Search Results - "Koblan, K."

Chronic neuropathic pain is accompanied by global changes in gene expression and shares pathobiology with neurodegenerative diseases by Wang, H, Sun, H, Della Penna, K, Benz, R.J, Xu, J, Gerhold, D.L, Holder, D.J, Koblan, K.S

“…Neuropathic pain is induced by injury or disease of the nervous system. Studies aimed at understanding the molecular pathophysiology of neuropathic pain have…”
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Assessment of human abuse potential of dasotraline compared to methylphenidate and placebo in recreational stimulant users by Koblan, K.S, Hopkins, S.C, Sarma, K, Gallina, N, Jin, F, Levy-Cooperman, N, Schoedel, K.A, Loebel, A

“…Abstract Aims The aim of this study was to evaluate the abuse potential of dasotraline, a novel dopamine and norepinephrine reuptake inhibitor with slow…”
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Functional neuroimaging study of a new compound for schizophrenia in healthy volunteers with high or low schizotypy by Perini, F, Nazimek, J, Browning, M, Dawson, G, Nishikawa, H, Campbell, U, Hopkins, S, Loebel, A, Koblan, K, Deakin, J.F.W

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The effects of a novel histamine-3 receptor inverse agonist on essential tremor in comparison to stable levels of alcohol by Zoethout, RWM, Iannone, R, Bloem, BR, Palcza, J, Murphy, G, Chodakewitz, J, Buntinx, A, Gottesdiener, K, Marsilio, S, Rosen, L, van Dyck, K, Louis, ED, Cohen, AF, Schoemaker, RC, Tokita, S, Sato, N, Koblan, KS, Hargreaves, RH, Renger, JJ, van Gerven, JMA

“…Essential tremor (ET) is a common movement disorder. Animal studies show that histaminergic modulation may affect the pathological processes involved in the…”
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Cloning, characterization and central nervous system distribution of receptor activity modifying proteins in the rat by Oliver, K. R., Kane, S. A., Salvatore, C. A., Mallee, J. J., Kinsey, A. M., Koblan, K. S., Keyvan-Fouladi, N., Heavens, R. P., Wainwright, A., Jacobson, M., Dickerson, I. M., Hill, R. G.

“…Calcitonin gene‐related peptide (CGRP), adrenomedullin (ADM), amylin and calcitonin (CT) are structurally and functionally related neuropeptides. It has…”
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Tuberoinfundibular peptide of 39 residues (TIP39): molecular structure and activity for parathyroid hormone 2 receptor by Della Penna, K., Kinose, F., Sun, H., Koblan, K.S., Wang, H.

“…The neuropeptide TIP39 was recently purified from bovine hypothalamus based on the ability of the peptide to activate the parathyroid hormone 2 receptor…”
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Mouse mammary tumor virus-Ki-rasB transgenic mice develop mammary carcinomas that can be growth-inhibited by a farnesyl :protein transferase inhibitor by OMER, C. A, ZUNXUAN CHEN, DAVIDE, J. P, ELLIS, M. S, GIBBS, J. B, GREENBERG, I, HAMILTON, K, KOBLAN, K. S, KRAL, A. M, DONGMING LIU, LOBELL, R. B, MILLER, P. J, DIEHL, R. E, MOSSER, S. D, O'NEILL, T. J, RANDS, E, SCHABER, M. D, SENDERAK, E. T, OLIFF, A, KOHL, N. E, CONNER, M. W, CHEN, H. Y, TRUMBAUER, M. E, GOPAL-TRUTER, S, SEEBURGER, G, BHIMNATHWALA, H, ABRAMS, M. T

“…For Ras oncoproteins to transform mammalian cells, they must be posttranslationally modified with a farnesyl group in a reaction catalyzed by the enzyme…”
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Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase by Dinsmore, Christopher J., Williams, Theresa M., O'Neill, Timothy J., Liu, Dongming, Rands, Elaine, Culberson, J.Christopher, Lobell, Robert B., Koblan, Kenneth S., Kohl, Nancy E., Gibbs, Jackson B., Oliff, Allen I., Graham, Samuel L., Hartman, George D.

“…The design and syntheses of non-thiol inhibitors of farnesyl-protein transferase are described. Optimization of cysteine-substituted diarylethers led to highly…”
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P.0450 The safety profile of the trace amine–associated receptor 1 agonist, SEP-363856, is distinct from atypical antipsychotics by Hopkins, S.C., Ogirala, A., Worden, M., Koblan, K.

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Design and Biological Activity of (S)-4-(5-{[1-(3-Chlorobenzyl)-2- oxopyrrolidin-3-ylamino]methyl}imidazol-1-ylmethyl)benzonitrile, a 3-Aminopyrrolidinone Farnesyltransferase Inhibitor with Excellent Cell Potency by Bell, Ian M, Gallicchio, Steven N, Abrams, Marc, Beshore, Douglas C, Buser, Carolyn A, Culberson, J. Christopher, Davide, Joseph, Ellis-Hutchings, Michelle, Fernandes, Christine, Gibbs, Jackson B, Graham, Samuel L, Hartman, George D, Heimbrook, David C, Homnick, Carl F, Huff, Joel R, Kassahun, Kelem, Koblan, Kenneth S, Kohl, Nancy E, Lobell, Robert B, Lynch, Joseph J, Miller, Patricia A, Omer, Charles A, Rodrigues, A. David, Walsh, Eileen S, Williams, Theresa M

“…The synthesis, structure−activity relationships, and biological properties of a novel series of imidazole-containing inhibitors of farnesyltransferase are…”
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P.163 SEP-363856, a novel psychotropic agent with a unique, non-d2 mechanism of action by Jones, P., Dedic, N., Hopkins, S., Synan, C., Koblan, K.

