- Identification and Optimization of a Novel Inhibitor of Mitochondrial Calpain 10.
[作者:Rasbach, Kyle A.;Arrington, David D.;Odejinmi, Sina;Giguere, Chris;Beeson, Craig C.;Schnellmann, Rick G.;,期刊:Journal of Medicinal Chemistry, 页码:181-188 , 文章类型: 研究论文,,卷期:2009年52-1]
- Calpain 10 has been localized to the mitochondria and is a key mediator of Ca2+ induced mitochondrial dysfunction. A peptide screen followed by a series of modifications identified the homodisulfide form of CYGAK2 as an...
- Short Antisense Oligonucleotides with Novel 2'-4' Conformationaly Restricted Nucleoside Analogues Show Improved Potency without Increased Toxicity in Animals.
[作者:Seth, Punit P.;Siwkowski, Andrew;Allerson, Charles R.;Vasquez, Guillermo;Lee, Sam;Prakash, Thazha P.;Wancewicz, Edward V.;Witchell, Donna;Swayze, Eric E.;,期刊:Journal of Medicinal Chemistry, 页码:10-13 , 文章类型: 研究论文,,卷期:2009年52-1]
- The potency of second generation antisense oligonucleotides (ASOs) in animals was increased 3- to 5 -fold (ED50 u 2-5 mg/kg) without producing hepatotoxicity, by reducing ASO length (20-mer to 14-mer) and by employing no...
- Discovery of a New Class of Potential Multifunctional Atypical Antipsychotic Agents Targeting Dopamine D3 and Serotonin 5-HT1A and 5-HT2A Receptors: Design, Synthesis, and Effects on Behavior.
[作者:Butini, Stefania;Gemma, Sandra;Campiani, Giuseppe;Franceschini, Silvia;Trotta, Francesco;Borriello, Marianna;Ceres, Nicoletta;Ros, Sindu;Sanna Coccone, Salvatore;Bernetti, Matteo;De Angelis, Meri;Brindisi, Margherita;Nacci, Vito;Fiorini, Isabella;Novellin,期刊:Journal of Medicinal Chemistry, 页码:151-169 , 文章类型: 研究论文,,卷期:2009年52-1]
- Dopamine D3 antagonism combined with serotonin 5-HT1A and 5-HT2A receptor occupancy may represent a novel paradigm for developing innovative antipsychotics. The unique pharmacol. features of 5i are a high affinity for d...
- Design and Synthesis of a Cyclic Double Mutant Peptide (cyclo(87-99)[A91,A96]MBP87-99) Induces Altered Responses in Mice after Conjugation to Mannan: Implications in the Immunotherapy of Multiple Sclerosis.
[作者:Katsara, Maria;Deraos, George;Tselios, Theodore;Matsoukas, Minos-Timotheos;Friligou, Irene;Matsoukas, John;Apostolopoulos, Vasso;,期刊:Journal of Medicinal Chemistry, 页码:214-218 , 文章类型: 研究论文,,卷期:2009年52-1]
- Altered peptide ligands that alter immune responses are a promising approach to the immunotherapy of multiple sclerosis. Cyclic peptides are of interest because the limited stability of linear peptides restricts their u...
- Discovery of Targeting Ligands for Breast Cancer Cells Using the One-Bead One-Compound Combinatorial Method.
[作者:Yao, Nianhuan;Xiao, Wenwu;Wang, Xiaobing;Marik, Jan;Park, See Hyoung;Takada, Yoshikazu;Lam, Kit S.;,期刊:Journal of Medicinal Chemistry, 页码:126-133 , 文章类型: 研究论文,,卷期:2009年52-1]
- Four "one-bead one-compd." (OBOC) combinatorial libraries were designed, synthesized, and screened against MDA-MB-231 breast cancer cells. A novel cyclic peptide 1 (LXY1) with high binding specificity to a3 integrin was...
- Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates.
[作者:Mor, Marco;Lodola, Alessio;Rivara, Silvia;Vacondio, Federica;Duranti, Andrea;Tontini, Andrea;Sanchini, Silvano;Piersanti, Giovanni;Clapper, Jason R.;King, Alvin R.;Tarzia, Giorgio;Piomelli, Daniele;,期刊:Journal of Medicinal Chemistry, 页码:224-224 , 文章类型: 研究论文,,卷期:2009年52-1]
- On page 3487, in the left column, in paragraph 1, in lines 7 and 8, "The mechanism responsible for the inactivation of FAAH...", was incorrectly given, and should read: "The catalytic mechanism of FAAH..".
- Antagonists of the Human A2A Adenosine Receptor. 4. Design, Synthesis, and Preclinical Evaluation of 7-Aryltriazolo[4,5-d]pyrimidines.
