TY - CHAP
T1 - Targeting malaria protein kinases
AU - Cassiano, G.C.
AU - Tavella, T.A.
AU - Nascimento, M.N.
AU - Rodrigues, D.A.
AU - Cravo, P.V.L.
AU - Andrade, C.H.
AU - Costa, F.T.M.
N1 - Funding Information:
This work was supported by Funda??o de Amparo ? Pesquisa do Estado de S?o Paulo (FAPESP, Grant 2017/18611-7), Conselho Nacional de Desenvolvimento Cient?fico e Tecnol?gico (CNPq) and a joint grant of FCT of Portugal and FAPESP of Brazil, within the scope of the project ?Identification of new antimalarial treatments through a target-centered ?drug repositioning? approach? (ref PTDC/SAU-PAR/28459/2017). GCC and TAT were sponsored by a FAPESP fellowship (Grants 2015/20774-6 and 2019/27626-3, respectively). MNN was supported by a CAPES fellowship. CHA and FTMC are CNPq researcher fellows.
Funding Information:
This work was supported by Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP, Grant 2017/18611-7), Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) and a joint grant of FCT of Portugal and FAPESP of Brazil, within the scope of the project “Identification of new antimalarial treatments through a target-centered “drug repositioning” approach” (ref PTDC/SAU-PAR/28459/2017). GCC and TAT were sponsored by a FAPESP fellowship (Grants 2015/20774-6 and 2019/27626-3, respectively). MNN was supported by a CAPES fellowship. CHA and FTMC are CNPq researcher fellows.
Publisher Copyright:
© 2021 Elsevier Inc.
PY - 2021/1
Y1 - 2021/1
N2 - Malaria is one of the most impacting public health problems in tropical and subtropical areas of the globe, with approximately 200 million cases worldwide annually. In the absence of an effective vaccine, rapid treatment is vital for effective malaria control. However, parasite resistance to currently available drugs underscores the urgent need for identifying new antimalarial therapies with new mechanisms of action. Among potential drug targets for developing new antimalarial candidates, protein kinases are attractive. These enzymes catalyze the phosphorylation of several proteins, thereby regulating a variety of cellular processes and playing crucial roles in the development of all stages of the malaria parasite life cycle. Moreover, the large phylogenetic distance between Plasmodium species and its human host is reflected in marked differences in structure and function of malaria protein kinases between the homologs of both species, indicating that selectivity can be attained. In this review, we describe the functions of the different types of Plasmodium kinases and highlight the main recent advances in the discovery of kinase inhibitors as potential new antimalarial drug candidates.
AB - Malaria is one of the most impacting public health problems in tropical and subtropical areas of the globe, with approximately 200 million cases worldwide annually. In the absence of an effective vaccine, rapid treatment is vital for effective malaria control. However, parasite resistance to currently available drugs underscores the urgent need for identifying new antimalarial therapies with new mechanisms of action. Among potential drug targets for developing new antimalarial candidates, protein kinases are attractive. These enzymes catalyze the phosphorylation of several proteins, thereby regulating a variety of cellular processes and playing crucial roles in the development of all stages of the malaria parasite life cycle. Moreover, the large phylogenetic distance between Plasmodium species and its human host is reflected in marked differences in structure and function of malaria protein kinases between the homologs of both species, indicating that selectivity can be attained. In this review, we describe the functions of the different types of Plasmodium kinases and highlight the main recent advances in the discovery of kinase inhibitors as potential new antimalarial drug candidates.
UR - https://www.sciencedirect.com/science/article/pii/S1876162320300821?via%3Dihub
M3 - Chapter
VL - 124
T3 - Advances in Protein Chemistry and Structural Biology
SP - 225
EP - 274
BT - Advances in protein chemistry and structural biology
ER -
