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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: meinke pt. 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
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: meinke pt. 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.
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: meinke pt. 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.
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: meinke pt. 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.
Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression.
Lama L, Adura C, Xie W, Tomita D, Kamei T, Kuryavyi V, Gogakos T, Steinberg JI, Miller M, Ramos-Espiritu L, Asano Y, Hashizume S, Aida J, Imaeda T, Okamoto R, Jennings AJ, Michino M, Kuroita T, Stamford A, Gao P, Meinke P, Glickman JF, Patel DJ, Tuschl T. Lama L, et al. Nat Commun. 2019 May 21;10(1):2261. doi: 10.1038/s41467-019-08620-4. Nat Commun. 2019. PMID: 31113940 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: meinke pt. 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.
Design, Synthesis, and Optimization of Macrocyclic Peptides as Species-Selective Antimalaria Proteasome Inhibitors.
Zhang H, Ginn J, Zhan W, Liu YJ, Leung A, Toita A, Okamoto R, Wong TT, Imaeda T, Hara R, Yukawa T, Michino M, Vendome J, Beuming T, Sato K, Aso K, Meinke PT, Nathan CF, Kirkman LA, Lin G. Zhang H, et al. Among authors: meinke pt. J Med Chem. 2022 Jul 14;65(13):9350-9375. doi: 10.1021/acs.jmedchem.2c00611. Epub 2022 Jun 21. J Med Chem. 2022. PMID: 35727231 Free PMC article.
Structure-Activity Relationship Studies of Antimalarial Plasmodium Proteasome Inhibitors─Part II.
Zhang H, Ginn J, Zhan W, Leung A, Liu YJ, Toita A, Okamoto R, Wong TT, Imaeda T, Hara R, Michino M, Yukawa T, Chelebieva S, Tumwebaze PK, Vendome J, Beuming T, Sato K, Aso K, Rosenthal PJ, Cooper RA, Liverton N, Foley M, Meinke PT, Nathan CF, Kirkman LA, Lin G. Zhang H, et al. Among authors: meinke pt. J Med Chem. 2023 Jan 26;66(2):1484-1508. doi: 10.1021/acs.jmedchem.2c01651. Epub 2023 Jan 11. J Med Chem. 2023. PMID: 36630286 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: meinke pt. 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
Whole Cell Active Inhibitors of Mycobacterial Lipoamide Dehydrogenase Afford Selectivity over the Human Enzyme through Tight Binding Interactions.
Ginn J, Jiang X, Sun S, Michino M, Huggins DJ, Mbambo Z, Jansen R, Rhee KY, Arango N, Lima CD, Liverton N, Imaeda T, Okamoto R, Kuroita T, Aso K, Stamford A, Foley M, Meinke PT, Nathan C, Bryk R. Ginn J, et al. Among authors: meinke pt. ACS Infect Dis. 2021 Feb 12;7(2):435-444. doi: 10.1021/acsinfecdis.0c00788. Epub 2021 Feb 2. ACS Infect Dis. 2021. PMID: 33527832 Free PMC article.
92 results