Chemical Biology & Drug Design

Cover image for Chemical Biology & Drug Design

June 2011

Volume 77, Issue 6

Pages i–iii, 399–500

  1. Issue Information

    1. Top of page
    2. Issue Information
    3. Review
    4. Research Articles
    5. Research Letters
    6. Calendar of Events – June 2011
    1. Issue Information (pages i–iii)

      Article first published online: 13 MAY 2011 | DOI: 10.1111/j.1747-0285.2011.01126.x

  2. Review

    1. Top of page
    2. Issue Information
    3. Review
    4. Research Articles
    5. Research Letters
    6. Calendar of Events – June 2011
    1. You have free access to this content
      Insight into Amyloid Structure Using Chemical Probes (pages 399–411)

      Ashley A. Reinke and Jason E. Gestwicki

      Article first published online: 26 APR 2011 | DOI: 10.1111/j.1747-0285.2011.01110.x

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      Many neurodegenerative diseases are thought to be caused by highly ordered, protein aggregates termed amyloids. The heterogeneity of amyloids creates challenges in determining their structure by typical methods. Rather, small molecules have proven to be powerful probes. Moreover, next generation amyloid ligands promise to provide insight into how distinct amyloid conformers contribute to disease.

  3. Research Articles

    1. Top of page
    2. Issue Information
    3. Review
    4. Research Articles
    5. Research Letters
    6. Calendar of Events – June 2011
    1. You have full text access to this OnlineOpen article
      Applying Molecular Dynamics Simulations to Identify Rarely Sampled Ligand-bound Conformational States of Undecaprenyl Pyrophosphate Synthase, an Antibacterial Target (pages 412–420)

      William Sinko, César de Oliveira, Sarah Williams, Adam Van Wynsberghe, Jacob D. Durrant, Rong Cao, Eric Oldfield and J. Andrew McCammon

      Article first published online: 29 MAR 2011 | DOI: 10.1111/j.1747-0285.2011.01101.x

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      Crystallography, molecular dynamics simulations, and structural analysis reveal a rare “expanded pocket” state key to drug design for undecaprenyl pyrophosphate synthase, an attractive target for anti-microbial therapy

    2. You have free access to this content
      Normalization of Proliferation and Tight Junction Formation in Bladder Epithelial Cells from Patients with Interstitial Cystitis/Painful Bladder Syndrome by d-Proline and d-Pipecolic Acid Derivatives of Antiproliferative Factor (pages 421–430)

      Susan Keay, Piotr Kaczmarek, Chen-Ou Zhang, Kristopher Koch, Zoltan Szekely, Joseph J. Barchi Jr and Christopher Michejda

      Article first published online: 27 APR 2011 | DOI: 10.1111/j.1747-0285.2011.01108.x

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      Data are presented showing the inhibitory activity of two synthetic derivatives on the activity of an Antiproliferative Factor (APF) from patients with interstitial cystitis/painful bladder syndrome

    3. A New Generation of Potent Complement Inhibitors of the Compstatin Family (pages 431–440)

      Aliana López de Victoria, Ronald D. Gorham Jr., Meghan L. Bellows-Peterson, Jun Ling, David D. Lo, Christodoulos A. Floudas and Dimitrios Morikis

      Article first published online: 26 APR 2011 | DOI: 10.1111/j.1747-0285.2011.01111.x

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      Compstatin family peptides are potent inhibitors of the complement system and promising drug candidates against diseases involving under-regulated complement activation. The design of new compstatin variants is presented, together with SPR and ELISA characterisation.

    4. 2,3-Dihydro-1,2-Diphenyl-substituted 4H-Pyridinone Derivatives as New Anti Flaviviridae Inhibitors (pages 441–449)

      Antonella Peduto, Antonio Massa, Antonia Di Mola, Paolo de Caprariis, Paolo La Colla, Roberta Loddo, Sergio Altamura, Giovanni Maga and Rosanna Filosa

      Article first published online: 17 MAR 2011 | DOI: 10.1111/j.1747-0285.2011.01102.x

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      A series of 2,3-dihydro-4H-pyridinone derivatives has been prepared and evaluated for antiviral activity. In the antiviral screening, several compounds showed to be fairly active against viruses belonging to the Flaviviridae family. Among these, three compouds (4a cis, 4c cis and 6a) showed an interesting activity against YFV, BVDV and HCV with an EC50 in a low micromolar range

