Leishmania Protein Kinases: Important Regulators of the Parasite Life Cycle and Molecular Targets for Treating Leishmaniasis

A Efstathiou, D Smirlis - Microorganisms, 2021 - mdpi.com
Leishmania is a protozoan parasite of the trypanosomatid family, causing a wide range of
diseases with different clinical manifestations including cutaneous, mucocutaneous and …

Recent progress in the development of indole-based compounds active against malaria, trypanosomiasis and leishmaniasis

PAF Pacheco, MMM Santos - Molecules, 2022 - mdpi.com
Human protozoan diseases represent a serious health problem worldwide, affecting mainly
people in social and economic vulnerability. These diseases have attracted little investment …

Water, water, everywhere… It's time to stop and think

MS Bodnarchuk - Drug Discovery Today, 2016 - Elsevier
Highlights•Six computational methods for water molecule placement and analysis reviewed
alongside relevant case studies.•Field is approaching maturity.•Adoption into mainstream …

Evaluating free energies of binding and conservation of crystallographic waters using SZMAP

AS Bayden, DT Moustakas… - Journal of chemical …, 2015 - ACS Publications
The SZMAP method computes binding free energies and the corresponding thermodynamic
components for water molecules in the binding site of a protein structure [SZMAP, 1.0. 0; …

Conditional gene deletion with DiCre demonstrates an essential role for CRK3 in Leishmania mexicana cell cycle regulation

SM Duncan, E Myburgh, C Philipon… - Molecular …, 2016 - Wiley Online Library
Leishmania mexicana has a large family of cyclin‐dependent kinases (CDKs) that reflect the
complex interplay between cell cycle and life cycle progression. Evidence from previous …

Chemoprevention of Leishmaniasis: In-vitro antiparasitic activity of dibenzalacetone, a synthetic curcumin analog leads to apoptotic cell death in Leishmania donovani

IS Chauhan, GS Rao, J Shankar, LKS Chauhan… - Parasitology …, 2018 - Elsevier
Curcumin is the major phenolic compound found in turmeric, a dry powder of rhizomes and
roots of the plant, Curcuma longa L., which is widely used as spice and food colorant around …

Molecular targets and pathways for the treatment of visceral leishmaniasis

V Jain, K Jain - Drug discovery today, 2018 - Elsevier
Highlights•Visceral leishmaniasis is a complicated infectious disease.•Emerging resistance
is one of the main complications in treatment visceral leishmaniasis.•A comprehensive …

From drug screening to target deconvolution: a target-based drug discovery pipeline using Leishmania casein kinase 1 isoform 2 to identify compounds with …

E Durieu, E Prina, O Leclercq, N Oumata… - Antimicrobial agents …, 2016 - Am Soc Microbiol
Existing therapies for leishmaniases present significant limitations, such as toxic side effects,
and are rendered inefficient by parasite resistance. It is of utmost importance to develop …

Indirubin derivatives: A patent review (2010–present)

N Gaboriaud-Kolar, K Vougogiannopoulou… - Expert opinion on …, 2015 - Taylor & Francis
Introduction: Indirubins are bisindole alkaloids naturally occurring in indigo-bearing plants or
in mollusks from the Muricidae family. They belong to the rather small family of indigoids …

Leishmania donovani 90 kD Heat Shock Protein – Impact of Phosphosites on Parasite Fitness, Infectivity and Casein Kinase Affinity

A Hombach-Barrigah, K Bartsch, D Smirlis… - Scientific reports, 2019 - nature.com
Leishmania parasites are thought to control protein activity at the post-translational level, eg
by protein phosphorylation. In the pathogenic amastigote, the mammalian stage of …