Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Louis V. LaFrance"'
Autor:
Christopher L. Carpenter, Eldridge N. Nartey, Dominic Suarez, Elisabeth A. Minthorn, Jesus R. Medina, Louis V. LaFrance, Ralph A. Rivero, James F. Mack, Charles F. McHugh, Xinrong Tian, Dirk A. Heerding, Christina Ng Di Marco, Thomas J. Berrodin, Aishwarya Bhaskar, Biju Mangatt, William Hoi Hong Li, Brackley James, Martyr Cuthbert, Lorena A. Kallal, Michael Butticello, Jacob Rubin
Publikováno v:
Journal of Medicinal Chemistry. 64:16056-16087
Elevated expression of the c-MYC oncogene is one of the most common abnormalities in human cancers. Unfortunately, efforts to identify pharmacological inhibitors that directly target MYC have not yet yielded a drug-like molecule due to the lack of an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::be3a3a04dfdce0aa0aa268d1655c5476
https://doi.org/10.1021/acs.jmedchem.1c01416
https://doi.org/10.1021/acs.jmedchem.1c01416
Autor:
Christine Thompson, Daryl A. Scherzer, Ryan G. Kruger, Steven D. Knight, Louis V. LaFrance, Heidi M. Ott, Dashyant Dhanak, Stuart Paul Romeril, Celine Duquenne, Dominic Suarez, William H. Miller, Art Shu, Seth W. Grant, Carl A. Machutta, Joelle Lorraine Burgess, Brackley James, Caretha L. Creasy, Xinrong Tian, Yong Jiang, Sharad K. Verma, Peter J. Tummino, Alan P. Graves, Glenn S. Van Aller, Elsie Diaz, Kenneth A. Newlander, Johnson Neil W, Michael T. McCabe
Publikováno v:
ACS Medicinal Chemistry Letters. 3:1091-1096
The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays a critical role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. As part of a drug discovery program targeting EZH2, we have ident
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09381bbf91f7d5cc9197b3635203cdfa
https://doi.org/10.1021/ml3003346
https://doi.org/10.1021/ml3003346
Autor:
Ryan G. Kruger, William H. Miller, Louis V. LaFrance, Celine Duquenne, Alan P. Graves, Heidi M. Ott, Dashyant Dhanak, Christine Thompson, Xinrong Tian, Martin Brandt, Michael T. McCabe, Charles F. McHugh, Mellinger Mark, Susan Korenchuk, Anthony Della Pietra, Peter J. Tummino, Yan Liu, Caretha L. Creasy, Sharad K. Verma, Elsie Diaz, Gopinath Ganji, Glenn S. Van Aller
Publikováno v:
Nature. 492:108-112
EZH2, the catalytic subunit of the polycomb repressive complex 2 (PRC2), is involved in repressing gene expression through methylation of histone H3 on lysine 27 (H3K27). Overexpression of EZH2 is implicated in tumorigenesis, and mutations within its
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::718ed388ff24dbe87c08172ea7b759b7
https://doi.org/10.1038/nature11606
https://doi.org/10.1038/nature11606
Autor:
Kristin K. Brown, Jack D. Leber, Sharad K. Verma, Shu-Yun Zhang, Hong Lin, Brian Donovan, Mei Li, Dirk A. Heerding, Elisabeth A. Minthorn, Louis V. LaFrance, Kimberly A. Robell, Barry S. Brown, Juan I. Luengo, Igor G. Safonov, Wenyong Wang, Dennis S. Yamashita, Michael D. Schaber, Dennis T. Takata, Dana S. Levy, Jason A. Kahana, Joseph W. Venslavsky, Jin Zeng, Rakesh Kumar, Ren Xie, Anthony E. Choudhry, Zhihong Lai
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:684-688
The synthesis and evaluation of tetrasubstituted aminopyridines, bearing novel azaindazole hinge binders, as potent AKT inhibitors are described. Compound 14c was identified as a potent AKT inhibitor that demonstrated reduced CYP450 inhibition and an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c35f1d03a41bbaae3c90655ee77ea89d
https://doi.org/10.1016/j.bmcl.2009.11.061
https://doi.org/10.1016/j.bmcl.2009.11.061
Autor:
Pierre Raboisson, Raul R. Calvo, Rose Tominovich, Louis V. LaFrance, Karen L. Milkiewicz, Dana L. Johnson, Anna C. Maroney, Shuyuan Zhao, Robert R. Donatelli, Maxwell D. Cummings, Bruce L. Grasberger, Christopher J. Molloy, Tianbao Lu, Juan J. Marugan, Daniel J. Parks, Kristi A. Leonard, Carol F. Franks, Joan Gushue, Holly K. Koblish
Publikováno v:
Molecular Cancer Therapeutics. 5:160-169
