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Page 1
The Next-Generation Oral Selective Estrogen Receptor Degrader Camizestrant (AZD9833) Suppresses ER+ Breast Cancer Growth and Overcomes Endocrine and CDK4/6 Inhibitor Resistance.
Lawson M, Cureton N, Ros S, Cheraghchi-Bashi A, Urosevic J, D'Arcy S, Delpuech O, DuPont M, Fisher DI, Gangl ET, Lewis H, Trueman D, Wali N, Williamson SC, Moss J, Montaudon E, Derrien H, Marangoni E, Miragaia RJ, Gagrica S, Morentin-Gutierrez P, Moss TA, Maglennon G, Sutton D, Polanski R, Rosen A, Cairns J, Zhang P, Sánchez-Guixé M, Serra V, Critchlow SE, Scott JS, Lindemann JPO, Barry ST, Klinowska T, Morrow CJ, Carnevalli LS. Lawson M, et al. Among authors: gangl et. Cancer Res. 2023 Dec 1;83(23):3989-4004. doi: 10.1158/0008-5472.CAN-23-0694. Cancer Res. 2023. PMID: 37725704 Free PMC article.
Novel Arginase Inhibitor, AZD0011, Demonstrates Immune Cell Stimulation and Antitumor Efficacy with Diverse Combination Partners.
Doshi AS, Cantin S, Hernandez M, Srinivasan S, Tentarelli S, Griffin M, Wang Y, Pop-Damkov P, Prickett LB, Kankkonen C, Shen M, Martin MS, Wu S, Castaldi MP, Ghadially H, Varnes J, Gales S, Henry D, Hoover C, Mele DA, Simpson I, Gangl ET, Mlynarski SN, Finlay MRV, Drew L, Fawell SE, Shao W, Schuller AG. Doshi AS, et al. Among authors: gangl et. Mol Cancer Ther. 2023 May 4;22(5):630-645. doi: 10.1158/1535-7163.MCT-22-0431. Mol Cancer Ther. 2023. PMID: 36912782
A phase 2 study of AZD4635 in combination with durvalumab or oleclumab in patients with metastatic castration-resistant prostate cancer.
Falchook GS, Reeves J, Gandhi S, Spigel DR, Arrowsmith E, George DJ, Karlix J, Pouliot G, Hattersley MM, Gangl ET, James GD, Thompson J, Russell DL, Patel B, Kumar R, Lim E. Falchook GS, et al. Among authors: gangl et. Cancer Immunol Immunother. 2024 Mar 2;73(4):72. doi: 10.1007/s00262-024-03640-6. Cancer Immunol Immunother. 2024. PMID: 38430405 Free PMC article. Clinical Trial.
Discovery of (2R,4R)-4-((S)-2-Amino-3-methylbutanamido)-2-(4-boronobutyl)pyrrolidine-2-carboxylic Acid (AZD0011), an Actively Transported Prodrug of a Potent Arginase Inhibitor to Treat Cancer.
Mlynarski SN, Aquila BM, Cantin S, Cook S, Doshi A, Finlay MRV, Gangl ET, Grebe T, Gu C, Kawatkar SP, Petersen J, Pop-Damkov P, Schuller AG, Shao W, Shields JD, Simpson I, Tavakoli S, Tentarelli S, Throner S, Wang H, Wang J, Wu D, Ye Q. Mlynarski SN, et al. Among authors: gangl et. J Med Chem. 2024 Dec 12;67(23):20827-20841. doi: 10.1021/acs.jmedchem.4c02309. Epub 2024 Nov 21. J Med Chem. 2024. PMID: 39572889
Design and Synthesis of Acyclic Boronic Acid Arginase Inhibitors.
Shields JD, Aquila BM, Emmons D, Finlay MRV, Gangl ET, Gu C, Mlynarski SN, Petersen J, Pop-Damkov P, Sha L, Simpson I, Tavakoli S, Tentarelli S, Wang H, Ye Q, Zheng X. Shields JD, et al. Among authors: gangl et. J Med Chem. 2024 Dec 12;67(23):20799-20826. doi: 10.1021/acs.jmedchem.4c02295. Epub 2024 Nov 14. J Med Chem. 2024. PMID: 39540340
A phase II study (AARDVARC) of AZD4635 in combination with durvalumab and cabazitaxel in patients with progressive, metastatic, castration-resistant prostate cancer.
Alonso-Gordoa T, Goodman M, Vulsteke C, Roubaud G, Zhang J, Parikh M, Piulats JM, Azaro A, James GD, Cavazzina R, Gangl ET, Thompson J, Pouliot G, Kumar R, Sweeney C. Alonso-Gordoa T, et al. Among authors: gangl et. ESMO Open. 2024 Jun;9(6):103446. doi: 10.1016/j.esmoop.2024.103446. Epub 2024 Jun 4. ESMO Open. 2024. PMID: 38838502 Free PMC article. Clinical Trial.
Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.
Scott JS, Stead D, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Cureton N, Davey PRJ, Fisher DI, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Hughes SJ, Hunt TA, Johnson T, Kavanagh SL, Klinowska TCM, Larner CJB, Lawson M, Lister AS, Longmire D, Marden S, McGuire TM, McMillan C, McMurray L, Morrow CJ, Nissink JWM, Moss TA, O'Donovan DH, Polanski R, Stokes S, Thakur K, Trueman D, Truman C, Tucker MJ, Wang H, Whalley N, Wu D, Wu Y, Yang B, Yang W. Scott JS, et al. Among authors: gangl et. J Med Chem. 2023 Feb 23;66(4):2918-2945. doi: 10.1021/acs.jmedchem.2c01964. Epub 2023 Feb 1. J Med Chem. 2023. PMID: 36727211
Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.
Scott JS, Moss TA, Barlaam B, Davey PRJ, Fairley G, Gangl ET, Greenwood RDR, Hatoum-Mokdad H, Lister AS, Longmire D, Polanski R, Stokes S, Tucker MJ, Varnes JG, Yang B. Scott JS, et al. Among authors: gangl et. ACS Med Chem Lett. 2020 Oct 28;11(12):2519-2525. doi: 10.1021/acsmedchemlett.0c00505. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335676 Free PMC article.
16 results