Neglected tropical diseases (NTD) are parasitic infections that affect the poorest people in less developed countries. For this reason, they did not and still do not have high visibility in Western societies. The name neglected diseases reflects also the failure of pharmaceutical companies to invest in research and development of new medicines. In fact, most of the drugs still used to treat these diseases were developed in colonial times. These are often expensive, have variable efficacy, toxic side effects and require long courses of administration. Furthermore, several of them are also becoming ineffective because of increasing parasite resistance. This gloomy outlook has changed during the past decade as a result of important advances in Kinetoplastida (comprising the genera Trypanosoma and Leishmania) basic research. In 2005, the genome sequences of the ‘Tritryp’ (T. brucei, T. cruzi and L. major) and in 2007 those of two other species of Leishmania (L. infantum and L. braziliensis) were completed, eliminating many of the hurdles to performing state-of-the-art drug discovery research. The vast amount of available information has made a more comprehensive and accurate identification and validation of novel possible drug targets. However, new licensed therapies have not yet resulted from genome-derived investigations, and trypanosomiases and leishmaniases, even in the post-genomic era, may remain incurable and often fatal. We have proposed the multi-target drug design strategy as a means to overcome the challenges of current drug discovery in NTD.[1, 2] This approach is based on the design of single chemical entities able to simultaneously modulate multiple targets. Although these concepts emerged less than 10 years ago, multi-target drugs are already a reality in the therapy of complex diseases. In NTD, multi-target agents have an added value with respect to the single-target ones: the onset of drug resistance might be significantly delayed

From target-based to multi-target-based drug design approaches for neglected tropical diseases

BOLOGNESI, MARIA LAURA
2010

Abstract

Neglected tropical diseases (NTD) are parasitic infections that affect the poorest people in less developed countries. For this reason, they did not and still do not have high visibility in Western societies. The name neglected diseases reflects also the failure of pharmaceutical companies to invest in research and development of new medicines. In fact, most of the drugs still used to treat these diseases were developed in colonial times. These are often expensive, have variable efficacy, toxic side effects and require long courses of administration. Furthermore, several of them are also becoming ineffective because of increasing parasite resistance. This gloomy outlook has changed during the past decade as a result of important advances in Kinetoplastida (comprising the genera Trypanosoma and Leishmania) basic research. In 2005, the genome sequences of the ‘Tritryp’ (T. brucei, T. cruzi and L. major) and in 2007 those of two other species of Leishmania (L. infantum and L. braziliensis) were completed, eliminating many of the hurdles to performing state-of-the-art drug discovery research. The vast amount of available information has made a more comprehensive and accurate identification and validation of novel possible drug targets. However, new licensed therapies have not yet resulted from genome-derived investigations, and trypanosomiases and leishmaniases, even in the post-genomic era, may remain incurable and often fatal. We have proposed the multi-target drug design strategy as a means to overcome the challenges of current drug discovery in NTD.[1, 2] This approach is based on the design of single chemical entities able to simultaneously modulate multiple targets. Although these concepts emerged less than 10 years ago, multi-target drugs are already a reality in the therapy of complex diseases. In NTD, multi-target agents have an added value with respect to the single-target ones: the onset of drug resistance might be significantly delayed
Program and Abstracts Proteine 2010
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O-11
ML Bolognesi
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11585/93441
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