T. Middleton, H.B. Lim, D. Montgomery, T. Rockway, D. Liu, L. Klein, W. Qin, J.E. Harlan, W.M. Kati & A. Molla

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Toxoflavin analogs have antibacterial, antifungal and antitumor effects, and were potent inhibitors of Hepatitis C virus RNA-dependent RNA polymerase. Inhibition appeared to be via a redox-related mechanism, which may explain the toxicity of this class of compounds.

Y. Shimada & F. Yamamoto

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The Na⁺/H⁺ exchange inhibitor shown to protect the heart against ischemia/reperfusion injury in experimental studies, but only limited protection in prospective and randomized clinical studies. We review the studies on Na⁺/H⁺ exchanger inhibitors and discuss the reasons for the inconsistencies in clinical studies.

T. Tuccinardi, Maria G. Cascio, V. Di Marzo, C. Manera, G. Ortore, G. Saccomanni & A. Martinelli

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A structure-based virtual screening, using AUTODOCK and a previously published CB2 receptor model, allowed to find three compound showing K_i values of 7.8-8.0 μM from the Maybridge database.

H. Tsutsumi, H. Tamamura & N. Fujii

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CXCR4 has played important roles in several intractable diseases, including HIV infection, cancer cell metastasis, leukemia cell progression and rheumatoid arthritis. Thus, CXCR4 is thought to be an important therapeutic target in all of these diseases, and a lot of CXCR4 antagonists have been developed all over the world.

S.K. Das, C. Abbineni, K.V.L.N. Rao, J. Iqbal, R.K. Babu & R. Chakrabarti

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The design and synthesis of the dual PPARα/γ agonists with three different heterocycles are described. 5cb possesses a potent dual PPARα/γ agonist property. It significantly reversed diabetic hyperglycemia while improving overall lipid homeostasis in preclinical animal models.

M. Werle, H. Kolmar & A. Bernkop-Schnürch

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Cystine knot microproteins are promising novel scaffolds for the oral delivery of pharmacophoric sequences. These scaffolds should be stable towards membrane bound enzymes of the intestinal mucosa. The hypothesis that scaffolds with 37 amino acids (SE-ET-TP-020) are more susceptible towards MBE caused degradation in comparison to scaffolds with about 30 amino acids (SE-MC-TR-020) could be supported.

A.M. Fialho, T.K.D. Gupta & A.M. Chakrabarty

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Azurin from Pseudomonas aeruginosa: a well designed drug candidate. The drug industry primarily has relied on drugs that target a single gene or enzyme in a pathway involved in disease progression with the idea that such a drug will have minimum side effects and maximal efficacy. Recent observations, however, indicate that a drug that has multiple targets, thus exhibiting promiscuity, is often more efficacious. Recent studies with pathogenic bacteria demonstrate that such bacteria produce redox proteins that appear to act as weapons against various invaders of human body that cause diseases such as cancers, malaria or AIDS. The potential of finding such promiscuous bacterial proteins may lead in the future to an antibiotic-like industry targeted towards non-prokaryotic agents of human diseases.

J.D. Adams Jr. & L.K. Klaidman

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Sirtuins are enzymes that deacetylate proteins at the expense of NAD. The nuclear forms of sirtuins have generated an enormous amount of interest due to their putative role in lifespan extension.

J.E.Charris, G.M. Lobo, J.R. Camacho, R.E. Ferrer, A.R. Barazarte, J.N. Domínguez, N. Gamboa, J.R. Rodrigues & J.E. Angel

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A series of (E) 2-quinolinylmethyliden-5,7-dimethoxyindanones were prepared by a base catalyzed Claisen-Schmidt condensation of 5,7 dimethoxy-1-indanone with the appropriate 2-chloro-3-formylquinoline derivatives. Compounds were evaluated in vitro for their ability to inhibit β hematin formation and hemoglobin hydrolysis and in vivo for their efficacy in rodent Plasmodium berghei. Compounds emerging from the in vitro studies together with a good survival in a malaria murine model suggest that quinolinylmethyliden-5,7-dimetoxyindanones exert their antimalarial activity via inhibition of the hemoglobinolytic proteases.

M. Klink & Z. Sulowska

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The effect of pharmacologically active compounds that liberate nitric oxide on human neutrophils activities in vitro is described. SNP, SIN-1, DEA/NO decrease the pro-inflammatory action of activated neutrophils, without reducing their ability to kill bacteria.

A.G. Tempone, M.S.C. Melhem, F.O. Prado, G. Motoie, R.M. Hiramoto, M.M. Antoniazzi, C.F.B. Haddad & C. Jared

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The antiparasitic and antifungal activities of nine amphibian skin secretions were studied in different in vitro models. Seven secretions presented a considerable antiprotozoan activity and one showed promising results against Candida sp. These results can be the basis for the development of new drugs, especially for neglected parasitic diseases.

M. Postema, F.J. ten Cate, G. Schmitz, N. de Jong & A. van Wamel

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Antibubbles consist of a liquid core encapsulated by a gas shell. They might be suitable carriers for ultrasound-assisted drug delivery. The creation of an antibubble with the aid of ultrasound has been demonstrated with high-speed photography.

N. Pachulski & J. Ulrich

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Tablet-like bodies are produced from a water based suspension by a sol-gel, a freeze-casting and a drying process without the standard compression. The dissolution influencing pores in these bodies correspond to the negative images of the former ice crystals and therefore can be regulated by the process conditions.