Search Results - "LaFrance, Louis V"

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2 by Verma, Sharad K, Tian, Xinrong, LaFrance, Louis V, Duquenne, Céline, Suarez, Dominic P, Newlander, Kenneth A, Romeril, Stuart P, Burgess, Joelle L, Grant, Seth W, Brackley, James A, Graves, Alan P, Scherzer, Daryl A, Shu, Art, Thompson, Christine, Ott, Heidi M, Aller, Glenn S. Van, Machutta, Carl A, Diaz, Elsie, Jiang, Yong, Johnson, Neil W, Knight, Steven D, Kruger, Ryan G, McCabe, Michael T, Dhanak, Dashyant, Tummino, Peter J, Creasy, Caretha L, Miller, William H

“…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…”
Get full text

Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase by Heerding, Dirk A, Rhodes, Nelson, Leber, Jack D, Clark, Tammy J, Keenan, Richard M, Lafrance, Louis V, Li, Mei, Safonov, Igor G, Takata, Dennis T, Venslavsky, Joseph W, Yamashita, Dennis S, Choudhry, Anthony E, Copeland, Robert A, Lai, Zhihong, Schaber, Michael D, Tummino, Peter J, Strum, Susan L, Wood, Edgar R, Duckett, Derek R, Eberwein, Derek, Knick, Victoria B, Lansing, Timothy J, McConnell, Randy T, Zhang, ShuYun, Minthorn, Elisabeth A, Concha, Nestor O, Warren, Gregory L, Kumar, Rakesh

“…Overexpression of AKT has an antiapoptotic effect in many cell types, and expression of dominant negative AKT blocks the ability of a variety of growth factors…”
Get full text

Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo by Koblish, Holly K, Zhao, Shuyuan, Franks, Carol F, Donatelli, Robert R, Tominovich, Rose M, LaFrance, Louis V, Leonard, Kristi A, Gushue, Joan M, Parks, Daniel J, Calvo, Raul R, Milkiewicz, Karen L, Marugán, Juan José, Raboisson, Pierre, Cummings, Maxwell D, Grasberger, Bruce L, Johnson, Dana L, Lu, Tianbao, Molloy, Christopher J, Maroney, Anna C

“…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…”
Get full text

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations by McCabe, Michael T., Ott, Heidi M., Ganji, Gopinath, Korenchuk, Susan, Thompson, Christine, Van Aller, Glenn S., Liu, Yan, Graves, Alan P., III, Anthony Della Pietra, Diaz, Elsie, LaFrance, Louis V., Mellinger, Mark, Duquenne, Celine, Tian, Xinrong, Kruger, Ryan G., McHugh, Charles F., Brandt, Martin, Miller, William H., Dhanak, Dashyant, Verma, Sharad K., Tummino, Peter J., Creasy, Caretha L.

“…EZH2 is a methyltransferase that is mutated in lymphoma; here a potent small molecule inhibitor of EZH2 is described, which inhibits the proliferation of EZH2…”
Get full text

Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells by Grasberger, Bruce L, Lu, Tianbao, Schubert, Carsten, Parks, Daniel J, Carver, Theodore E, Koblish, Holly K, Cummings, Maxwell D, LaFrance, Louis V, Milkiewicz, Karen L, Calvo, Raul R, Maguire, Diane, Lattanze, Jennifer, Franks, Carol F, Zhao, Shuyuan, Ramachandren, Kannan, Bylebyl, Gwendolyn R, Zhang, Marie, Manthey, Carl L, Petrella, Eugene C, Pantoliano, Michael W, Deckman, Ingrid C, Spurlino, John C, Maroney, Anna C, Tomczuk, Bruce E, Molloy, Christopher J, Bone, Roger F

“…HDM2 binds to an α-helical transactivation domain of p53, inhibiting its tumor suppressive functions. A miniaturized thermal denaturation assay was used to…”
Get full text

1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2–p53 interaction: discovery and SAR by Parks, Daniel J., LaFrance, Louis V., Calvo, Raul R., Milkiewicz, Karen L., Gupta, Varsha, Lattanze, Jennifer, Ramachandren, Kannan, Carver, Theodore E., Petrella, Eugene C., Cummings, Maxwell D., Maguire, Diane, Grasberger, Bruce L., Lu, Tianbao

“…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…”
Get full text

A facile method for the synthesis of substituted pyrazolo[3,4- c]pyridines by Verma, Sharad K., LaFrance, Louis V.

