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Regulated Induced Proximity Targeting Chimeras (RIPTACs): a Novel Heterobifunctional Small Molecule Therapeutic Strategy for Killing Cancer Cells Selectively.
Raina K, Forbes CD, Stronk R, Rappi JP Jr, Eastman KJ, Gerritz SW, Yu X, Li H, Bhardwaj A, Forgione M, Hundt A, King MP, Posner ZM, Denny A, McGovern A, Puleo DE, Garvin E, Chenard R, Zaware N, Mousseau JJ, Macaluso J, Martin M, Bassoli K, Jones K, Garcia M, Howard K, Smith LM, Chen JM, De Leon CA, Hines J, Kayser-Bricker KJ, Crews CM. Raina K, et al. Among authors: eastman kj. bioRxiv [Preprint]. 2023 Jan 2:2023.01.01.522436. doi: 10.1101/2023.01.01.522436. bioRxiv. 2023. PMID: 36711980 Free PMC article. Preprint.
The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase.
Eastman KJ, Parcella K, Yeung KS, Grant-Young KA, Zhu J, Wang T, Zhang Z, Yin Z, Beno BR, Sheriff S, Kish K, Tredup J, Jardel AG, Halan V, Ghosh K, Parker D, Mosure K, Fang H, Wang YK, Lemm J, Zhuo X, Hanumegowda U, Rigat K, Donoso M, Tuttle M, Zvyaga T, Haarhoff Z, Meanwell NA, Soars MG, Roberts SB, Kadow JF. Eastman KJ, et al. Medchemcomm. 2017 Feb 8;8(4):796-806. doi: 10.1039/c6md00636a. eCollection 2017 Apr 1. Medchemcomm. 2017. PMID: 30108798 Free PMC article.
Phosphocholine conjugation: an unexpected in vivo conjugation pathway associated with hepatitis c ns5b inhibitors featuring a bicyclo[1.1.1]pentane.
Zhuo X, Cantone JL, Wang Y, Leet JE, Drexler DM, Yeung KS, Huang XS, Eastman KJ, Parcella KE, Mosure KW, Soars MG, Kadow JF, Johnson BM. Zhuo X, et al. Among authors: eastman kj. Drug Metab Dispos. 2016 Aug;44(8):1332-1340. doi: 10.1124/dmd.115.069062. Epub 2016 Mar 9. Drug Metab Dispos. 2016. PMID: 26961241
Applications of Fluorine in Medicinal Chemistry.
Gillis EP, Eastman KJ, Hill MD, Donnelly DJ, Meanwell NA. Gillis EP, et al. Among authors: eastman kj. J Med Chem. 2015 Nov 12;58(21):8315-59. doi: 10.1021/acs.jmedchem.5b00258. Epub 2015 Jul 22. J Med Chem. 2015. PMID: 26200936 Review.
Identification of a novel series of potent HCV NS5B Site I inhibitors.
Eastman KJ, Yang Z, Bender JA, Mosure K, Lemm JA, Meanwell NA, Roberts SB, Knipe J, Kadow JF. Eastman KJ, et al. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1993-7. doi: 10.1016/j.bmcl.2014.02.047. Epub 2014 Feb 28. Bioorg Med Chem Lett. 2014. PMID: 24656612
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