The activity and stability of the p53 tumor suppressor are regulated by the human homologue of the mouse double minute 2 (Hdm2) oncoprotein. It has been hypothesized that small molecules disrupting the Hdm2:p53 complex would allow for the activation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30835600d455b26ccf94cf87ed7132f4
https://doi.org/10.1158/1535-7163.mct-05-0199
https://doi.org/10.1158/1535-7163.mct-05-0199
Autor:
Jennifer Lattanze, Tianbao Lu, Karen L. Milkiewicz, Bruce L. Grasberger, Theodore E. Carver, Louis V. LaFrance, Daniel J. Parks, Kannan Ramachandren, Varsha Gupta, Raul R. Calvo, Diane M. Maguire, Eugene C. Petrella, Maxwell D. Cummings
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:765-770
A library of 1,4-benzodiazepine-2,5-diones was screened for binding to the p53-binding domain of HDM2 using Thermofluor ® , a miniaturized thermal denaturation assay. The hits obtained were shown to bind to HDM2 in the p53-binding pocket using a flu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eed49474f88d1fb7a63d4bf5e23b6ee3
https://doi.org/10.1016/j.bmcl.2004.11.009
https://doi.org/10.1016/j.bmcl.2004.11.009
Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells
Autor:
Tianbao Lu, Jennifer Lattanze, Ingrid Deckman, Marie Zhang, Bruce L. Grasberger, Carl L. Manthey, and Christopher J. Molloy, John C. Spurlino, Diane M. Maguire, Eugene C. Petrella, Kannan Ramachandren, Holly K. Koblish, Shuyuan Zhao, Bruce E. Tomczuk, Gwendolyn R. Bylebyl, Louis V. LaFrance, Carsten Schubert, Daniel J. Parks, Karen L. Milkiewicz, Carol F. Franks, Theodore E. Carver, Roger F. Bone, Anna C. Maroney, Maxwell D. Cummings, Raul R. Calvo, W. Michael Avondale Pantoliano
Publikováno v:
Journal of Medicinal Chemistry. 48:909-912
HDM2 binds to an alpha-helical transactivation domain of p53, inhibiting its tumor suppressive functions. A miniaturized thermal denaturation assay was used to screen chemical libraries, resulting in the discovery of a novel series of benzodiazepined
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ad2c720d92aeda8d7b96e67eadcedf4
https://doi.org/10.1021/jm049137g
https://doi.org/10.1021/jm049137g
Autor:
Louis V. LaFrance, Sharad K. Verma
Publikováno v:
Tetrahedron Letters. 50:383-385
Methods for a facile high-yielding synthesis of substituted pyrazolo[3,4-c]pyridines from 2-bromo-5-fluoropyridine are described, along with a brief mechanistic discussion for the key cyclization step. The methods utilize inexpensive commercially ava
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::57d83a3a0969618a458247cfd7831e2d
https://doi.org/10.1016/j.tetlet.2008.11.013
https://doi.org/10.1016/j.tetlet.2008.11.013
Autor:
Stephanie Chen, Mehul Patel, Louis V. LaFrance, Glenn S. Van Aller, BaoChau Le, Sharon Sweitzer, Yong Jiang, Andrew J. Pope, Danielle Key, Zining Wu, Christopher J. Nixon, Ryan G. Kruger, Melissa B. Pappalardi, Caretha L. Creasy, Carl A. Machutta, Michael T. McCabe, Sara H. Thrall, Benjamin Schwartz, Martin Brandt, Elsie Diaz, Sharad K. Verma, Glenn A. Hofmann, Peter J. Tummino
Publikováno v:
Journal of biomolecular screening. 17(10)
Histone methyltransferases (HMT) catalyze the methylation of histone tail lysines, resulting in changes in gene transcription. Misregulation of these enzymes has been associated with various forms of cancer, making this target class a potential new a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9cf081021cb76a8796692374384fa80
https://pubmed.ncbi.nlm.nih.gov/22904200
https://pubmed.ncbi.nlm.nih.gov/22904200
Autor:
Sharad K. Verma, Louis V. LaFrance
Publikováno v:
ChemInform. 40
Methods for a facile high-yielding synthesis of substituted pyrazolo[3,4-c]pyridines from 2-bromo-5-fluoropyridine are described, along with a brief mechanistic discussion for the key cyclization step. The methods utilize inexpensive commercially ava
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::95c837f4aea5f4bba9348b87dfbd4ca5
https://doi.org/10.1002/chin.200918149
https://doi.org/10.1002/chin.200918149