Search Results - "Girijavallabhan, V"

SCH 503034, a Mechanism-Based Inhibitor of Hepatitis C Virus NS3 Protease, Suppresses Polyprotein Maturation and Enhances the Antiviral Activity of Alpha Interferon in Replicon Cells by MALCOLM, B. A, LIU, R, INGRAVALLO, P, JIANG, C, KONG, R, LU, J, PICHARDO, J, PRONGAY, A, SKELTON, A, TONG, X, VENKATRAMAN, S, XIA, E, LAHSER, F, GIRIJAVALLABHAN, V, NJOROGE, F. G, AGRAWAL, S, BELANGER, B, BUTKIEWICZ, N, CHASE, R, GHEYAS, F, HART, A, HESK, D

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Characterization of resistance mutations against HCV ketoamide protease inhibitors by Tong, Xiao, Bogen, Stephane, Chase, Robert, Girijavallabhan, V., Guo, Zhuyan, Njoroge, F. George, Prongay, Andrew, Saksena, Anil, Skelton, Angela, Xia, Ellen, Ralston, Robert

“…An issue of clinical importance in the development of new antivirals for HCV is emergence of resistance. Several resistance loci to ketoamide inhibitors of the…”
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Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and Wap-ras transgenic mice by MING LIU, BRYANT, M. S, DELL, J, SINHA, D, SYED, J, KORFMACHER, W. A, NOMEIR, A. A, LIN, C.-C, WANG, L, TAVERAS, A. G, DOLL, R. J, NJOROGE, F. G, JIANPING CHEN, MALLAMS, A. K, REMISZEWSKI, S, CATINO, J. J, GIRIJAVALLABHAN, V. M, KIRSCHMEIER, P, BISHOP, W. R, SUINING LEE, YAREMKO, B, LIPARI, P, MALKOWSKI, M, FERRARI, E, NIELSEN, L, PRIOLI, N

“…We have been developing a series of nonpeptidic, small molecule farnesyl protein transferase inhibitors that share a common tricyclic nucleus and compete with…”
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Hepatitis C virus NS3-4A serine protease inhibitors: SAR of new P1 derivatives of SCH 503034 by Bogen, S., Arasappan, A., Pan, W., Ruan, S., Padilla, A., Saksena, A.K., Girijavallabhan, V., Njoroge, F.G.

“…Substitutions on the P 1 cyclobutyl side chain of SCH 503034 were studied by introduction of hydroxyl and fluoro substituents. Additionally, effects of fluoro…”
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Farnesyl protein transferase inhibition: a novel approach to anti-tumor therapy. the discovery and development of SCH 66336 by Ganguly, A K, Doll, R J, Girijavallabhan, V M

“…Farnesyl protein transferase (FPT) inhibition is an interesting and promising approach to non-cytotoxic anticancer therapy. Research in this area has resulted…”
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Tricyclic Farnesyl Protein Transferase Inhibitors:  Crystallographic and Calorimetric Studies of Structure−Activity Relationships by Strickland, Corey L, Weber, Patricia C, Windsor, William T, Wu, Zhen, Le, Hung V, Albanese, Margaret M, Alvarez, Carmen S, Cesarz, David, del Rosario, Joycelyn, Deskus, Jeffrey, Mallams, Alan K, Njoroge, F. George, Piwinski, John J, Remiszewski, Stacy, Rossman, Randall R, Taveras, Arthur G, Vibulbhan, Bancha, Doll, Ronald J, Girijavallabhan, Viyyoor M, Ganguly, Ashit K

“…Crystallographic and thermodynamic studies of farnesyl protein transferase (FPT) complexed with novel tricyclic inhibitors provide insights into the observed…”
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Structure of poliovirus type 2 Lansing complexed with antiviral agent SCH48973: comparison of the structural and biological properties of the three poliovirus serotypes by Lentz, Karen N, Smith, Allen D, Geisler, Sheila C, Cox, Stuart, Buontempo, Peter, Skelton, Angela, DeMartino, Jason, Rozhon, Edward, Schwartz, Jerome, Girijavallabhan, V, O’Connell, John, Arnold, Edward

“…Background: Polioviruses are human pathogens and the causative agents of poliomyelitis. Polioviruses are icosahedral single-standed RNA viruses, which belong…”
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Farnesyl protein transferase inhibitors targeting the catalytic zinc for enhanced binding by Njoroge, F. George, Vibulbhan, Bancha, Pinto, Patrick, Strickland, Corey, Kirschmeier, Paul, Bishop, W. Robert, Girijavallabhan, V.

