Drug discovery and development for neglected parasitic diseases

AR Renslo, JH McKerrow - Nature chemical biology, 2006 - nature.com
Diseases caused by tropical parasites affect hundreds of millions of people worldwide but
have been largely neglected for drug development because they affect poor people in poor …

Keeping uracil out of DNA: physiological role, structure and catalytic mechanism of dUTPases

BG Vértessy, J Tóth - Accounts of chemical research, 2009 - ACS Publications
The thymine− uracil exchange constitutes one of the major chemical differences between
DNA and RNA. Although these two bases form the same Watson− Crick base pairs with …

Purine and pyrimidine pathways as targets in Plasmodium falciparum

M Belen Cassera, Y Zhang… - Current topics in …, 2011 - ingentaconnect.com
Malaria is a leading cause of morbidity and mortality in the tropics. Chemotherapeutic and
vector control strategies have been applied for more than a century but have not been …

Structure-based virtual screening approach reveals natural multi-target compounds for the development of antimalarial drugs to combat drug resistance

B Naik, N Gupta, P Godara, V Srivastava… - Journal of …, 2024 - Taylor & Francis
Compared to the previous year, there has been an increase of nearly 2 million malaria
cases in 2021. The emergence of drug-resistant strains of Plasmodium falciparum, the most …

1, 2, 3-Triazole-containing uracil derivatives with excellent pharmacokinetics as a novel class of potent human deoxyuridine triphosphatase inhibitors

H Miyakoshi, S Miyahara, T Yokogawa… - Journal of medicinal …, 2012 - ACS Publications
Deoxyuridine triphosphatase (dUTPase) has emerged as a potential target for drug
development as a 5-fluorouracil-based combination chemotherapy. We describe the design …

Identification of inhibitors for putative malaria drug targets among novel antimalarial compounds

GJ Crowther, AJ Napuli, JH Gilligan, K Gagaring… - Molecular and …, 2011 - Elsevier
The efficacy of most marketed antimalarial drugs has been compromised by evolution of
parasite resistance, underscoring an urgent need to find new drugs with new mechanisms of …

Development of a target identification approach using native mass spectrometry

M Liu, WC Van Voorhis, RJ Quinn - Scientific reports, 2021 - nature.com
A key step in the development of new pharmaceutical drugs is the identification of the
molecular target and distinguishing this from all other gene products that respond indirectly …

Crystal structure of African swine fever virus dUTPase reveals a potential drug target

C Li, Y Chai, H Song, C Weng, J Qi, Y Sun, GF Gao - MBio, 2019 - Am Soc Microbiol
ABSTRACT E165R, a highly specific dUTP nucleotidohydrolase (dUTPase) encoded by the
African swine fever virus (ASFV) genome, is required for productive replication of ASFV in …

Antimalarial Properties of Isoquinoline Derivative from Streptomyces hygroscopicus subsp. Hygroscopicus: An In Silico Approach

RYB Nugraha, IFD Faratisha… - BioMed Research …, 2020 - Wiley Online Library
Malaria is one of the life‐threatening diseases in the world. The spread of resistance to
antimalarial drugs is a major challenge, and resistance to artemisinin has been reported in …

The dUTPase Enzyme Is Essential in Mycobacterium smegmatis

I Pecsi, R Hirmondo, AC Brown, A Lopata, T Parish… - PloS one, 2012 - journals.plos.org
Thymidine biosynthesis is essential in all cells. Inhibitors of the enzymes involved in this
pathway (eg methotrexate) are thus frequently used as cytostatics. Due to its pivotal role in …