Zobrazeno 1 - 10
of 79
pro vyhledávání: '"Thelma S, Angeles"'
Autor:
Bruce A. Ruggeri, Giorgio Inghirami, Bruce D. Dorsey, Mark A. Ator, Cristina Abele, Rodolfo Machiorlatti, Flavio Cristofani, Lisa D. Aimone, Thelma S. Angeles, Mark S. Albom, Weihua Wan, Lihui Lu, Gregory R. Ott, Diane E. Gingrich, Matthew R. Quail, Mangeng Cheng
PDF file - 102K
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b6a0a50e0c286d90b24603959f90aa4c
https://doi.org/10.1158/1535-7163.22498291
https://doi.org/10.1158/1535-7163.22498291
Autor:
Bruce A. Ruggeri, Giorgio Inghirami, Bruce D. Dorsey, Mark A. Ator, Cristina Abele, Rodolfo Machiorlatti, Flavio Cristofani, Lisa D. Aimone, Thelma S. Angeles, Mark S. Albom, Weihua Wan, Lihui Lu, Gregory R. Ott, Diane E. Gingrich, Matthew R. Quail, Mangeng Cheng
PDF file - 300K
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::36ff3acce277a3f9ee6d65f11bbc8c38
https://doi.org/10.1158/1535-7163.22498288
https://doi.org/10.1158/1535-7163.22498288
Autor:
Thao Ung, Ronald Robinson, Chrysanthe Spais, Justin Schreiber, Hussein Hallak, Jean Husten, Thelma S. Angeles, Jacquelyn Lyons, Yun Liu
Publikováno v:
Bioanalysis. 13:575-585
Aim: To quantify the free form of a protein as a target-engagement biomarker in nonhuman primate serum, a Meso Scale Discovery ligand-binding assay was developed and qualified. Results: The initial assay produced an unexpected artifact when used to m
Autor:
R. Curtis Haltiwanger, Mark A. Olsen, Mark A. Ator, Emily Kordwitz, Gregory R. Ott, Jason C. Wagner, Bruce D. Dorsey, Zeqi Huang, Mangeng Cheng, Bruce Ruggeri, Eugen F. Mesaros, Weihua Wan, Lihui Lu, Amy J. Landis, Lisa D. Aimone, Mark S. Albom, Thelma S. Angeles
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1047-1052
The diastereoselective synthesis and biological activity of piperidine-3,4-diol and piperidine-3-ol-derived pyrrolotriazine inhibitors of anaplastic lymphoma kinase (ALK) are described. Although piperidine-3,4-diol and piperidine-3-ol derivatives sho
Autor:
Thelma S. Angeles, Robert L. Hudkins
Publikováno v:
Expert opinion on drug discovery. 11(12)
Elevated lipogenesis has been associated with a variety of diseases including obesity, cancer and nonalcoholic fatty liver disease (NAFLD). Fatty acid synthase (FASN) plays a pivotal role in de novo lipogenesis, making this multi-catalytic protein an
Autor:
Sheryl L. Meyer, Jean Husten, Thelma S. Angeles, Chrysanthe Spais, Mark A. Ator, Seetha Murthy, Jennifer L. Mason, Mark S. Albom, Lisa Saville
Publikováno v:
ASSAY and Drug Development Technologies. 10:551-557
Homogeneous cellular assays can streamline product detection in the drug discovery process. One commercially available assay employing time-resolved fluorescence resonance energy transfer (TR-FRET) that detects phosphorylated products was used to eva
Autor:
Nathan Anderson, Diane E. Gingrich, Arup K. Ghose, Mark S. Albom, Bruce D. Dorsey, Lisa D. Aimone, Elizabeth Bruckheimer, Jason C. Wagner, Matthew A. Curry, Lihui Lu, Jay Friedman, Mark A. Ator, Bruce Ruggeri, Eugen F. Mesaros, Mangeng Cheng, Zeqi Huang, Keith S. Learn, Matthew R. Quail, Thelma S. Angeles, Pawel Dobrzanski, Gregory R. Ott, Sandra V. Fernandez, Joseph G. Lisko, Kevin J. Wells-Knecht, Weihua Wan
Publikováno v:
Journal of medicinal chemistry. 59(16)
Analogues structurally related to anaplastic lymphoma kinase (ALK) inhibitor 1 were optimized for metabolic stability. The results from this endeavor not only led to improved metabolic stability, pharmacokinetic parameters, and in vitro activity agai
Autor:
Thomas J. Connors, Jie Qian, Zeck Huang, Joanne R. Mathiasen, Edward R. Bacon, Thelma S. Angeles, Mark J. Huffman, Emir Duzic, Joseph M. Salvino, Beth Ann McKenna, Hervé Schaffhauser, Robert J. McHugh, Lily D. Lu, George C. Morton, Beverly P. Holskin, Karla Kopec, Amy DiCamillo, Gerard C. Rosse, Chrysanthe Spais, Rabindranath Tripathy, Lisa D. Aimone
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1421-1426
Serotoninergic neurotransmission has been implicated in modulation of learning and memory. It has been demonstrated that 5-hydroxytryptamine(6) (5-HT(6)) receptor antagonists show beneficial effect on cognition in several animal models. Based on a ph
Autor:
Beverly P. Holskin, Karla Kopec, Joanne R. Mathiasen, Amy DiCamillo, Babu G. Sundar, Thomas J. Connors, Emir Duzic, Edward R. Bacon, Gerard C. Rosse, Chrysanthe Spais, Thomas R. Bailey, Beth Ann McKenna, Rebecca A. Brown, Jie Qian, Derek Dunn, Mark J. Huffman, Joseph M. Salvino, Huang Zeqi, Lisa D. Aimone, Hervé Schaffhauser, Deborah Galinis, Thelma S. Angeles, Lily D. Lu, George C. Morton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:120-123
7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel scaffold for 5HT(6) receptor antagonists. Optimization by substitution at C-1 position led to identification of selective, orally bioavailable, brain penetrant antagonists with
Autor:
Gregory J. Wells, Weihua Wan, Henry J. Breslin, Kevin J. Wells-Knecht, Bruce D. Dorsey, Mark A. Ator, Rabindranath Tripathy, Lisa D. Aimone, Mangeng Cheng, Ashley T. Wohler, Zeqi Huang, Tho V. Thieu, Thelma S. Angeles, Matthew R. Quail, Eugen F. Mesaros, Craig A. Zificsak, James Diebold, Jason C. Wagner, Gregory R. Ott, Lihui Lu, Robert J. McHugh, Mark S. Albom
Publikováno v:
Journal of Medicinal Chemistry. 55:115-125
Chemical strategies to mitigate cytochrome P450-mediated bioactivation of novel 2,7-disubstituted pyrrolo[2,1-f][1,2,4]triazine ALK inhibitors are described along with synthesis and biological activity. Piperidine-derived analogues showing minimal mi