“…Design and synthesis of farnesyl protein transferase inhibitors, targeting catalytic zinc are reported. Successful efforts to make farnesyl transferase (FT)…”
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SCH 48973: a potent, broad-spectrum, antienterovirus compound by BUONTEMPO, P. J, COX, S, O'CONNELL, J. F, WRIGHT-MINOGUE, J, DEMARTINO, J. L, SKELTON, A. M, FERRARI, E, ALBIN, R, ROZHON, E. J, GIRIJAVALLABHAN, V, MODLIN, J. F

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Ras oncoprotein inhibitors: The discovery of potent, ras nucleotide exchange inhibitors and the structural determination of a drug-protein complex by Taveras, A.G., Remiszewski, S.W., Doll, R.J., Cesarz, D., Huang, E.C., Kirschmeier, P., Pramanik, B.N., Snow, M.E., Wang, Y.-S., del Rosario, J.D., Vibulbhan, B., Bauer, B.B., Brown, J.E., Carr, D., Catino, J., Evans, C.A., Girijavallabhan, V., Heimark, L., James, L., Liberles, S., Nash, C., Perkins, L., Senior, M.M., Tsarbopoulos, A., Ganguly, A.K., Aust, R., Brown, E., Delisle, D., Fuhrman, S., Hendrickson, T., Kissinger, C., Love, R., Sisson, W., Villafranca, E., Webber, S.E.

“…The nucleotide exchange process is one of the key activation steps regulating the ras protein. This report describes the development of potent, non-nucleotide,…”
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Hepatitis C virus NS3-4A serine protease inhibitors : Use of a P2-P1 cyclopropyl alanine combination for improved potency by BOGEN, S, SAKSENA, A. K, ARASAPPAN, A, GU, H, NJOROGE, F. G, GIRIJAVALLABHAN, V, PICHARDO, J, BUTKIEWICZ, N, PRONGAY, A, MADISON, V

“…Modification of the P(2) and P(1) side chains of earlier P(3)-capped alpha-ketoamide inhibitor of HCV NS3 serine protease 1 resulted in the discovery of…”
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Binding affinities and geometries of various metal ligands in peptide deformylase inhibitors by Madison, V, Duca, J, Bennett, F, Bohanon, S, Cooper, A, Chu, M, Desai, J, Girijavallabhan, V, Hare, R, Hruza, A, Hendrata, S, Huang, Y, Kravec, C, Malcolm, B, McCormick, J, Miesel, L, Ramanathan, L, Reichert, P, Saksena, A, Wang, J, Weber, P.C, Zhu, H, Fischmann, T

“…Removal of the N-terminal formyl group from newly synthesized proteins by the enzyme peptide deformylase (PDF) is essential for normal growth of bacteria but…”
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Trihalobenzocycloheptapyridine analogues of Sch 66336 as potent inhibitors of farnesyl protein transferase by Njoroge, F.George, Vibulbhan, Bancha, Pinto, Patrick, Strickland, Corey L, Bishop, W.Robert, Kirschmeir, Paul, Girijavallabhan, V, Ganguly, Ashit K

“…SCH 66336 is a trihalo tricyclic compound that is currently undergoing Phase II clinical trials for the treatment of solid tumors. Modifications of SCH 66336…”
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Structure−Activity Relationship of 3-Substituted N-(Pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)- piperidine Inhibitors of Farnesyl-Protein Transferase:  Design and Synthesis of in Vivo Active Antitumor Compounds by Njoroge, F. George, Vibulbhan, Bancha, Rane, Dinananth F, Bishop, W. Robert, Petrin, Joanne, Patton, Robert, Bryant, Mathew S, Chen, K.-J, Nomeir, Amin A, Lin, C.-C, Liu, Ming, King, Ivan, Chen, Jianping, Lee, Suining, Yaremko, Bohdan, Dell, Janet, Lipari, Philip, Malkowski, Michael, Li, Zujun, Catino, Joseph, Doll, Ronald J, Girijavallabhan, V, Ganguly, Ashit K

