Search Results - "BHATTACHARYA, Samit K"

Discovery and Preclinical Characterization of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy by Cameron, Kimberly O, Kung, Daniel W, Kalgutkar, Amit S, Kurumbail, Ravi G, Miller, Russell, Salatto, Christopher T, Ward, Jessica, Withka, Jane M, Bhattacharya, Samit K, Boehm, Markus, Borzilleri, Kris A, Brown, Janice A, Calabrese, Matthew, Caspers, Nicole L, Cokorinos, Emily, Conn, Edward L, Dowling, Matthew S, Edmonds, David J, Eng, Heather, Fernando, Dilinie P, Frisbie, Richard, Hepworth, David, Landro, James, Mao, Yuxia, Rajamohan, Francis, Reyes, Allan R, Rose, Colin R, Ryder, Tim, Shavnya, Andre, Smith, Aaron C, Tu, Meihua, Wolford, Angela C, Xiao, Jun

“…Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human…”
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Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis by Roth Flach, Rachel J., Skoura, Athanasia, Matevossian, Anouch, Danai, Laura V., Zheng, Wei, Cortes, Christian, Bhattacharya, Samit K., Aouadi, Myriam, Hagan, Nana, Yawe, Joseph C., Vangala, Pranitha, Menendez, Lorena Garcia, Cooper, Marcus P., Fitzgibbons, Timothy P., Buckbinder, Leonard, Czech, Michael P.

“…Signalling pathways that control endothelial cell (EC) permeability, leukocyte adhesion and inflammation are pivotal for atherosclerosis initiation and…”
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Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels by Roth Flach, Rachel J., Bollinger, Eliza, Reyes, Allan R., Laforest, Brigitte, Kormos, Bethany L., Liu, Shenping, Reese, Matthew R., Martinez Alsina, Luis A., Buzon, Leanne, Zhang, Yuan, Bechle, Bruce, Rosado, Amy, Sahasrabudhe, Parag V., Knafels, John, Bhattacharya, Samit K., Omoto, Kiyoyuki, Stansfield, John C., Hurley, Liam D., Song, LouJin, Luo, Lina, Breitkopf, Susanne B., Monetti, Mara, Cunio, Teresa, Tierney, Brendan, Geoly, Frank J., Delmore, Jake, Siddall, C. Parker, Xue, Liang, Yip, Ka N., Kalgutkar, Amit S., Miller, Russell A., Zhang, Bei B., Filipski, Kevin J.

“…Branched chain amino acid (BCAA) catabolic impairments have been implicated in several diseases. Branched chain ketoacid dehydrogenase (BCKDH) controls the…”
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Lead-like Drugs: A Perspective by Raymer, Brian, Bhattacharya, Samit K

“…Lead-like drugs, or drugs below molecular weight 300, are an important and sometimes overlooked component of the current pharmacopeia and contemporary…”
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PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy by Jani, Jitesh P, Arcari, Joel, Bernardo, Vincent, Bhattacharya, Samit K, Briere, David, Cohen, Bruce D, Coleman, Kevin, Christensen, James G, Emerson, Erling O, Jakowski, Amy, Hook, Kenneth, Los, Gerrit, Moyer, James D, Pruimboom-Brees, Ingrid, Pustilnik, Leslie, Rossi, Ann Marie, Steyn, Stefan J, Su, Chunyan, Tsaparikos, Konstantinos, Wishka, Donn, Yoon, Kwansik, Jakubczak, John L

“…The Aurora family of highly related serine/threonine kinases plays a key role in the regulation of mitosis. Aurora1 and Aurora2 play important but distinct…”
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Lead-like Drugs: A Perspective: Miniperspective by Raymer, Brian, Bhattacharya, Samit K

“…Lead-like drugs, or drugs below molecular weight 300, are an important and sometimes overlooked component of the current pharmacopeia and contemporary…”
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Small Molecule Ghrelin Receptor Inverse Agonists and Antagonists by Cameron, Kimberly O, Bhattacharya, Samit K, Loomis, A. Katrina

“…Ghrelin is an endogenous peptide hormone secreted primarily by the stomach and is involved in a number of physiological processes including growth hormone…”
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Structural studies identify angiotensin II receptor blocker-like compounds as branched-chain ketoacid dehydrogenase kinase inhibitors by Liu, Shenping, Kormos, Bethany L., Knafels, John D., Sahasrabudhe, Parag V., Rosado, Amy, Sommese, Ruth F., Reyes, Allan R., Ward, Jessica, Roth Flach, Rachel J., Wang, Xiaochun, Buzon, Leanne M., Reese, Matthew R., Bhattacharya, Samit K., Omoto, Kiyoyuki, Filipski, Kevin J.

