jun 1;41:128007. doi: 10.1016/j.bmcl.2021.128007. Epub 2021 Mar 31. Bioorg Med Chem Lett. 2021. PMID: 33798699
Discovery of Orally Bioavailable Purine-Based Inhibitors of the Low-Molecular-Weight Protein Tyrosine Phosphatase.
Stanford SM, Diaz MA, Ardecky RJ, Zou J, Roosild T, Holmes ZJ, Nguyen TP, Hedrick MP, Rodiles S, Guan A, Grotegut S, Santelli E, Chung TDY, Jackson MR, Bottini N, Pinkerton AB. Stanford SM, et al. Among authors: jackson mr. J Med Chem. 2021 May 13;64(9):5645-5653. doi: 10.1021/acs.jmedchem.0c02126. Epub 2021 Apr 29. J Med Chem. 2021. PMID: 33914534 Free PMC article.
261 results