“…Novel tricyclic Ras farnesyl-protein transferase (FPT) inhibitors are described. A comprehensive structure−activity relationship (SAR) study of compounds…”
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Enzymatic Kinetic Resolution of Piperidine Atropisomers:  Synthesis of a Key Intermediate of the Farnesyl Protein Transferase Inhibitor, SCH66336 by Morgan, Brian, Zaks, Aleksey, Dodds, David R, Liu, Jinchu, Jain, Rama, Megati, Sreeni, Njoroge, F. George, Girijavallabhan, Viyyoor M

“…The resolution of secondary amines via enzyme-catalyzed acylation is a relatively rare process. The kinetic resolution of a series of intermediates of SCH66336…”
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Identification of Pharmacokinetically Stable 3,10-Dibromo-8-chlorobenzocycloheptapyridine Farnesyl Protein Transferase Inhibitors with Potent Enzyme and Cellular Activities by Taveras, Arthur G, Deskus, Jeff, Chao, Jianping, Vaccaro, Cynthia J, Njoroge, F. George, Vibulbhan, Bancha, Pinto, Pat, Remiszewski, Stacy, del Rosario, Jocelyn, Doll, Ronald J, Alvarez, Carmen, Lalwani, Tarik, Mallams, Alan K, Rossman, Randall R, Afonso, Adriano, Girijavallabhan, Viyyoor M, Ganguly, Ashit K, Pramanik, Birendra, Heimark, Larry, Bishop, W. Robert, Wang, Lynn, Kirschmeier, Paul, James, Linda, Carr, Donna, Patton, Robert, Bryant, Mathew S, Nomeir, Amin A, Liu, Ming

“…Farnesyl protein transferase (FPT) is a promising target for the development of cancer chemotherapeutics because it is responsible for the farnesylation of…”
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Potent, Selective, and Orally Bioavailable Tricyclic Pyridyl Acetamide N-Oxide Inhibitors of Farnesyl Protein Transferase with Enhanced in Vivo Antitumor Activity by Njoroge, F. George, Vibulbhan, Bancha, Pinto, Patrick, Bishop, W. Robert, Bryant, Mathew S, Nomeir, Amin A, Lin, C.-C, Liu, Ming, Doll, Ronald J, Girijavallabhan, V, Ganguly, Ashit K

“…We previously reported compound 1 as a potent farnesyl protein transferase (FPT) inhibitor that exhibited reasonable pharmacokinetic stability and showed…”
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Synthesis of 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase by Cooper, Alan B, Strickland, Corey L, Wang, James, Desai, Jagdish, Kirschmeier, Paul, Patton, Robert, Bishop, W Robert, Weber, Patricia C, Girijavallabhan, V

“…A series of novel N-cyanoguanidine tricyclic farnesyl protein transferase (FPT) inhibitors was prepared. Replacement of a piperidine amide-group with a…”
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Effects of SCH 59228, an orally bioavailable farnesyl protein transferase inhibitor, on the growth of oncogene-transformed fibroblasts and a human colon carcinoma xenograft in nude mice by MING LIU, BRYANT, M. S, ROSSMAN, R. R, KORFMACHER, W. A, NOMEIR, A. A, LIN, C.-C, MALLAMS, A. K, DOLL, R. J, CATINO, J. J, GIRIJAVALLABHAN, V. M, KIRSCHMEIER, P, BISHOP, W. R, JIANPING CHEN, SUININHG LEE, YAREMKO, B, ZUJUN LI, DELL, J, LIPARI, P, MALKOWSKI, M, PRIOLI, N

“…The products of the Ha-, Ki-, and N-ras proto-oncogenes comprise a family of 21 kDa guanine nucleotide-binding proteins which play a crucial role in growth…”
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Discovery of novel nonpeptide tricyclic inhibitors of ras farnesyl protein transferase by Njoroge, F. George, Doll, Ronald J., Vibulbhan, Bancha, Alvarez, Carmen S., Bishop, W. Robert, Petrin, Joanne, Kirschmeier, Paul, Carruthers, Nicholas I., Wong, Jesse K., Albanese, Margaret M., Piwinski, John J., Catino, Joseph, Girijavallabhan, V., Ganguly, Ashit K.

“…A comprehensive structure-activity relationship (SAR) study of novel tricyclic amides has been undertaken. The discovery of compounds that are potent FPT…”
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