[作者:Gillespie, Roger J.;Bamford, Samantha J.;Botting, Ruth;Comer, Mike;Denny, Sarah;Gaur, Suneel;Griffin, Michael;Jordan, Allan M.;Knight, Anthony R.;Lerpiniere, Joanne;Leonardi, Stefania;Lightowler, Sean;McAteer, Steven;Merrett, Angela;Misra, Anil;Padfield,,期刊:Journal of Medicinal Chemistry, 页码:33-47 , 文章类型: 研究论文,,卷期:2009年52-1]
- Antagonism of the human A2A receptor has been implicated as a point of therapeutic intervention in the alleviation of the symptoms assocd. with Parkinson's disease. This is thought to occur, at least in part, by increas...
- Highly Potent 4-Amino-indolo[2,3-c]azepin-3-one-Containing Somatostatin Mimetics with a Range of sst Receptor Selectivities.
[作者:Feytens, Debby;De Vlaeminck, Magali;Cescato, Renzo;Tourwe, Dirk;Reubi, Jean Claude;,期刊:Journal of Medicinal Chemistry, 页码:95-104 , 文章类型: 研究论文,,卷期:2009年52-1]
- The synthesis, biol. evaluation, and conformational anal. of 4-amino-indolo[2,3-c]azepin-3-one (Aia)-contg. SRIF mimetics, i.e. I譚FA, are reported. Different subtype selectivities are obsd. depending on the N- and C-ter...
- Synthesis and Evaluation of Benzothiazole-Based Analogues as Novel, Potent, and Selective Fatty Acid Amide Hydrolase Inhibitors.
[作者:Wang, Xueqing;Sarris, Katerina;Kage, Karen;Zhang, Di;Brown, Scott P.;Kolasa, Teodozyi;Surowy, Carol;El Kouhen, Odile F.;Muchmore, Steven W.;Brioni, Jorge D.;Stewart, Andrew O.;,期刊:Journal of Medicinal Chemistry, 页码:170-180 , 文章类型: 研究论文,,卷期:2009年52-1]
- High-throughput screening (HTS) identified benzothiazole analog (I) as a potent fatty acid amide hydrolase (FAAH) inhibitor. Structure-activity relationship (SAR) studies indicated that the sulfonyl group, the piperidin...
- Modulation of Wnt Signaling Through Inhibition of Secreted Frizzled-Related Protein I (sFRP-1) with N-Substituted Piperidinyl Diphenylsulfonyl Sulfonamides.
[作者:Moore, William J.;Kern, Jeffrey C.;Bhat, Ramesh;Commons, Thomas J.;Fukayama, Shoichi;Goljer, Igor;Krishnamurthy, Girija;Magolda, Ronald L.;Nogle, Lisa;Pitts, Keith;Stauffer, Barb;Trybulski, Eugene J.;Welmaker, Gregory S.;Wilson, Matthew;Bodine, Peter V. N,期刊:Journal of Medicinal Chemistry, 页码:105-116 , 文章类型: 研究论文,,卷期:2009年52-1]
- The diphenylsulfonyl sulfonamide scaffold represented by 1 (WAY-316606) are small mol. inhibitors of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. Modulators of the Wnt pathway h...
- Chemical Modification and Biological Evaluation of New Semisynthetic Derivatives of 28,29-Didehydronystatin A1 (S44HP), a Genetically Engineered Antifungal Polyene Macrolide Antibiotic.
[作者:Preobrazhenskaya, Maria N.;Olsufyeva, Evgenia N.;Solovieva, Svetlana E.;Tevyashova, Anna N.;Reznikova, Marina I.;Luzikov, Yuryi N.;Terekhova, Larisa P.;Trenin, Aleksei S.;Galatenko, Olga A.;Treshalin, Ivan D.;Mirchink, Elena P.;Bukhman, Vladimir M.;Sletta,期刊:Journal of Medicinal Chemistry, 页码:189-196 , 文章类型: 研究论文,,卷期:2009年52-1]
- Twenty-three new derivs. of the heptaene nystatin analog 28,29-didehydronystatin A1 (S44HP) were obtained by chem. modification of C16 carboxyl and amino groups of mycosamine. These derivs. comprised 15 carboxamides, 4 ...
- The Design, Synthesis, and Antiviral Activity of 4'-Azidocytidine Analogues against Hepatitis C Virus Replication: The Discovery of 4'-Azidoarabinocytidine.
[作者:Smith, David B.;Kalayanov, Genadiy;Sund, Christian;Winqvist, Anna;Pinho, Pedro;Maltseva, Tatiana;Morisson, Veronique;Leveque, Vincent;Rajyaguru, Sonal;Le Pogam, Sophie;Najera, Isabel;Benkestock, Kurt;Zhou, Xiao-Xiong;Maag, Hans;Cammack, Nick;Martin, Josep,期刊:Journal of Medicinal Chemistry, 页码:219-223 , 文章类型: 研究论文,,卷期:2009年52-1]
- and selective inhibitor of HCV replication targeting the RNA-dependent RNA polymerase of hepatitis C virus, NS5B. Here the synthesis and biol. evaluation of several derivs. of 4'-azidocytidine by varying the substituent...
|