Inhibitory drugs

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  • The era of pharmacology, the science concerned with the understanding of drug action, began only about 150 years ago when Rudolf Buchheim established the first pharmacological laboratory in Dorpat (now, Tartu, Estonia). Since then, pharmacology has always been a lively discipline with “open borders”, reaching out not only to other life sciences such as physiology, biochemistry, cell biology and clinical medicine, but also to chemistry and physics.

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  • Introduction: An organophosphorus nerve agent VX (O-ethyl S-2-diisopropylaminoethyl methylphosphonothiolate, Figure 2.1) shows potent inhibitory action on acetylcholinesterase; its development, production, stockpiling and use are being prohibited by the CWC international treaty as a chemical weapon together with those of sarin and soman. In addition, even material compounds for VX synthesis are being also controlled strictly. In the world history, there had been no records on the use of VX in any international dispute.

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  • Drugs Acting on Motor Systems spinal disorders. Benzodiazepines enhance the effectiveness of the inhibitory transmitter GABA (p. 226) at GABAA receptors. Baclofen stimulates GABAB receptors. !2-Adrenoceptor agonists such as clonidine and tizanidine probably act presynaptically to inhibit release of excitatory amino acid transmitters. The convulsant toxins, tetanus toxin (cause of wound tetanus) and strychnine diminish the efficacy of interneuronal synaptic inhibition mediated by the amino acid glycine (A).

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  • Chronic consumption For benefits of chronic alcohol consumption, see page 187. Central nervous system. The development of dependence on alcohol appears to involve alterations in central nervous system neurotransmission. The acute effect of alcohol is to block NMDA receptors for which the normal agonist is glutamate, the main excitatory transmitter in the brain. Chronic exposure increases the number of NMDA receptors and also 'L type' calcium channels, while the action of the (inhibitory) GABA neurotransmitter is reduced.

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  • Despite my many years of research and teaching in platelet physiology and pharmacology at the University of Minnesota, I am often confronted with conflicting opinions as to the relevance of nonnucleated platelets in human health and disease. It is fascinating to think that how cells with no apparent nucleus, have such a towering impact on concepts, dealing with often overlapping physiological (i.e. hemostasis, wound healing, etc.) and pathophysiological (i.e. thrombosis, stroke, atherosclerosis, wound healing, diabetes, inflammation and cancer) components.

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  • Many physiologically important proproteins, pathogenic bacterial exo-toxins and viral envelope glycoproteins are activated by the proprotein con-vertase furin, which makes furin inhibitor a hot target for basic research and drug design. Although synthetic and bioengineered inhibitors of furin have been well characterized, its endogenous inhibitor has not been directly purified from mammalian tissues to date.

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  • Addiction, increasingly perceived as a heterogeneous brain disorder, is one of the most peculiar psychiatric pathologies in that its management involves various, often non-overlapping, resources from the biological, psychological, medical, economical, social, and legal realms. Despite extensive efforts from the players of these various fields, to date there are no reliably effective treatments of addiction.

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  • The K103N substitution is a frequently observed HIV-1 RT mutation in patients who do not respond to combinationtherapy. The drugs Efavirenz, MSC194 and PNU142721 belong to the recent generation of NNRTIs characterized by an improved resistance profile to the most common single point mutations within HIV-1 RT, including the K103N mutation. In the present study we present structural observations from Efavirenz in complex with wild-type protein and the K103N mutant and PNU142721 and MSC194 in complex with the K103N mutant.

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  • Highly active, small-molecule furin inhibitors are attractive drug candidates to fend off bacterial exotoxins and viral infection. Based on the 22-residue, active Lys fragment of the mung bean trypsin inhibitor, a series of furin inhibitors were designed and synthesized, and their inhibitory activity towards furin and kexin was evaluated using enzyme kinetic analysis.

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  • HIV-1 protease is an important target for treatment of AIDS, and efficient drugs have been developed. However, the resistance and negative side effects of the current drugs has necessitated the development of new compounds with different binding patterns. In this study, nine C-terminally duplicated HIV-1 protease inhibitors were cocrystallised with the enzyme, the crystal structures analysed at 1.8–2.3 A˚ resolution, and the inhibitory activity of the compounds characterized inorder toevaluate the effects of the individual modifications. ...

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  • The Tet repressor protein (TetR) regulates transcription of a family of tetracycline (tc) resistance determinants in Gram-negative bacteria. The resistance protein TetA, a membrane-spanning H + -[tcÆM]+ antiporter, must be sen-sitively regulated because its expression is harmful in the absence of tc, yet it has to be expressed before the drugs’ concentration reaches cytoplasmic levels inhibitory for protein synthesis.

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