“…The mammalian mitochondrial branched-chain ketoacid dehydrogenase (BCKD) complex is a multienzyme complex involved in the catabolism of branched-chain amino…”
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Understanding the Impact of the P-loop Conformation on Kinase Selectivity by Guimarães, Cristiano R. W, Rai, Brajesh K, Munchhof, Michael J, Liu, Shenping, Wang, Jian, Bhattacharya, Samit K, Buckbinder, Leonard

“…This work addresses the link between selectivity and an unusual, folded conformation for the P-loop observed initially for MAP4K4 and subsequently for other…”
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A Total Synthesis of the Methyl Glycoside of Ganglioside GM1 by Bhattacharya, Samit K, Danishefsky, Samuel J

“…The total synthesis of the methyl glycoside of GM1 (1b) has been accomplished. The key step in the synthesis involves the sulfonamidoglycosidation reaction,…”
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2‑Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety by Dow, Robert L, Ammirati, Mark, Bagley, Scott W, Bhattacharya, Samit K, Buckbinder, Leonard, Cortes, Christian, El-Kattan, Ayman F, Ford, Kristen, Freeman, Gary B, Guimarães, Cristiano R. W, Liu, Shenping, Niosi, Mark, Skoura, Athanasia, Tess, David

“…Studies have linked the serine-threonine kinase MAP4K4 to the regulation of a number of biological processes and/or diseases, including diabetes, cancer,…”
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Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1) by Filipski, Kevin J, Sammons, Matthew F, Bhattacharya, Samit K, Panteleev, Jane, Brown, Janice A, Loria, Paula M, Boehm, Markus, Smith, Aaron C, Shavnya, Andre, Conn, Edward L, Song, Kun, Weng, Yan, Facemire, Carie, Jüppner, Harald, Clerin, Valerie

“…Sodium-phosphate cotransporter 2a, or NaPi2a (SLC34A1), is a solute-carrier (SLC) transporter located in the kidney proximal tubule that reabsorbs…”
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Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK) by Edmonds, David J, Kung, Daniel W, Kalgutkar, Amit S, Filipski, Kevin J, Ebner, David C, Cabral, Shawn, Smith, Aaron C, Aspnes, Gary E, Bhattacharya, Samit K, Borzilleri, Kris A, Brown, Janice A, Calabrese, Matthew F, Caspers, Nicole L, Cokorinos, Emily C, Conn, Edward L, Dowling, Matthew S, Eng, Heather, Feng, Bo, Fernando, Dilinie P, Genung, Nathan E, Herr, Michael, Kurumbail, Ravi G, Lavergne, Sophie Y, Lee, Esther C.-Y, Li, Qifang, Mathialagan, Sumathy, Miller, Russell A, Panteleev, Jane, Polivkova, Jana, Rajamohan, Francis, Reyes, Allan R, Salatto, Christopher T, Shavnya, Andre, Thuma, Benjamin A, Tu, Meihua, Ward, Jessica, Withka, Jane M, Xiao, Jun, Cameron, Kimberly O

“…Optimization of the pharmacokinetic (PK) properties of a series of activators of adenosine monophosphate-activated protein kinase (AMPK) is described…”
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Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate by Bhattacharya, Samit K, Andrews, Kim, Beveridge, Ramsay, Cameron, Kimberly O, Chen, Chiliu, Dunn, Matthew, Fernando, Dilinie, Gao, Hua, Hepworth, David, Jackson, V. Margaret, Khot, Vishal, Kong, Jimmy, Kosa, Rachel E, Lapham, Kimberly, Loria, Paula M, Londregan, Allyn T, McClure, Kim F, Orr, Suvi T. M, Patel, Jigna, Rose, Colin, Saenz, James, Stock, Ingrid A, Storer, Gregory, VanVolkenburg, Maria, Vrieze, Derek, Wang, Guoqiang, Xiao, Jun, Zhang, Yingxin

“…The identification of potent, highly selective orally bioavailable ghrelin receptor inverse agonists from a spiro-azetidino-piperidine series is described…”
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MAP4K4 Is a Threonine Kinase That Phosphorylates FARP1 by Schwaid, Adam G, Su, Chunyan, Loos, Paula, Wu, Jiang, Nguyen, Chuong, Stone, Kathryn L, Kanyo, Jean, Geoghegan, Kieran F, Bhattacharya, Samit K, Dow, Robert L, Buckbinder, Leonard, Carpino, Philip A

