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Page 1
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.
Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity.
Coburn CA, Meinke PT, Chang W, Fandozzi CM, Graham DJ, Hu B, Huang Q, Kargman S, Kozlowski J, Liu R, McCauley JA, Nomeir AA, Soll RM, Vacca JP, Wang D, Wu H, Zhong B, Olsen DB, Ludmerer SW. Coburn CA, et al. Among authors: kargman s. ChemMedChem. 2013 Dec;8(12):1930-40. doi: 10.1002/cmdc.201300343. Epub 2013 Oct 14. ChemMedChem. 2013. PMID: 24127258
Identification of an indole series of prostaglandin D2 receptor antagonists.
Sturino CF, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N, Brideau C, Cauchon E, Carriere MC, Denis D, Greig G, Kargman S, Lamontagne S, Mathieu MC, Sawyer N, Slipetz D, O'Neill G, Wang Z, Zamboni R, Metters KM, Young RN. Sturino CF, et al. Among authors: kargman s. Bioorg Med Chem Lett. 2006 Jun 1;16(11):3043-8. doi: 10.1016/j.bmcl.2006.02.062. Epub 2006 Mar 10. Bioorg Med Chem Lett. 2006. PMID: 16529930
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.
Design, synthesis, and evaluation of novel 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective CXCR2 chemokine receptor antagonists.
Liu S, Liu Y, Wang H, Ding Y, Wu H, Dong J, Wong A, Chen SH, Li G, Chan M, Sawyer N, Gervais FG, Henault M, Kargman S, Bedard LL, Han Y, Friesen R, Lobell RB, Stout DM. Liu S, et al. Among authors: kargman s. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5741-5. doi: 10.1016/j.bmcl.2009.08.014. Epub 2009 Aug 7. Bioorg Med Chem Lett. 2009. PMID: 19713110
2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Ducharme Y, Blouin M, Carrière MC, Chateauneuf A, Côté B, Denis D, Frenette R, Greig G, Kargman S, Lamontagne S, Martins E, Nantel F, O'Neill G, Sawyer N, Metters KM, Friesen RW. Ducharme Y, et al. Among authors: kargman s. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1155-60. doi: 10.1016/j.bmcl.2004.12.005. Bioorg Med Chem Lett. 2005. PMID: 15686932
The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14.
Gauthier JY, Belley M, Deschênes D, Fournier JF, Gagné S, Gareau Y, Hamel M, Hénault M, Hyjazie H, Kargman S, Lavallée G, Levesque JF, Li L, Mamane Y, Mancini J, Morin N, Mulrooney E, Robichaud J, Thérien M, Tranmer G, Wang Z, Wu J, Black WC. Gauthier JY, et al. Among authors: kargman s. Bioorg Med Chem Lett. 2011 May 15;21(10):2836-9. doi: 10.1016/j.bmcl.2011.03.081. Epub 2011 Mar 31. Bioorg Med Chem Lett. 2011. PMID: 21507640
65 results