Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need
The WHO recognizes human African trypanosomiasis, Chagas disease and the
leishmaniases as neglected tropical diseases. These diseases are caused by parasitic …
leishmaniases as neglected tropical diseases. These diseases are caused by parasitic …
The therapeutic journey of pyridazinone
Pyridazinones have drawn a substantial attention within the field of research analysis and
development. The moiety is a subject matter of intensive research because of its wide …
development. The moiety is a subject matter of intensive research because of its wide …
Identification of potent and orally efficacious phosphodiesterase inhibitors in Cryptosporidium parvum-infected immunocompromised male mice
J Ajiboye, JE Teixeira, M Gasonoo, EB Mattice… - Nature …, 2024 - nature.com
Cryptosporidium parvum and C. hominis are parasites that cause life-threatening diarrhea in
children and immunocompromised people. There is only one approved treatment that is …
children and immunocompromised people. There is only one approved treatment that is …
Unpacking the Pathogen Box—an open source tool for fighting neglected tropical disease
CGL Veale - ChemMedChem, 2019 - Wiley Online Library
Abstract The Pathogen Box is a 400‐strong collection of drug‐like compounds, selected for
their potential against several of the world's most important neglected tropical diseases …
their potential against several of the world's most important neglected tropical diseases …
Flagellar cAMP signaling controls trypanosome progression through host tissues
S Shaw, SF DeMarco, R Rehmann, T Wenzler… - Nature …, 2019 - nature.com
The unicellular parasite Trypanosoma brucei is transmitted between mammals by tsetse
flies. Following the discovery that flagellar phosphodiesterase PDEB1 is required for …
flies. Following the discovery that flagellar phosphodiesterase PDEB1 is required for …
Nucleoside analogue activators of cyclic AMP-independent protein kinase A of Trypanosoma
S Bachmaier, Y Volpato Santos, S Kramer… - Nature …, 2019 - nature.com
Protein kinase A (PKA), the main effector of cAMP in eukaryotes, is a paradigm for the
mechanisms of ligand-dependent and allosteric regulation in signalling. Here we report the …
mechanisms of ligand-dependent and allosteric regulation in signalling. Here we report the …
Phenotypic, chemical and functional characterization of cyclic nucleotide phosphodiesterase 4 (PDE4) as a potential anthelmintic drug target
Background Reliance on just one drug to treat the prevalent tropical disease,
schistosomiasis, spurs the search for new drugs and drug targets. Inhibitors of human cyclic …
schistosomiasis, spurs the search for new drugs and drug targets. Inhibitors of human cyclic …
Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal …
AR Blaazer, AK Singh, E De Heuvel… - Journal of medicinal …, 2018 - ACS Publications
Several trypanosomatid cyclic nucleotide phosphodiesterases (PDEs) possess a unique,
parasite-specific cavity near the ligand-binding region that is referred to as the P-pocket …
parasite-specific cavity near the ligand-binding region that is referred to as the P-pocket …
[HTML][HTML] 3-nitroimidazo [1, 2-b] pyridazine as a novel scaffold for antiparasitics with sub-nanomolar anti-Giardia lamblia activity
Y Zheng, J Müller, S Kunz, M Siderius, L Maes… - International Journal for …, 2022 - Elsevier
As there is a continuous need for novel anti-infectives, the present study aimed to fuse two
modes of action into a novel 3-nitroimidazo [1, 2-b] pyridazine scaffold to improve …
modes of action into a novel 3-nitroimidazo [1, 2-b] pyridazine scaffold to improve …
Structural Investigations of Phthalazinone Derivatives as Allosteric Inhibitors of Human DNA Methyltransferase 3A
I Hernandez, E Ward, TRR Pettus… - ACS Medicinal …, 2024 - ACS Publications
The development of new therapeutics targeting enzymes involved in epigenetic pathways
such as histone modification and DNA methylation has received a lot of attention …
such as histone modification and DNA methylation has received a lot of attention …