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 …

Trends in research of antitrypanosomal agents among synthetic heterocycles

A Kryshchyshyn, D Kaminskyy, P Grellier… - European journal of …, 2014 - Elsevier
To date treatment of trypanosomiasis urgently requires new effective and non-toxic drugs.
The article covers some of the achievements in the search for new antitrypanosomal agents; …

The Trypanosoma brucei cAMP phosphodiesterases TbrPDEBl and TbrPDEB2: flagellar enzymes that are essential for parasite virulence

M Oberholzer, G Marti, M Baresic, S Kunz… - The FASEB …, 2007 - Wiley Online Library
Cyclic nucleotide specific phosphodiesterases (PDEs) are pivotal regulators of cellular
signaling. They are also important drug targets. Besides catalytic activity and substrate …

[图书][B] Cyclic nucleotide phosphodiesterases in health and disease

J Beavo, SH Francis, MD Houslay - 2007 - api.taylorfrancis.com
The establishment of a Gordon Research Conference devoted to cyclic nucleotide
phosphodiesterases has had an enormous impact on the field by facilitating collaborations …

Pharmacological Validation of Trypanosoma brucei Phosphodiesterases as Novel Drug Targets

HP de Koning, MK Gould, GJ Sterk… - Journal of infectious …, 2012 - academic.oup.com
The development of drugs for neglected infectious diseases often uses parasite-specific
enzymes as targets. We here demonstrate that parasite enzymes with highly conserved …

The ever unfolding story of cAMP signaling in trypanosomatids: vive la difference!

DNA Tagoe, TD Kalejaiye, HP Koning - Frontiers in pharmacology, 2015 - frontiersin.org
Kinetoplastids are unicellular, eukaryotic, flagellated protozoans containing the eponymous
kinetoplast. Within this order, the family of trypanosomatids are responsible for some of the …

Cyclic AMP effectors in African trypanosomes revealed by genome-scale RNA interference library screening for resistance to the phosphodiesterase inhibitor CpdA

MK Gould, S Bachmaier, JAM Ali… - Antimicrobial agents …, 2013 - Am Soc Microbiol
One of the most promising new targets for trypanocidal drugs to emerge in recent years is
the cyclic AMP (cAMP) phosphodiesterase (PDE) activity encoded by TbrPDEB1 and …

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 …

Cyclic-nucleotide signalling in protozoa

MK Gould, HP de Koning - FEMS microbiology reviews, 2011 - academic.oup.com
Compared with the impressive progress in understanding signal transduction pathways and
mechanisms in mammalian systems, advances in protozoan signalling processes, including …

New approaches for the identification of drug targets in protozoan parasites

J Müller, A Hemphill - International review of cell and molecular biology, 2013 - Elsevier
Antiparasitic chemotherapy is an important issue for drug development. Traditionally, novel
compounds with antiprotozoan activities have been identified by screening of compound …