Search Results - "Kamenecka, T."

Small molecule PGC-1α1 protein stabilizers induce adipocyte Ucp1 expression and uncoupled mitochondrial respiration by Pettersson-Klein, A.T., Izadi, M., Ferreira, D.M.S., Cervenka, I., Correia, J.C., Martinez-Redondo, V., Southern, M., Cameron, M., Kamenecka, T., Agudelo, L.Z., Porsmyr-Palmertz, M., Martens, U., Lundgren, B., Otrocka, M., Jenmalm-Jensen, A., Griffin, P.R., Ruas, J.L.

“…The peroxisome proliferator-activated receptor-γ coactivator-1α1 (PGC-1α1) regulates genes involved in energy metabolism. Increasing adipose tissue energy…”
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PPARG Post-translational Modifications Regulate Bone Formation and Bone Resorption by Stechschulte, L.A., Czernik, P.J., Rotter, Z.C., Tausif, F.N., Corzo, C.A., Marciano, D.P., Asteian, A., Zheng, J., Bruning, J.B., Kamenecka, T.M., Rosen, C.J., Griffin, P.R., Lecka-Czernik, B.

“…The peroxisome proliferator-activated receptor gamma (PPARγ) regulates osteoblast and osteoclast differentiation, and is the molecular target of…”
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Discovery through Total Synthesis: A Retrospective on the Himastatin Problem by Kamenecka, Theodore M., Danishefsky, Samuel J.

“…A total synthesis of a structure proposed for himastatin was accomplished. The non‐identity of the fully synthetic material with himastatin necessitated a…”
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Deprotection of N- tert-butoxycarbonyl (Boc) groups in the presence of tert-butyl esters by Lin, Linus S, Lanza, Thomas, de Laszlo, Stephen E, Truong, Quang, Kamenecka, Theodore, Hagmann, William K

“…Deprotection of Boc groups in the presence of tert-butyl esters was achieved by using concentrated H 2SO 4 (1.5–3.0 equiv.) in tBuOAc or MeSO 3H (1.5–3.0…”
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Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers by Hamill, Terence G., Krause, Stephen, Ryan, Christine, Bonnefous, Celine, Govek, Steve, Seiders, T. Jon, Cosford, Nicholas D.P., Roppe, Jeffrey, Kamenecka, Ted, Patel, Shil, Gibson, Raymond E., Sanabria, Sandra, Riffel, Kerry, Eng, Waisi, King, Christopher, Yang, Xiaoqing, Green, Mitchell D., O'malley, Stacey S., Hargreaves, Richard, Burns, H. Donald

“…Three metabotropic glutamate receptor subtype 5 (mGluR5) PET tracers have been labeled with either carbon‐11 or fluorine‐18 and their in vitro and in vivo…”
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Small molecule PGC-1 alpha 1 protein stabilizers induce adipocyte Ucp1 expression and uncoupled mitochondrial respiration by Pettersson-Klein, A. T., Izadi, M., Ferreira, D. M. S., Cervenka, I., Correia, J. C., Martinez-Redondo, V., Southern, M., Cameron, M., Kamenecka, T., Agudelo, L. Z., Porsmyr-Palmertz, M., Martens, Ulf, Lundgren, Bo, Otrocka, M., Jenmalm-Jensen, A., Griffin, P. R., Ruas, J. L.

“…Objective : The peroxisome proliferator-activated receptor-gamma coactivator-1 alpha 1 (PGC-1 alpha 1) regulates genes involved in energy metabolism…”
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Total Syntheses of Epothilones A and B by Meng, Dongfang, Bertinato, Peter, Balog, Aaron, Su, Dai-Shi, Kamenecka, Ted, Sorensen, Erik J, Danishefsky, Samuel J

“…Convergent, stereocontrolled total syntheses of the microtubule-stabilizing macrolides epothilones A (2) and B (3) have been achieved. Four distinct…”
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Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists by Bonnefous, Céline, Vernier, Jean-Michel, Hutchinson, John H., Chung, Janice, Reyes-Manalo, Grace, Kamenecka, Theodore

“…The mGlu5 receptor has been implicated in a number of CNS disorders. Herein, we report on the discovery, synthesis, and biological evaluation of dipyridyl…”
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TRPV4 Is a Regulator of Adipose Oxidative Metabolism, Inflammation, and Energy Homeostasis by Ye, Li, Kleiner, Sandra, Wu, Jun, Sah, Rajan, Gupta, Rana K, Banks, Alexander S, Cohen, Paul, Khandekar, Melin J, Boström, Pontus, Mepani, Rina J, Laznik, Dina, Kamenecka, Theodore M, Song, Xinyi, Liedtke, Wolfgang, Mootha, Vamsi K, Puigserver, Pere, Griffin, Patrick R, Clapham, David E, Spiegelman, Bruce M

“…PGC1α is a key transcriptional coregulator of oxidative metabolism and thermogenesis. Through a high-throughput chemical screen, we found that molecules…”
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5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3′-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity by Roppe, Jeffrey R, Wang, Bowei, Huang, Dehua, Tehrani, Lida, Kamenecka, Theodore, Schweiger, Edwin J, Anderson, Jeffery J, Brodkin, Jesse, Jiang, Xiaohui, Cramer, Merryl, Chung, Janice, Reyes-Manalo, Grace, Munoz, Benito, Cosford, Nicholas D.P