“…Mitogen-activated protein kinase 4 (MAP4K4) regulates the MEK kinase cascade and is implicated in cytoskeletal rearrangement and migration; however,…”
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Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor by McClure, Kim F., Jackson, Margaret, Cameron, Kimberly O., Kung, Daniel W., Perry, David A., Orr, Suvi T.M., Zhang, Yingxin, Kohrt, Jeffrey, Tu, Meihua, Gao, Hua, Fernando, Dilinie, Jones, Ryan, Erasga, Noe, Wang, Guoqiang, Polivkova, Jana, Jiao, Wenhua, Swartz, Roger, Ueno, Hirokazu, Bhattacharya, Samit K., Stock, Ingrid A., Varma, Sam, Bagdasarian, Victoria, Perez, Sylvie, Kelly-Sullivan, Dawn, Wang, Ruduan, Kong, Jimmy, Cornelius, Peter, Michael, Laura, Lee, Eunsun, Janssen, Ann, Steyn, Stefanus J., Lapham, Kimberly, Goosen, Theunis

“…The optimization for selectivity and central receptor occupancy for a series of spirocyclic azetidine–piperidine inverse agonists of the ghrelin receptor is…”
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Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment by Ammirati, Mark, Bagley, Scott W, Bhattacharya, Samit K, Buckbinder, Leonard, Carlo, Anthony A, Conrad, Rebecca, Cortes, Christian, Dow, Robert L, Dowling, Matthew S, El-Kattan, Ayman, Ford, Kristen, Guimarães, Cristiano R. W, Hepworth, David, Jiao, Wenhua, LaPerle, Jennifer, Liu, Shenping, Londregan, Allyn, Loria, Paula M, Mathiowetz, Alan M, Munchhof, Michael, Orr, Suvi T. M, Petersen, Donna N, Price, David A, Skoura, Athanasia, Smith, Aaron C, Wang, Jian

“…Recent studies in adipose tissue, pancreas, muscle, and macrophages suggest that MAP4K4, a serine/threonine protein kinase may be a viable target for…”
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Design and Synthesis of Truncated EGF-A Peptides that Restore LDL-R Recycling in the Presence of PCSK9 In Vitro by Schroeder, Christina I., Swedberg, Joakim E., Withka, Jane M., Rosengren, K. Johan, Akcan, Muharrem, Clayton, Daniel J., Daly, Norelle L., Cheneval, Olivier, Borzilleri, Kris A., Griffor, Matt, Stock, Ingrid, Colless, Barbara, Walsh, Phillip, Sunderland, Philip, Reyes, Allan, Dullea, Robert, Ammirati, Mark, Liu, Shenping, McClure, Kim F., Tu, Meihua, Bhattacharya, Samit K., Liras, Spiros, Price, David A., Craik, David J.

“…Disrupting the binding interaction between proprotein convertase (PCSK9) and the epidermal growth factor-like domain A (EGF-A domain) in the low-density…”
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Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor by JANI, Jitesh P, FINN, Richard S, MORRIS, Joel, MOYER, James D, PUSTILNIK, Leslie R, RAFIDI, Kristina, RALSTON, Sherry, ROSSI, Ann Marie K, STEYN, Stefanus J, WAGNER, Larry, WINTER, Steven M, BHATTACHARYA, Samit K, CAMPBELL, Mary, COLEMAN, Kevin G, CONNELL, Richard D, CURRIER, Nicolas, EMERSON, Erling O, FLOYD, Eugenia, HARRIMAN, Shawn, KATH, John C

“…Amplification and overexpression of erbB2 (Her-2/neu) proto-oncogene has been linked to human malignancies including tumors of the breast, ovary, and stomach…”
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Evaluation and Synthesis of Polar Aryl- and Heteroaryl Spiroazetidine-Piperidine Acetamides as Ghrelin Inverse Agonists by Orr, Suvi T. M, Beveridge, Ramsay, Bhattacharya, Samit K, Cameron, Kimberly O, Coffey, Steven, Fernando, Dilinie, Hepworth, David, Jackson, Margaret V, Khot, Vishal, Kosa, Rachel, Lapham, Kimberly, Loria, Paula M, McClure, Kim F, Patel, Jigna, Rose, Colin, Saenz, James, Stock, Ingrid A, Storer, Gregory, von Volkenburg, Maria, Vrieze, Derek, Wang, Guoqiang, Xiao, Jun, Zhang, Yingxin

“…Several polar heteroaromatic acetic acids and their piperidine amides were synthesized and evaluated as ghrelin or type 1a growth hormone secretagogue receptor…”
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