“…Methods are described for a facile high-yielding synthesis of substituted pyrazolo[3,4- c]pyridines from inexpensive commercially available starting materials…”
Get full text

Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein–protein interaction through structure-based drug design by Parks, Daniel J., LaFrance, Louis V., Calvo, Raul R., Milkiewicz, Karen L., José Marugán, Juan, Raboisson, Pierre, Schubert, Carsten, Koblish, Holly K., Zhao, Shuyuan, Franks, Carol F., Lattanze, Jennifer, Carver, Theodore E., Cummings, Maxwell D., Maguire, Diane, Grasberger, Bruce L., Maroney, Anna C., Lu, Tianbao

“…Guided by structure-based drug design, modification of the BDP lead compound 1 resulted in the discovery of 19, a potent and orally bioavailable antagonist of…”
Get full text

Substituted 1,4-Benzodiazepine-2,5-diones as α-Helix Mimetic Antagonists of the HDM2-p53 Protein-Protein Interaction by Cummings, Maxwell D., Schubert, Carsten, Parks, Daniel J., Calvo, Raul R., LaFrance, Louis V., Lattanze, Jennifer, Milkiewicz, Karen L., Lu, Tianbao

“…Small molecule antagonists of protein–protein interactions represent a particular challenge for pharmaceutical discovery. One approach to finding molecules…”
Get full text

Abstract 3260: Identification and synthesis of benzimidazole carboxamides as potent inhibitors of focal adhesion kinase (FAK) by Verma, Sharad K., Leber, Jack D., LaFrance, Louis V., Li, Mei, Duquenne, Celine, Cui, Guanglei, Miller, William H.

“…Abstract Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that integrates signals from integrins and growth factor receptors. FAK has been…”
Get full text

Abstract 4700: A novel selective EZH2 inhibitor exhibits anti-tumor activity in lymphoma with EZH2 activating mutations by Creasy, Caretha L., McCabe, Michael T., Korenchuk, Susan, Diaz, Elsie, Ott, Heidi, Thompson, Christine S., Ganji, Gopi, Gorman, Shelby A., LaFrance, Louis V., Brandt, Martin, McHugh, Charles, Verma, Sharad K., Tummino, Peter J.

“…Abstract EZH2 is the catalytic subunit of the Polycomb Repressive Complex 2 (PRC2) responsible for methylating histone H3 on lysine 27 (H3K27) and repressing…”
Get full text

Abstract 2939: Discovery and synthesis of highly potent and selective small molecule inhibitors of the histone methyltransferase EZH2 by Verma, Sharad K., LaFrance, Louis V., Tian, Xinrong, Newlander, Ken, Duquenne, Céline, Suarez, Dominic, Knight, Steven D., Burgess, Joelle, Brackley, James, Johnson, Neil W., Graves, Alan P., Mellinger, Mark, Romeril, Stuart, Grant, Seth W., Scherzer, Daryl, Shu, Art, Creasy, Caretha L., Kruger, Ryan, Diaz, Elsie, Le, Baochau, Thompson, Christine, Morgan-Ott, Heidi, McCabe, Michael T., McHugh, Charles F., Miller, William H., Tummino, Peter, Dhanak, Dash

“…Abstract The histone methyltransferases are a group of enzymes which catalyze the transfer of a methyl group from the co-factor S-Adenosylmethionine (SAM) to…”
Get full text

Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3 S )-3-piperidinylmethyl]oxy}-1 H -imidazo[4,5- c ]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase by Heerding, Dirk A., Rhodes, Nelson, Leber, Jack D., Clark, Tammy J., Keenan, Richard M., Lafrance, Louis V., Li, Mei, Safonov, Igor G., Takata, Dennis T., Venslavsky, Joseph W., Yamashita, Dennis S., Choudhry, Anthony E., Copeland, Robert A., Lai, Zhihong, Schaber, Michael D., Tummino, Peter J., Strum, Susan L., Wood, Edgar R., Duckett, Derek R., Eberwein, Derek, Knick, Victoria B., Lansing, Timothy J., McConnell, Randy T., Zhang, ShuYun, Minthorn, Elisabeth A., Concha, Nestor O., Warren, Gregory L., Kumar, Rakesh

Get full text

Identification of 4-2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-([(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase by HEERDING, Dirk A, RHODES, Nelson, YAMASHITA, Dennis S, CHOUDHRY, Anthony E, COPELAND, Robert A, ZHIHONG LAI, SCHABER, Michael D, TUMMINO, Peter J, STRUM, Susan L, WOOD, Edgar R, DUCKETT, Derek R, EBERWEIN, Derek, LEBER, Jack D, KNICK, Victoria B, LANSING, Timothy J, MCCONNELL, Randy T, SHUYUN ZHANG, MINTHORN, Elisabeth A, CONCHA, Nestor O, WARREN, Gregory L, KUMAR, Rakesh, CLARK, Tammy J, KEENAN, Richard M, LAFRANCE, Louis V, MEI LI, SAFONOV, Igor G, TAKATA, Dennis T, VENSLAVSKY, Joseph W

Get full text

Research Article: Substituted 1,4-Benzodiazepine-2,5-diones as alpha -Helix Mimetic Antagonists of the HDM2-p53 Protein-Protein Interaction by Cummings, Maxwell D, Schubert, Carsten, Parks, Daniel J, Calvo, Raul R, LaFrance, Louis V, Lattanze, Jennifer, Milkiewicz, Karen L, Lu, Tianbao

“…Small molecule antagonists of protein-protein interactions represent a particular challenge for pharmaceutical discovery. One approach to finding molecules…”
Get full text