    5. Antiandrogenic activity of anthranilic acid ester derivatives as novel lead structures to inhibit prostate cancer cell proliferation (pages 450–459)

      Daniela Roell, Thomas W. Rösler, Stephanie Degen, Rudolf Matusch and Aria Baniahmad

      Article first published online: 27 APR 2011 | DOI: 10.1111/j.1747-0285.2011.01116.x

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      Prostate cancer is one of the most often diagnosed cancers in men and treated with androgen receptor (AR) antagonists. Derivatives of the natural compound anthranilic acid provide a novel scaffold for new AR antagonists that bind to the AR, inhibit the AR-mediated transactivation, the expression of the AR target gene PSA, and prostate cancer cell proliferation.

    6. Rottlerin Exhibits Antiangiogenic Effects In vitro (pages 460–470)

      Giuseppe Valacchi, Alessandra Pecorelli, Claudia Sticozzi, Claudia Torricelli, Michela Muscettola, Carlo Aldinucci and Emanuela Maioli

      Article first published online: 4 MAY 2011 | DOI: 10.1111/j.1747-0285.2011.01121.x

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      The downregulation of cyclin D-1 and ET-1, via NFκB inhibition, and the increase in NO, via Ca++/eNOS, are responsible for growth arrest. The loss of ET-1 and the production of NO contribute to the Rottlerin anti-hypertensive effect.

    7. coral Software: QSAR for Anticancer Agents (pages 471–476)

      Emilio Benfenati, Andrey A. Toropov, Alla P. Toropova, Alberto Manganaro and Rodolfo Gonella Diaza

      Article first published online: 4 MAY 2011 | DOI: 10.1111/j.1747-0285.2011.01117.x

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      The good correlation between experimental and calculated values of an endpoint for sub-training and calibration sets can be in fact a poor model

    8. Biologic Activity of a Dinuclear Pd(II)–Spermine Complex Toward Human Breast Cancer (pages 477–488)

      Sónia M. Fiuza, Jon Holy, Luis A. E. Batista de Carvalho and Maria P. M. Marques

      Article first published online: 1 APR 2011 | DOI: 10.1111/j.1747-0285.2011.01081.x

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      A spermine dinuclear palladium(II) complex (Pd2-Spm) was synthesized and tested towards two human breast cancer cell lines (MCF-7 and MDA-MB-231) as to its antiproliferative properties, and compared to the widely used drug cisplatin (cDDP). For optimized concentrations Pd2-Spm induced a rapid growth-inhibiting effect, as opposed to cDDP which seems to have a slower kinetics. The results evidence a possible distinct mechanism of action for these two Pt(II) complexes, which may explain their synergistic activity when co-administered.

  4. Research Letters

    1. Top of page
    2. Issue Information
    3. Review
    4. Research Articles
    5. Research Letters
    6. Calendar of Events – June 2011
    1. Antitubercular Activity of New Coumarins (pages 489–493)

      Silvia H. Cardoso, Milena B. Barreto, Maria C. S. Lourenço, Maria das Graças M. de O. Henriques, André L. P. Candéa, Carlos R. Kaiser and Marcus V. N. de Souza

      Article first published online: 19 APR 2011 | DOI: 10.1111/j.1747-0285.2011.01120.x

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      The present article describes a series of twenty-one coumarine derivatives, which were synthesized and evaluated against Mycobacterium tuberculosis.

    2. In Vitro Inhibition of Human Carbonic Anhydrase I and II Isozymes with Natural Phenolic Compounds (pages 494–499)

      Murat Şentürk, İlhami Gülçin, Şükrü Beydemir, Ö. İrfan Küfrevioğlu and Claudiu T. Supuran

      Article first published online: 25 MAR 2011 | DOI: 10.1111/j.1747-0285.2011.01104.x

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      The inhibition effects of some natural phenolic derivatives such as resveratrol, catechin, silymarin, dobutamin, and curcumin were determined on human cytosolic carbonic anhydrase isozymes I and II. These natural product phenols had marked inhibitory effects and were generally found as competitive inhibitors with 4-nitrophenyl acetate substrate

  5. Calendar of Events – June 2011

    1. Top of page
    2. Issue Information
    3. Review
    4. Research Articles
    5. Research Letters
    6. Calendar of Events – June 2011
    1. Calendar of Events – June 2011 (page 500)

      Article first published online: 13 MAY 2011 | DOI: 10.1111/j.1747-0285.2011.01131.x

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