- Designed Glycopeptides with Different b-Turn Types as Synthetic Probes for the Detection of Autoantibodies as Biomarkers of Multiple Sclerosis.
[作者:Carotenuto, Alfonso;Alcaro, Maria Claudia;Saviello, Maria Rosaria;Peroni, Elisa;Nuti, Francesca;Papini, Anna Maria;Novellino, Ettore;Rovero, Paolo;,期刊:Journal of Medicinal Chemistry, 页码:5304-5309 , 文章类型: 研究论文,,卷期:2008年51-17]
- Circulating autoantibodies have been recognized as disease biomarkers of autoimmune diseases. We have previously disclosed a synthetic glycopeptide that is able to detect specific autoantibodies in sera of patients who ...
- Cocrystal Structures of Primed Side-Extending a-Ketoamide Inhibitors Reveal Novel Calpain-Inhibitor Aromatic Interactions.
[作者:Qian, Jin;Cuerrier, Dominic;Davies, Peter L.;Li, Zhaozhao;Powers, James C.;Campbell, Robert L.;,期刊:Journal of Medicinal Chemistry, 页码:5264-5270 , 文章类型: 研究论文,,卷期:2008年51-17]
- of target proteins in response to Ca2+ signaling. When Ca2+ homeostasis is disrupted, calpain overactivation causes unregulated proteolysis, which can contribute to diseases such as postischemic injury and cataract form...
- Crystal Structures of Rat Vitamin D Receptor Bound to Adamantyl Vitamin D Analogs: Structural Basis for Vitamin D Receptor Antagonism and Partial Agonism.
[作者:Nakabayashi, Makoto;Yamada, Sachiko;Yoshimoto, Nobuko;Tanaka, Takashi;Igarashi, Miharu;Ikura, Teikichi;Ito, Nobutoshi;Makishima, Makoto;Tokiwa, Hiroaki;DeLuca, Hector F.;Shimizu, Masato;,期刊:Journal of Medicinal Chemistry, 页码:5320-5329 , 文章类型: 研究论文,,卷期:2008年51-17]
- The X-ray crystal structures of the rat VDR ligand-binding domain complexed with 19-norvitamin D compds. that contain an adamantyl and a coactivator peptide derived from DRIP205 are reported. These compds. show a series...
- Effect of Cathepsin K Inhibitors on Bone Resorption.
[作者:Teno, Naoki;Masuya, Keiichi;Ehara, Takeru;Kosaka, Takatoshi;Miyake, Takahiro;Irie, Osamu;Hitomi, Yuko;Matsuura, Naoko;Umemura, Ichiro;Iwasaki, Genji;Fukaya, Hiroaki;Toriyama, Kazuhiro;Uchiyama, Noriko;Nonomura, Kazuhiko;Sugiyama, Ikuo;Kometani, Motohiko;,期刊:Journal of Medicinal Chemistry, 页码:5459-5462 , 文章类型: 研究论文,,卷期:2008年51-17]
- On the basis of the pyrrolopyrimidine core structure that was previously discovered, cathepsin K inhibitors having a spiro amine at the P3 have been explored to enhance the target, bone marrow, tissue distribution. Sever...
- Inhibition of IkB Kinase-b and Anticancer Activities of Novel Chalcone Adamantyl Arotinoids.
[作者:Lorenzo, Paula;Alvarez, Rosana;Ortiz, Maria A.;Alvarez, Susana;Piedrafita, F. Javier;de Lera, Angel R.;,期刊:Journal of Medicinal Chemistry, 页码:5431-5440 , 文章类型: 研究论文,,卷期:2008年51-17]
- On the basis of the observations that chalcone 7 (MX781) and some activity, inhibit cell growth, and induce apoptosis in cancer cells, a new series of AdArs structurally related to 7 have been designed and synthesized. ...
- Knowledge Based Prediction of Ligand Binding Modes and Rational Inhibitor Design for Kinase Drug Discovery.
[作者:Ghose, Arup K.;Herbertz, Torsten;Pippin, Douglas A.;Salvino, Joseph M.;Mallamo, John P.;,期刊:Journal of Medicinal Chemistry, 页码:5149-5171 , 文章类型: 综述,,卷期:2008年51-17]
- A review describing the use of Protein Data Bank (PDB) entries specifically for kinase inhibitor drug discovery. Topics discussed include: the current state of structure-aided ligand design, kinase structure queries and...
- Discovery of Pyrrolopyridine-Pyridone Based Inhibitors of Met Kinase: Synthesis, X-ray Crystallographic Analysis, and Biological Activities.
[作者:Kim, Kyoung Soon;Zhang, Liping;Schmidt, Robert;Cai, Zhen-Wei;Wei, Donna;Williams, David K.;Lombardo, Louis J.;Trainor, George L.;Xie, Dianlin;Zhang, Yaquan;An, Yongmi;Sack, John S.;Tokarski, John S.;Darienzo, Celia;Kamath, Amrita;Marathe, Punit;Zhang, Yue,期刊:Journal of Medicinal Chemistry, 页码:5330-5341 , 文章类型: 研究论文,,卷期:2008年51-17]
- Conformationally constrained 2-pyridone analog 2 is a potent Met kinase inhibitor with an IC50 value of 1.8 nM. Further SAR of the 2-pyridone based inhibitors of Met kinase led to potent 4-pyridone and pyridine N-oxide ...
- Potent, Plasmodium-Selective Farnesyltransferase Inhibitors That Arrest the Growth of Malaria Parasites: Structure-Activity Relationships of Ethylenediamine-Analogue Scaffolds and Homology Model Validation.
[作者:Fletcher, Steven;Cummings, Christopher G.;Rivas, Kasey;Katt, William P.;Horney, Carrie;Buckner, Frederick S.;Chakrabarti, Debopam;Sebti, Said M.;Gelb, Michael H.;Van Voorhis, Wesley C.;Hamilton, Andrew D.;,期刊:Journal of Medicinal Chemistry, 页码:5176-5197 , 文章类型: 研究论文,,卷期:2008年51-17]
- New chemotherapeutics are urgently needed to combat malaria. We previously reported on a novel series of antimalarial, ethylenediamine-based inhibitors of protein farnesyltransferase (PFT). In the current study, we desi...
- The Alkaloid Conessine and Analogues as Potent Histamine H3 Receptor Antagonists.
[作者:Zhao, Chen;Sun, Minghua;Bennani, Youssef L.;Gopalakrishnan, Sujatha M.;Witte, David G.;Miller, Thomas R.;Krueger, Kathleen M.;Browman, Kaitlin E.;Thiffault, Christine;Wetter, Jill;Marsh, Kennan C.;Hancock, Arthur A.;Esbenshade, Timothy A.;Cowart, Marlon D,期刊:Journal of Medicinal Chemistry, 页码:5423-5430 , 文章类型: 研究论文,,卷期:2008年51-17]
- The naturally occurring alkaloid, conessine (6), was discovered to bind to histamine H3 receptors in a radioligand-based high-throughput screen. Conessine displayed high affinity at both rat and human H3 receptors (pKi ...
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