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Design and in Vivo Analysis of Potent Non-Thiol Inhibitors of Farnesyl Protein Transferase by Anthony, Neville J, Gomez, Robert P, Schaber, Micheal D, Mosser, Scott D, Hamilton, Kelly A, O'Neil, Timothy J, Koblan, Kenneth S, Graham, Samuel L, Hartman, George D, Shah, Daksha, Rands, Elaine, Kohl, Nancy E, Gibbs, Jackson B, Oliff, Allen I

“…Inhibitors of farnesyl protein transferase (FPTase) based upon a pseudotripeptide template are described that comprise an imidazole group substituted with a…”
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Characterization and localization of a human serine racemase by Xia, Menghang, Liu, Yuan, Figueroa, David J., Chiu, Chi-Sung, Wei, Nan, Lawlor, Ann-Marie, Lu, Ping, Sur, Cyrille, Koblan, Ken S., Connolly, Thomas M.

“…d-serine is present in the mammalian central nervous system, where it acts as one of the co-activators of N-methyl-D aspartate receptors. Synthesis of d-serine…”
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2-Substituted Piperazines as Constrained Amino Acids. Application to the Synthesis of Potent, Non Carboxylic Acid Inhibitors of Farnesyltransferase by Williams, Theresa M, Ciccarone, Terrence M, MacTough, Suzanne C, Bock, Rhonda L, Conner, Michael W, Davide, Joseph P, Hamilton, Kelly, Koblan, Kenneth S, Kohl, Nancy E, Kral, Astrid M, Mosser, Scott D, Omer, Charles A, Pompliano, David L, Rands, Elaine, Schaber, Michael D, Shah, Daksha, Wilson, Francine R, Gibbs, Jackson B, Graham, Samuel L, Hartman, George D, Oliff, Allen I, Smith, Robert L

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A Farnesyltransferase Inhibitor Induces Tumor Regression in Transgenic Mice Harboring Multiple Oncogenic Mutations by Mediating Alterations in Both Cell Cycle Control and Apoptosis by Barrington, Rebecca E., Subler, Mark A., Rands, Elaine, Omer, Charles A., Miller, Patricia J., Hundley, Jeffrey E., Koester, Steven K., Troyer, Dean A., Bearss, David J., Conner, Michael W., Gibbs, Jackson B., Hamilton, Kelly, Koblan, Kenneth S., Mosser, Scott D., O'Neill, Timothy J., Schaber, Michael D., Senderak, Edith T., Windle, Jolene J., Oliff, Allen, Kohl, Nancy E.

“…Article Usage Stats Services MCB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase by Ciccarone, Terrence M., MacTough, Suzanne C., Williams, Theresa M., Dinsmore, Christopher J., O'Neill, Timothy J., Shah, Daksha, Culberson, J.Christopher, Koblan, Kenneth S., Kohl, Nancy E., Gibbs, Jackson B., Oliff, Allen I., Graham, Samuel L., Hartman, George D.

“…The design and syntheses of non-thiol inhibitors of farnesyl-protein transferase are described. Substitutions on an imidazolylmethyl-AMBA-methionine template…”
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Sub-chronic administration of zolpidem affects modifications to rat sleep architecture by Renger, John J, Dunn, Susan L, Motzel, Sherri L, Johnson, Colena, Koblan, Kenneth S

“…Gamma-aminobutyric acid A receptor (GABA AR) modulators constitute the majority of clinically relevant sedative-hypnotics. Animal studies have clearly…”
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P.100 Efficacy and safety of SEP-363856, a novel non-D2 agent, in the treatment of schizophrenia: A 4-week, randomized, placebo-controlled trial by Koblan, K., Hopkins, S., Kent, J., Cheng, H., Goldman, R., Loebel, A.

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Characterisation of the effects of a non-peptide CGRP receptor antagonist in SK-N-MC cells and isolated human cerebral arteries by Edvinsson, Lars, Sams, Anette, Jansen-Olesen, Inger, Tajti, Janos, Kane, Stefanie A, Rutledge, Ruth Z, Koblan, Kenneth S, Hill, Raymond G, Longmore, Jenny

“…The cerebral circulation is innervated by calcitonin gene-related peptide (CGRP) containing fibers originating in the trigeminal ganglion. During a migraine…”
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Site-specific enthalpic regulation of DNA transcription at bacteriophage .lambda. OR by Koblan, Kenneth S, Ackers, Gary K

“…Binding of cI repressor to DNA fragments containing the three specific binding sites of the right operator (OR) of bacteriophage lambda was studied in vitro…”
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