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Biochemical characterization and chemical validation of Leishmania MAP Kinase-3 as a potential drug target
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Biochemical characterization and chemical validation of Leishmania MAP Kinase-3 as a potential drug target
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Journal Article
Biochemical characterization and chemical validation of Leishmania MAP Kinase-3 as a potential drug target
2019
Overview
Protozoan parasites of the
Leishmania
genus have evolved unique signaling pathways that can sense various environmental changes and trigger stage differentiation for survival and host infectivity. MAP kinase (MAPK) plays a critical role in various cellular activities like cell differentiation, proliferation, stress regulation, and apoptosis. The
Leishmania donovani
MAPK3 (
Ld
MAPK3) is involved in the regulation of flagella length and hence plays an important role in disease transmission. Here, we reported the gene cloning, protein expression, biochemical characterizations, inhibition studies and cell proliferation assay of
Ld
MAPK3. The recombinant purified
Ld
MAPK3 enzyme obeys the Michaelis-Menten equation with K
m
and V
max
of
Ld
MAPK3 was found to be 20.23 nM and 38.77 ± 0.71 nmoles ATP consumed/mg
Ld
MAPK3/min respectively. The maximum kinase activity of
Ld
MAPK3 was recorded at 35 °C and pH 7. The
in-vitro
inhibition studies with two natural inhibitors genistein (GEN) and chrysin (CHY) was evaluated against
Ld
MAPK3. The K
i
value for GEN and CHY were found to be 3.76 ± 0.28 µM and K
i
= 8.75 ± 0.11 µM respectively. The IC
50
value for the compounds, GEN and CHY against
L. donovani
promastigotes were calculated as 9.9 µg/mL and 13 µg/mL respectively. Our study, therefore, reports
Ld
MAPK3 as a new target for therapeutic approach against leishmaniasis.
Publisher
Nature Publishing Group UK,Nature Publishing Group
Subject
/ 631/45
/ 631/92
/ Cloning
/ Flagella
/ Humanities and Social Sciences
/ Kinases
/ Leishmania donovani - drug effects
/ Leishmania donovani - enzymology
/ Mitogen-Activated Protein Kinase 3 - antagonists & inhibitors
/ Mitogen-Activated Protein Kinase 3 - chemistry
/ Mitogen-Activated Protein Kinase 3 - metabolism
/ Protein Kinase Inhibitors - pharmacology
/ Protozoa
/ Science
