Ernst Jucker – författare

Contents: V. Zingel, C. Leschke and W. Schunack: Developments in research on histamine (H1) receptor agonists / P.D. Hoeprich: Antifungal chemotherapy / G. de Stevens: The diversity of heterocyclic compounds and their biological activities / R.M. Schultz: Newer antifolate compounds in cancer therapy / P.K. Mehrotra, S. Batra and A.P. Bhadun: Non-steroidal agents for regulation of the menstrual cycle / A.K. Saxena and M. Saxena: Developments in anti-convulsant drugs

Nikolaus Seiler, Benoit Duranton and Francis Raul: The polyamine oxidase inactivator MDL 72527.- Zhi Hong and Craig E. Cameron: Pleiotropic mechanisms of ribavirin antiviral activities.- Jie Hong Hu and Charles Krieger: Protein phosphorylation networks in motor neuron death.- James O. Schenk: The functioning neuronal transporter for dopamine: kinetic mechanisms and effects of amphetamines, cocaine and methylphenidate.- Laszlo Prokai: Central nervous system effects of thyrotropin-releasing hormone and ist analogues: opportunities and perspectives for drug discovery and development.- David F. Horrobin: A new category of psychotropic drugs: neuroactive lipids as exemplified by ethyl eicosapentaenoate (E-E).- Suprabhat Ray, Reema Rastogi and Atul Kumar: Current status of estrogen receptors

Jay A. Glasel: Drugs, the human genome, and individual-based medicine.- Vera M. Kolb: Herbal medicine of Wisconsin Indians.- Paul L. Skatrud: The impact of multiple drug resistance (MDR) proteins on chemotherapy and drug discovery.- John W. Ford, Edward B. Stevens, J. Mark Treherne, Jeremy Packer and Mark Bushfield: Potassium channels: Gene family, therapeutic relevance, high-throughput screening technologies and drug discovery.- David T. Wong and Frank P. Bymaster: Dual serotonin and noradrenaline uptake inhibitor class of antidepressants - Potential for greater efficacy of just hype?.- Satya P. Gupta: Advances in QSAR studies of HIV-1 reverse transcriptase inhibitors

Due tothedevelopmentofdrugresistanceandotherlimitationsinthe treat- ment of AIDS patients with reverse transcriptase (RT) inhibitors like zidovu- dineandothers, itbecamenecessarytoexploreantiviralagentsactingontar- getsotherthan RT. Inthepastfewyears, hundredsofHIVproteaseinhibitoLs have been synthesized and tested. Among these protease inhibitors, saquinavir, ritonavir, indinavir and nelfinavir have been marketed during 1995-1997. In this review, emphasis is placed on the development of HIV protease inhibitors as antiviral agents against HIV, structure-activity rela- tionship (SAR) analysis ofsaquinavirand relatedcompounds, comparisonof four marketed HIV protease inhibitors, and future prospect in developing new anti-HIV drugs. 2 Introduction HIV protease inhibitors 3 HIV protease as a target for chemotherapy HIV protease was first suggested as a potential target for AIDS therapy by Kramer et a1. in 1986 [5]. HIV protease is a proteolytic enzyme responsible for cleaving large numbers of amino acid sequences. This enzyme regulates conversionoftheselargeaminoacid sequencesintobiologicallyactive struc- tural and functional protein products.Specifically, HIV protease is responsi- the enzymatic processing of the gagand gag-pol genes of HIV, which ble for encode for functional core proteins and viral enzymes (reverse transcriptase, ribonuclease H, integrase, and HIV protease). The polyproteins encoded by the gagand gag-pol genes undergo post-translational processing by HIV pro- tease to form functional protein products as the viral particles budding out from infected cells. Therefore, inhibition of HIV protease by a protease inhibitor results in the release ofimmature, noninfectious viral particles [4].

Volume 47 of "Progress in Drug Research" contains eight reviews and the various indexes which facilitate its use and establish the connection with the previous volumes. The articles in this volume deal with inotropic steroids, with chemokines and their involvement in a wide range of inflam­ matory diseases, with the subclassification and nomenclature of ul- and Uz-adrenoceptors, with Chinese traditional medicine, with drug targets in the molecular pathogenesis of asthma, with cytokines and their therapeutic application in immunosuppression and immunostimulation, with alter­ native medicine and with the potential use of calcium blockers in psy­ chiatry. These reviews and the quotations of original articles provide the reader with valuable information on several new developments in the world-wide search for new and better medicines. In 1959, when the Editor started this series of monographs, it was his intention to help disseminate informa­ tion on the vast and fast growing domain of drug research. Already at that time,it was not possible to follow the major individual publications in this field, and the reader was thereby provided with a tool to keep abreast of the latest developments and trends. This goal remained unchanged over the last 37 years, and I believe that the reviews in PDR are useful to the non-specialist who can obtain an overview of a particular field of drug research in a relatively short time.

Volume 47 of "Progress in Drug Research" contains eight reviews and the various indexes which facilitate its use and establish the connection with the previous volumes. The articles in this volume deal with inotropic steroids, with chemokines and their involvement in a wide range of inflam­ matory diseases, with the subclassification and nomenclature of ul- and Uz-adrenoceptors, with Chinese traditional medicine, with drug targets in the molecular pathogenesis of asthma, with cytokines and their therapeutic application in immunosuppression and immunostimulation, with alter­ native medicine and with the potential use of calcium blockers in psy­ chiatry. These reviews and the quotations of original articles provide the reader with valuable information on several new developments in the world-wide search for new and better medicines. In 1959, when the Editor started this series of monographs, it was his intention to help disseminate informa­ tion on the vast and fast growing domain of drug research. Already at that time,it was not possible to follow the major individual publications in this field, and the reader was thereby provided with a tool to keep abreast of the latest developments and trends. This goal remained unchanged over the last 37 years, and I believe that the reviews in PDR are useful to the non-specialist who can obtain an overview of a particular field of drug research in a relatively short time.