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Structure-Based Drug Design to Overcome Drug Resistance: Challenges and Opportunities

[ Vol. 20 , Issue. 5 ]


Rafaela S. Ferreira and Adriano D. Andricopulo   Pages 687 - 693 ( 7 )


Drug resistance is a common concern for the development of novel antiviral, antimicrobial and anticancer therapies. To overcome this problem, several strategies have been developed, many of which involving the theme of this review, the use of structure-based drug design (SBDD) approaches. These include the successful design of new compounds that target resistant mutant proteins, as well as the development of drugs that target multiple proteins involved in specific biochemical pathways. Finally, drug resistance can also be considered in the early stages of drug discovery, through the use of strategies to delay the development of resistance. The purpose of this brief review is to underline the usefulness of SBDD approaches based on case studies, highlighting present challenges and opportunities in drug design.


Drug discovery, drug resistance, structure-based drug design, therapeutic agents.


, Laboratorio de Química Medicinal e Computacional, Instituto de Física de Sao Carlos, Universidade de Sao Paulo, Av. Trabalhador Sao-carlense, 400, Sao Carlos - Sao Paulo - Brasil - CEP 13566-590.

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