Current and Future Strategies for Improving Drug Discovery Efficiency

Njogu, Peter Mbugua; Chibale, Kelly

doi:10.1002/9781118819586.ch11

Cited by 2 publications

(1 citation statement)

References 165 publications

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“…It is the contention of the authors that CADD approaches represent the best opportunity so far for enhancing productivity pipelines in tropical infectious diseases. The easy availability of many diverse chemical libraries in pharmaceutical companies, virtual discovery organizations, and academic institutions and the increased genomic information facilitative of computational predictions make CADD a very attractive venture for improved and efficient drug discovery for tropical infections …”

Section: Conclusion and Future Outlookmentioning

confidence: 99%

Computer-Aided Drug Discovery Approaches against the Tropical Infectious Diseases Malaria, Tuberculosis, Trypanosomiasis, and Leishmaniasis

et al. 2015

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Despite the tremendous improvement in overall global health heralded by the adoption of the Millennium Declaration in the year 2000, tropical infections remain a major health problem in the developing world. Recent estimates indicate that the major tropical infectious diseases, namely, malaria, tuberculosis, trypanosomiasis, and leishmaniasis, account for more than 2.2 million deaths and a loss of approximately 85 million disability-adjusted life years annually. The crucial role of chemotherapy in curtailing the deleterious health and economic impacts of these infections has invigorated the search for new drugs against tropical infectious diseases. The research efforts have involved increased application of computational technologies in mainstream drug discovery programs at the hit identification, hit-to-lead, and lead optimization stages. This review highlights various computer-aided drug discovery approaches that have been utilized in efforts to identify novel antimalarial, antitubercular, antitrypanosomal, and antileishmanial agents. The focus is largely on developments over the past 5 years (2010-2014).

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Section: Conclusion and Future Outlookmentioning

confidence: 99%

Computer-Aided Drug Discovery Approaches against the Tropical Infectious Diseases Malaria, Tuberculosis, Trypanosomiasis, and Leishmaniasis

et al. 2015

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A drug repositioning success: The repositioned therapeutic applications and mechanisms of action of thalidomide

Amare

Meharie

Belayneh

2020

J Oncol Pharm Pract

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Background Thalidomide is the most teratogenic human medicine ever marketed and was associated with birth defects in approximately 10,000 children in the 1960s. The pharmacological effects of thalidomide are attributed to its anti-angiogenic, anti-inflammatory and modulatory effect on cytokines principally tumor necrosis factor-α, while the teratogenic effects are linked to two molecular targets, namely cereblon and tubulin. Teratogenicity is the gravest adverse effect of thalidomide depending on the dose and time of exposure. Nonetheless, with System for Thalidomide Education and Prescribing Safety program, the possibility of teratogenicity can be completely avoided. The sensitive period during pregnancy for thalidomide teratogenicity in humans is approximately 20-34 days after fertilization. Methods Relevant articles were identified from Google scholar and PubMed (MEDLINE) using different search strategies. Conclusion Clinical trials showed that thalidomide has been found effective in the treatment of advanced renal cancer, esophageal cancer, chemotherapy refractory endometrial cancer and pancreatic cancer, which can suggest its future therapeutic potential in cancer treatment. Thalidomide is also used in the treatment of inflammatory skin disorders and has shown promising effect in the treatment of autoimmune disorders and inflammatory bowel disease. Despite thalidomide being a renowned teratogen and neurotoxin, it has been successfully repositioned and FDA approved for the treatment of erythema nodosum leprosum and multiple myeloma under strict control.

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Current and Future Strategies for Improving Drug Discovery Efficiency

Cited by 2 publications

References 165 publications

Computer-Aided Drug Discovery Approaches against the Tropical Infectious Diseases Malaria, Tuberculosis, Trypanosomiasis, and Leishmaniasis

Computer-Aided Drug Discovery Approaches against the Tropical Infectious Diseases Malaria, Tuberculosis, Trypanosomiasis, and Leishmaniasis

A drug repositioning success: The repositioned therapeutic applications and mechanisms of action of thalidomide

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