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Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer.
Han X, Zhao L, Xiang W, Miao B, Qin C, Wang M, Xu T, McEachern D, Lu J, Wang Y, Metwally H, Yang CY, Kirchhoff PD, Wang L, Matvekas A, Takyi-Williams J, Wen B, Sun D, Ator M, Mckean R, Wang S. Han X, et al. Among authors: ator m. J Med Chem. 2023 Jul 13;66(13):8822-8843. doi: 10.1021/acs.jmedchem.3c00405. Epub 2023 Jun 29. J Med Chem. 2023. PMID: 37382562
Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer.
Xiang W, Zhao L, Han X, Xu T, Kregel S, Wang M, Miao B, Qin C, Wang M, McEachern D, Lu J, Bai L, Yang CY, Kirchhoff PD, Takyi-Williams J, Wang L, Wen B, Sun D, Ator M, Mckean R, Chinnaiyan AM, Wang S. Xiang W, et al. Among authors: ator m. J Med Chem. 2023 Sep 28;66(18):13280-13303. doi: 10.1021/acs.jmedchem.3c01264. Epub 2023 Sep 8. J Med Chem. 2023. PMID: 37683104
Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein-Ligand Complexes.
Cansfield AD, Ator MA, Banerjee J, Bestwick M, Bortolato A, Brown GA, Brown J, Butkovic K, Cansfield JE, Christopher JA, Congreve M, Cseke G, Deflorian F, Dugan B, Hunjadi MP, Hutinec A, Inturi TK, Landek G, Mason J, O'Brien A, Ott GR, Rupcic R, Saxty G, Southall SM, Zadravec R, Watson SP. Cansfield AD, et al. Among authors: ator ma. ACS Chem Neurosci. 2022 Mar 16;13(6):751-765. doi: 10.1021/acschemneuro.1c00696. Epub 2022 Mar 4. ACS Chem Neurosci. 2022. PMID: 35245037
Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine.
Bucknell SJ, Ator MA, Brown AJH, Brown J, Cansfield AD, Cansfield JE, Christopher JA, Congreve M, Cseke G, Deflorian F, Jones CR, Mason JS, O'Brien MA, Ott GR, Pickworth M, Southall SM. Bucknell SJ, et al. Among authors: ator ma. J Med Chem. 2020 Jul 23;63(14):7906-7920. doi: 10.1021/acs.jmedchem.0c01003. Epub 2020 Jul 8. J Med Chem. 2020. PMID: 32558564
Combined inhibition of atypical PKC and histone deacetylase 1 is cooperative in basal cell carcinoma treatment.
Mirza AN, Fry MA, Urman NM, Atwood SX, Roffey J, Ott GR, Chen B, Lee A, Brown AS, Aasi SZ, Hollmig T, Ator MA, Dorsey BD, Ruggeri BR, Zificsak CA, Sirota M, Tang JY, Butte A, Epstein E, Sarin KY, Oro AE. Mirza AN, et al. Among authors: ator ma. JCI Insight. 2017 Nov 2;2(21):e97071. doi: 10.1172/jci.insight.97071. JCI Insight. 2017. PMID: 29093271 Free PMC article.
Laquinimod arrests experimental autoimmune encephalomyelitis by activating the aryl hydrocarbon receptor.
Kaye J, Piryatinsky V, Birnberg T, Hingaly T, Raymond E, Kashi R, Amit-Romach E, Caballero IS, Towfic F, Ator MA, Rubinstein E, Laifenfeld D, Orbach A, Shinar D, Marantz Y, Grossman I, Knappertz V, Hayden MR, Laufer R. Kaye J, et al. Among authors: ator ma. Proc Natl Acad Sci U S A. 2016 Oct 11;113(41):E6145-E6152. doi: 10.1073/pnas.1607843113. Epub 2016 Sep 26. Proc Natl Acad Sci U S A. 2016. PMID: 27671624 Free PMC article.
Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
Ott GR, Cheng M, Learn KS, Wagner J, Gingrich DE, Lisko JG, Curry M, Mesaros EF, Ghose AK, Quail MR, Wan W, Lu L, Dobrzanski P, Albom MS, Angeles TS, Wells-Knecht K, Huang Z, Aimone LD, Bruckheimer E, Anderson N, Friedman J, Fernandez SV, Ator MA, Ruggeri BA, Dorsey BD. Ott GR, et al. Among authors: ator ma. J Med Chem. 2016 Aug 25;59(16):7478-96. doi: 10.1021/acs.jmedchem.6b00487. Epub 2016 Aug 15. J Med Chem. 2016. PMID: 27527804
3-(1'-Cyclobutylspiro[4H-1,3-benzodioxine-2,4'-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazin-6-one (CEP-32215), a new wake-promoting histamine H3 antagonist/inverse agonist.
Hudkins RL, Gruner JA, Raddatz R, Mathiasen JR, Aimone LD, Marino MJ, Bacon ER, Williams M, Ator MA. Hudkins RL, et al. Among authors: ator ma. Neuropharmacology. 2016 Jul;106:37-45. doi: 10.1016/j.neuropharm.2015.09.025. Epub 2015 Sep 21. Neuropharmacology. 2016. PMID: 26400408
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