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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: stamford aw. 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
Recruitment of FBXO22 for Targeted Degradation of NSD2.
Nie DY, Tabor JR, Li J, Kutera M, St-Germain J, Hanley RP, Wolf E, Paulakonis E, Kenney TMG, Duan S, Shrestha S, Owens DDG, Pon A, Szewczyk M, Lamberto AJ, Menes M, Li F, Barsyte-Lovejoy D, Brown NG, Barsotti AM, Stamford AW, Collins JL, Wilson DJ, Raught B, Licht JD, James LI, Arrowsmith CH. Nie DY, et al. Among authors: stamford aw. bioRxiv [Preprint]. 2023 Nov 30:2023.11.01.564830. doi: 10.1101/2023.11.01.564830. bioRxiv. 2023. PMID: 37961297 Free PMC article. Preprint.
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: stamford aw. 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.
Structure-function analysis of the SHOC2-MRAS-PP1C holophosphatase complex.
Kwon JJ, Hajian B, Bian Y, Young LC, Amor AJ, Fuller JR, Fraley CV, Sykes AM, So J, Pan J, Baker L, Lee SJ, Wheeler DB, Mayhew DL, Persky NS, Yang X, Root DE, Barsotti AM, Stamford AW, Perry CK, Burgin A, McCormick F, Lemke CT, Hahn WC, Aguirre AJ. Kwon JJ, et al. Among authors: stamford aw. Nature. 2022 Sep;609(7926):408-415. doi: 10.1038/s41586-022-04928-2. Epub 2022 Jul 13. Nature. 2022. PMID: 35831509 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: stamford aw. 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.
Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules.
Singh K, Lin J, Lecomte N, Mohan P, Gokce A, Sanghvi VR, Jiang M, Grbovic-Huezo O, Burčul A, Stark SG, Romesser PB, Chang Q, Melchor JP, Beyer RK, Duggan M, Fukase Y, Yang G, Ouerfelli O, Viale A, de Stanchina E, Stamford AW, Meinke PT, Rätsch G, Leach SD, Ouyang Z, Wendel HG. Singh K, et al. Among authors: stamford aw. Cancer Res. 2021 Apr 15;81(8):2002-2014. doi: 10.1158/0008-5472.CAN-20-2929. Epub 2021 Feb 25. Cancer Res. 2021. PMID: 33632898 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: stamford aw. 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.
Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.
Mandal M, Mitra K, Grotz D, Lin X, Palamanda J, Kumari P, Buevich A, Caldwell JP, Chen X, Cox K, Favreau L, Hyde L, Kennedy ME, Kuvelkar R, Liu X, Mazzola RD, Parker E, Rindgen D, Sherer E, Wang H, Zhu Z, Stamford AW, Cumming JN. Mandal M, et al. Among authors: stamford aw. J Med Chem. 2018 Dec 13;61(23):10700-10708. doi: 10.1021/acs.jmedchem.8b01326. Epub 2018 Nov 15. J Med Chem. 2018. PMID: 30388368
Discovery of MK-8282 as a Potent G-Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes.
Neelamkavil SF, Stamford AW, Kowalski T, Biswas D, Boyle C, Chackalamannil S, Xia Y, Jayne C, Neustadt B, Hao J, Liu H, Dai X, Baker H, Hawes B, O'Neill K, Tang H, Greenlee WJ. Neelamkavil SF, et al. Among authors: stamford aw. ACS Med Chem Lett. 2018 Apr 10;9(5):457-461. doi: 10.1021/acsmedchemlett.8b00073. eCollection 2018 May 10. ACS Med Chem Lett. 2018. PMID: 29795759 Free PMC article.
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.
Bungard CJ, Williams PD, Schulz J, Wiscount CM, Holloway MK, Loughran HM, Manikowski JJ, Su HP, Bennett DJ, Chang L, Chu XJ, Crespo A, Dwyer MP, Keertikar K, Morriello GJ, Stamford AW, Waddell ST, Zhong B, Hu B, Ji T, Diamond TL, Bahnck-Teets C, Carroll SS, Fay JF, Min X, Morris W, Ballard JE, Miller MD, McCauley JA. Bungard CJ, et al. Among authors: stamford aw. ACS Med Chem Lett. 2017 Nov 13;8(12):1292-1297. doi: 10.1021/acsmedchemlett.7b00386. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259750 Free PMC article.
38 results