Skip to main content
. 2020 Dec 15;25(24):5949. doi: 10.3390/molecules25245949

Table 13.

Plasmodial kinases targeted by inhibiting compounds described in this review.

Protein Role of Protein—Consequence(s) of Inhibition 1 Development Stage of the Most Advanced Compound(s) Studies Reviewed
CDPK1 Egress and invasion processes regulator—Inhibition of asexual blood-stage growth and gametogenesis, reduced mosquito infection Hit to lead [23,24,28,29,30,31,32,33]
CDPK4 Exflagellation regulator—Reduced mosquito infection Lead optimization [33,36,37,38,39]
CK Transformation of choline into phosphocholine Hit discovery—Target validation needed [41,45,46,47]
CK2 Serine/threonine kinase, possibly phosphorylating many proteins during asexual blood-stage Hit discovery—In vitro activity to be determined [50]
CLK1 Phosphorylation of spliceosomes proteins—Inhibition of asexual and sexual blood-stage growth Hit discovery—In vitro activity to be determined [53,55]
CLK3 Phosphorylation of spliceosomes proteins—All-stage activity Hit to lead [53,54,56]
PanK Transformation of pantothenate into 4′-phosphopantothenate Hit discovery [58,59,60]
DPCK Transformation of dephospho-coenzyme A into coenzyme A Hit discovery [61]
FKk8 Not defined Hit discovery [64,65]
GK Transformation of (deoxy) guanosine-monophosphate into (deoxy) guanosine-diphosphate Hit discovery—Target validation needed [46]
GSK3 Not defined Hit to lead [70,71]
HK Transformation of glucose into glucose-6-phosphate Hit discovery [74,75]
MAP2 Involved in many key cellular processes—Inhibition of asexual blood-stage and exflagellation Hit discovery—Target validation needed [77]
MRK Regulation of gene expression and DNA replication Hit discovery [79,80,81]
NEK1 Regulation of cell division processes Hit discovery [83,84]
PI4K Transformation of phosphatidyl-inositol into phosphatidyl-inositol 4 phosphate—All-stage activity Phase II clinical trial [85,87,89,90,91,92]
PK5 Cyclin-dependent like kinase, possibly regulating cell division Hit discovery [95]
PK6 Cyclin-dependent like kinase, role not defined Hit discovery - In vitro activity to be determined [33]
PK7 Orphan kinase, role not defined—Inhibition of asexual blood-stage and reduced mosquito infection Hit to lead [101,102,103]
PK9 Orphan kinase, role unclear, able to phosphorylate PfUBC13—Deregulation of asexual hepatic stage growth Hit discovery [100]
PKG Serine/threonine kinase—All-stage activity Hit to lead [109,110,112,113,114,116,117,118]
TMK Transformation of thymidine monophosphate into thymidine diphosphate Hit to lead [121,122,123]

1 When not specified, each of these proteins is assumed to at least inhibit asexual blood-stage growth.