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Page 1
Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055.
Michino M, Khan TA, Miller MW, Fukase Y, Vendome J, Adura C, Glickman JF, Liu Y, Wan L, Allis CD, Stamford AW, Meinke PT, Renzetti LM, Kargman S, Liverton NJ, Huggins DJ. Michino M, et al. Among authors: kargman s. ACS Med Chem Lett. 2024 Mar 12;15(4):524-532. doi: 10.1021/acsmedchemlett.4c00016. eCollection 2024 Apr 11. ACS Med Chem Lett. 2024. PMID: 38628784
Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.
Miller M, Rossetti T, Ferreira J, Ghanem L, Balbach M, Kaur N, Levin LR, Buck J, Kehr M, Coquille S, van den Heuvel J, Steegborn C, Fushimi M, Finkin-Groner E, Myers RW, Kargman S, Liverton NJ, Huggins DJ, Meinke PT. Miller M, et al. Among authors: kargman s. J Med Chem. 2022 Nov 24;65(22):15208-15226. doi: 10.1021/acs.jmedchem.2c01133. Epub 2022 Nov 8. J Med Chem. 2022. PMID: 36346696 Free PMC article.
Scaffold Hopping and Optimization of Small Molecule Soluble Adenyl Cyclase Inhibitors Led by Free Energy Perturbation.
Sun S, Fushimi M, Rossetti T, Kaur N, Ferreira J, Miller M, Quast J, van den Heuvel J, Steegborn C, Levin LR, Buck J, Myers RW, Kargman S, Liverton N, Meinke PT, Huggins DJ. Sun S, et al. Among authors: kargman s. J Chem Inf Model. 2023 May 8;63(9):2828-2841. doi: 10.1021/acs.jcim.2c01577. Epub 2023 Apr 15. J Chem Inf Model. 2023. PMID: 37060320
Addition to "Scaffold Hopping and Optimization of Small Molecule Soluble Adenyl Cyclase Inhibitors Led by Free Energy Perturbation".
Sun S, Fushimi M, Rossetti T, Kaur N, Ferreira J, Miller M, Quast J, van den Heuvel J, Steegborn C, Levin LR, Buck J, Myers RW, Kargman S, Liverton N, Meinke PT, Huggins DJ. Sun S, et al. Among authors: kargman s. J Chem Inf Model. 2024 Feb 12;64(3):1106. doi: 10.1021/acs.jcim.4c00068. Epub 2024 Jan 23. J Chem Inf Model. 2024. PMID: 38258980 No abstract available.
Small-Molecule Inhibition of the Acyl-Lysine Reader ENL as a Strategy against Acute Myeloid Leukemia.
Liu Y, Li Q, Alikarami F, Barrett DR, Mahdavi L, Li H, Tang S, Khan TA, Michino M, Hill C, Song L, Yang L, Li Y, Pokharel SP, Stamford AW, Liverton N, Renzetti LM, Taylor S, Watt GF, Ladduwahetty T, Kargman S, Meinke PT, Foley MA, Shi J, Li H, Carroll M, Chen CW, Gardini A, Maillard I, Huggins DJ, Bernt KM, Wan L. Liu Y, et al. Among authors: kargman s. Cancer Discov. 2022 Nov 2;12(11):2684-2709. doi: 10.1158/2159-8290.CD-21-1307. Cancer Discov. 2022. PMID: 36053276 Free PMC article.
A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors.
Liang R, Tomita D, Sasaki Y, Ginn J, Michino M, Huggins DJ, Baxt L, Kargman S, Shahid M, Aso K, Duggan M, Stamford AW, DeStanchina E, Liverton N, Meinke PT, Foley MA, Phillips RE. Liang R, et al. Among authors: kargman s. ACS Med Chem Lett. 2022 Feb 10;13(3):377-387. doi: 10.1021/acsmedchemlett.1c00448. eCollection 2022 Mar 10. ACS Med Chem Lett. 2022. PMID: 35300079 Free PMC article.
Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10).
Fushimi M, Buck H, Balbach M, Gorovyy A, Ferreira J, Rossetti T, Kaur N, Levin LR, Buck J, Quast J, van den Heuvel J, Steegborn C, Finkin-Groner E, Kargman S, Michino M, Foley MA, Miller M, Liverton NJ, Huggins DJ, Meinke PT. Fushimi M, et al. Among authors: kargman s. ACS Med Chem Lett. 2021 Jul 14;12(8):1283-1287. doi: 10.1021/acsmedchemlett.1c00273. eCollection 2021 Aug 12. ACS Med Chem Lett. 2021. PMID: 34413957 Free PMC article.
Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells.
Mullarky E, Xu J, Robin AD, Huggins DJ, Jennings A, Noguchi N, Olland A, Lakshminarasimhan D, Miller M, Tomita D, Michino M, Su T, Zhang G, Stamford AW, Meinke PT, Kargman S, Cantley LC. Mullarky E, et al. Among authors: kargman s. Bioorg Med Chem Lett. 2019 Sep 1;29(17):2503-2510. doi: 10.1016/j.bmcl.2019.07.011. Epub 2019 Jul 6. Bioorg Med Chem Lett. 2019. PMID: 31327531 Free PMC article.
Antibacterial small molecules targeting the conserved TOPRIM domain of DNA gyrase.
Walker SS, Labroli M, Painter RE, Wiltsie J, Sherborne B, Murgolo N, Sher X, Mann P, Zuck P, Garlisi CG, Su J, Kargman S, Xiao L, Scapin G, Salowe S, Devito K, Sheth P, Buist N, Tan CM, Black TA, Roemer T. Walker SS, et al. Among authors: kargman s. PLoS One. 2017 Jul 10;12(7):e0180965. doi: 10.1371/journal.pone.0180965. eCollection 2017. PLoS One. 2017. PMID: 28700746 Free PMC article.
Discovery of MK-8831, A Novel Spiro-Proline Macrocycle as a Pan-Genotypic HCV-NS3/4a Protease Inhibitor.
Neelamkavil SF, Agrawal S, Bara T, Bennett C, Bhat S, Biswas D, Brockunier L, Buist N, Burnette D, Cartwright M, Chackalamannil S, Chase R, Chelliah M, Chen A, Clasby M, Colandrea VJ, Davies IW, Eagen K, Guo Z, Han Y, Howe J, Jayne C, Josien H, Kargman S, Marcantonio K, Miao S, Miller R, Nolting A, Pinto P, Rajagopalan M, Ruck RT, Shah U, Soriano A, Sperbeck D, Velazquez F, Wu J, Xia Y, Venkatraman S. Neelamkavil SF, et al. Among authors: kargman s. ACS Med Chem Lett. 2015 Dec 22;7(1):111-6. doi: 10.1021/acsmedchemlett.5b00425. eCollection 2016 Jan 14. ACS Med Chem Lett. 2015. PMID: 26819676 Free PMC article.
65 results