Search Results - "HRUBY, V. J"

Genetic and pharmacological antagonism of NK1 receptor prevents opiate abuse potential by Sandweiss, A J, McIntosh, M I, Moutal, A, Davidson-Knapp, R, Hu, J, Giri, A K, Yamamoto, T, Hruby, V J, Khanna, R, Largent-Milnes, T M, Vanderah, T W

“…Development of an efficacious, non-addicting analgesic has been challenging. Discovery of novel mechanisms underlying addiction may present a solution. Here we…”
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Spinal or systemic TY005, a peptidic opioid agonist/neurokinin 1 antagonist, attenuates pain with reduced tolerance by Largent‐Milnes, TM, Yamamoto, T, Nair, P, Moulton, JW, Hruby, VJ, Lai, J, Porreca, F, Vanderah, TW

“…BACKGROUND AND PURPOSE The use of opioids in treating pain is limited due to significant side effects including somnolence, constipation, analgesic tolerance,…”
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Conformational and topographical considerations in designing agonist peptidomimetics from peptide leads by Hruby, V J, Balse, P M

“…The design of peptidomimetic ligands with agonist biological activities in vitro and in vivo has been challenging. Lofty goals have been set for this research…”
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Development and characterisation of novel fentanyl-delta opioid receptor antagonist based bivalent ligands by Bird, M.F., Vardanyan, R.S., Hruby, V.J., Calò, G., Guerrini, R., Salvadori, S., Trapella, C., McDonald, J., Rowbotham, D.J., Lambert, D.G.

“…Opioid tolerance is a limiting factor in chronic pain. Delta opioid peptide (DOP)(δ) receptor antagonism has been shown to reduce tolerance. Here, the common…”
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Design in Topographical Space of Peptide and Peptidomimetic Ligands That Affect Behavior. A Chemist's Glimpse at the Mind−Body Problem by Hruby, Victor J

“…Efforts to determine the bioactive conformations of peptide ligands for membrane-bound proteins such as G-protein-coupled receptors (GPCRs) have been…”
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Exploring Ramachandran and chi space: conformationally constrained amino acids and peptides in the design of bioactive polypeptide ligands by Cowell, S M, Lee, Y S, Cain, J P, Hruby, V J

“…Ligand binding and concomitant changes in receptor structure provide the means to target signal transduction pathways. With appropriate refinement of the…”
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Role of melanocortinergic neurons in feeding and the agouti obesity syndrome by Fan, W, Boston, B.A, Kesterson, R.A, Hruby, V.J, Cone, R.D

“…Dominant alleles at the agouti locus (A) cause an obesity syndrome in the mouse, as a consequence of ectopic expression of the agouti peptide. This peptide,…”
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Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 induces penile erection via brain and spinal melanocortin receptors by WESSELLS, H, HRUBY, V. J, HACKETT, J, HAN, G, BALSE-SRINIVASAN, P, VANDERAH, T. W

“…Penile erection induced by alpha-melanocyte-stimulating hormone and melanocortin receptors (MC-R) in areas of the spinal cord and periphery has not been…”
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D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity by Grieco, P, Balse, P M, Weinberg, D, MacNeil, T, Hruby, V J

“…In our search for potent and receptor-selective agonists and antagonists, we report here the results of D-amino acid substitution at each position of the short…”
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Solid-Phase Synthesis of O-Linked Glycopeptide Analogues of Enkephalin by Mitchell, Scott A, Pratt, Matt R, Hruby, Victor J, Polt, Robin

“…The synthesis of 18 N-α-FMOC-amino acid glycosides for solid-phase glycopeptide assembly is reported. The glycosides were synthesized either from the…”
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SNC 80, a selective, nonpeptidic and systemically active opioid delta agonist by Bilsky, E J, Calderon, S N, Wang, T, Bernstein, R N, Davis, P, Hruby, V J, McNutt, R W, Rothman, R B, Rice, K C, Porreca, F

“…The present study has investigated the pharmacology of SNC 80, a nonpeptidic ligand proposed to be a selective delta agonist in vitro and in vivo. SNC 80 was…”
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Plasmon resonance studies of agonist/antagonist binding to the human delta-opioid receptor: new structural insights into receptor-ligand interactions by Salamon, Z, Cowell, S, Varga, E, Yamamura, H I, Hruby, V J, Tollin, G

“…Structural changes accompanying the binding of ligands to the cloned human delta-opioid receptor immobilized in a solid-supported lipid bilayer have been…”
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Design of Novel Chimeric Melanotropin−Deltorphin Analogues. Discovery of the First Potent Human Melanocortin 1 Receptor Antagonist by Han, G, Quillan, J. M, Carlson, K, Sadée, W, Hruby, V. J

“…A number of novel α-melanotropin (α-MSH) analogues have been designed, synthesized, and assayed for bioactivity at the melanocortin-1 (MC1) receptor from…”
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Practical and Efficient Synthesis of Orthogonally Protected Constrained 4-Guanidinoprolines by Tamaki, Makoto, Han, Guoxia, Hruby, Victor J

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Emerging approaches in the molecular design of receptor-selective peptide ligands: conformational, topographical and dynamic considerations by Hruby, V J, al-Obeidi, F, Kazmierski, W

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A new type of synthetic peptide library for identifying ligand-binding activity by Lam, Kit S, Salmon, Sydney E, Hersh, Evan M, Hruby, Victor J, Kazmierski, Wieslaw M, Knapp, Richard J

“…Our aim was to improve techniques for drug development by facilitating the identification of small molecules that bind with high affinity to acceptor molecules…”
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Enkephalin Glycopeptide Analogues Produce Analgesia with Reduced Dependence Liability by Bilsky, Edward J, Egleton, Richard D, Mitchell, Scott A, Palian, Michael M, Davis, Peg, Huber, Jason D, Jones, Heather, Yamamura, Henry I, Janders, Jacqueline, Davis, Thomas P, Porreca, Frank, Hruby, Victor J, Polt, Robin

“…Endogenous peptides (e.g. enkephalins) control many aspects of brain function, cognition, and perception. The use of these neuroactive peptides in diverse…”
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Molecular biology and pharmacology of cloned opioid receptors by Knapp, R J, Malatynska, E, Collins, N, Fang, L, Wang, J Y, Hruby, V J, Roeske, W R, Yamamura, H I

“…The cloning and expression of DNA for the three major opioid receptor types (mu, delta, and kappa) present new research opportunities for the characterization…”
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Plasmon resonance methods in GPCR signaling and other membrane events by Alves, I D, Park, C K, Hruby, V J

“…The existence of surface guided electromagnetic waves has been theoretically predicted from Maxwell's equations and investigated during the first decades of…”
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The effect of halogenation on blood–brain barrier permeability of a novel peptide drug by Gentry, C.L, Egleton, R.D, Gillespie, T, Abbruscato, T.J, Bechowski, H.B, Hruby, V.J, Davis, T.P

“…The utility of a drug depends on its ability to reach appropriate receptors at the target tissue and remain metabolically stable to produce the desired effect…”
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