“…Graphic Structure–activity relationship studies leading to the discovery of a new, orally active mGlu5 receptor antagonist are described. The title compound,…”
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N-Aryl 2,6-Dimethoxybiphenylalanine Analogues as VLA-4 Antagonists by Doherty, George A, Kamenecka, Theodore, McCauley, Ermenegilda, Van Riper, Gail, Mumford, Richard A, Tong, Sharon, Hagmann, William K

“…A series of N-arylated phenylalanine derivatives has been synthesized and has been shown to be potent inhibitors of the integrin VLA-4. N-phenyl and…”
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The discovery of sulfonylated dipeptides as Potent VLA-4 antagonists by Hagmann, William K, Durette, Philippe L, Lanza, Thomas, Kevin, Nancy Jo, de Laszlo, Stephen E, Kopka, Ihor E, Young, David, Magriotis, Plato A, Li, Bing, Lin, Linus S, Yang, Ginger, Kamenecka, Theodore, Chang, Linda L, Wilson, Jonathan, MacCoss, Malcolm, Mills, Sander G, Van Riper, Gail, McCauley, Ermengilda, Egger, Linda A, Kidambi, Usha, Lyons, Kathryn, Vincent, Stella, Stearns, Ralph, Colletti, Adria, Teffera, Johannes, Tong, Sharon, Fenyk-Melody, Judy, Owens, Karen, Levorse, Dorothy, Kim, Philip, Schmidt, John A, Mumford, Richard A

“…Directed screening of a carboxylic acid-containing combinatorial library led to the discovery of potent inhibitors of the integrin VLA-4. Subsequent…”
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Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4 by LIN, Linus S, LANZA, Thomas J, SCHMIDT, John A, HAGMANN, William K, CASTONGUAY, Laurie A, KAMENECKA, Theodore, MCCAULEY, Ermenegilda, VAN RIPER, Gail, EGGER, Linda A, MUMFORD, Richard A, XINCHUN TONG, MACCOSS, Malcolm

“…We have designed and synthesized a series of heterocyclic bioisosteres for an anilide based on molecular modeling. Excellent potency was retained in the…”
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ROR Inverse Agonist Suppresses Insulitis and Prevents Hyperglycemia in a Mouse Model of Type 1 Diabetes by Solt, Laura A, Banerjee, Subhashis, Campbell, Sean, Kamenecka, Theodore M, Burris, Thomas P

“…Hyperglycemia associated with type 1 diabetes is a consequence of immune-mediated destruction of insulin producing pancreatic β-cells. Although it is apparent…”
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The Discovery of acylated β-Amino acids as potent and orally bioavailable VLA-4 antagonists by Lin, Linus S., Kopka, Ihor E., Mumford, Richard A., Magriotis, Plato A., Lanza, Thomas, Durette, Philippe L., Kamenecka, Theodore, Young, David N., Laszlo, Stephen E.de, McCauley, Ermenegilda, Riper, Gail Van, Kidambi, Usha, Egger, Linda A., Tong, Xinchun, Lyons, Kathryn, Vincent, Stella, Stearns, Ralph, Colletti, Adria, Teffera, Yohannes, Fenyk-Melody, Judy, Schmidt, John A., MacCoss, Malcolm, Hagmann, William K.

“…Acylated β-amino acids are described as potent, specific and orally bioavailable antagonists of VLA-4. The initial lead was identified from a combinatorial…”
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Total Synthesis of Himastatin: Confirmation of the Revised Stereostructure by Kamenecka, Theodore M., Danishefsky, Samuel J.

“…A stereoisomer of the natural product and not himastatin, an unusual dimeric depsipeptide with promising antibiotic and antitumor properties, was obtained from…”
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Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor by Bonnefous, Céline, Vernier, Jean-Michel, Hutchinson, John H., Gardner, Michael F., Cramer, Merryl, James, Joyce K., Rowe, Blake A., Daggett, Lorrie P., Schaffhauser, Hervé, Kamenecka, Theodore M.

“…The metabotropic glutamate receptor 2 has been implicated in a number of central nervous system disorders. Herein, we report on the discovery, synthesis, and…”
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Identification of a Novel Non-retinoid Pan Inverse Agonist of the Retinoic Acid Receptors by Busby, Scott A, Kumar, Naresh, Kuruvilla, Dana S, Istrate, Monica A, Conkright, Juliana J, Wang, Yongjun, Kamenecka, Theodore M, Cameron, Michael D, Roush, William R, Burris, Thomas P, Griffin, Patrick R

“…Retinoids are potent forms of vitamin A and are involved in a broad range of physiological processes and the pharmacological effects of retinoids are primarily…”
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Studies in the Total Synthesis of Himastatin: A Revision of the Stereochemical Assignment by Kamenecka, Theodore M., Danishefsky, Samuel J.

“…A stereoisomer of the natural product and not himastatin, an unusual dimeric depsipeptide with promising antibiotic and antitumor properties, was obtained from…”
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Construction of Substituted Cyclohexanones by Reductive Cyclization of 7-Oxo-2,8-alkadienyl Esters by Kamenecka, Theodore M, Overman, Larry E, Ly Sakata, Sylvie K

“…Cyclization of 7-oxo-2,8-alkadienyl esters upon reaction with triphenylphosphinecopper hydride hexamer stereoselectively yields substituted cyclohexanones…”
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