M1 aminopeptidases as drug targets: broad applications or therapeutic niche?
N Drinkwater, J Lee, W Yang, TR Malcolm… - The FEBS …, 2017 - Wiley Online Library
M1 aminopeptidase enzymes are a diverse family of metalloenzymes characterized by
conserved structure and reaction specificity. Excluding viruses, M1 aminopeptidases are …
conserved structure and reaction specificity. Excluding viruses, M1 aminopeptidases are …
Proteases as antimalarial targets: strategies for genetic, chemical, and therapeutic validation
E Deu - The FEBS journal, 2017 - Wiley Online Library
Malaria is a devastating parasitic disease affecting half of the world's population. The rapid
emergence of resistance against new antimalarial drugs, including artemisinin‐based …
emergence of resistance against new antimalarial drugs, including artemisinin‐based …
Direct arene C–H fluorination with 18F− via organic photoredox catalysis
Positron emission tomography (PET) plays key roles in drug discovery and development, as
well as medical imaging. However, there is a dearth of efficient and simple radiolabeling …
well as medical imaging. However, there is a dearth of efficient and simple radiolabeling …
Design, synthesis, conformational and molecular docking study of some novel acyl hydrazone based molecular hybrids as antimalarial and antimicrobial agents
Background Acyl hydrazones are an important class of heterocyclic compounds promising
pharmacological characteristics. Malaria is a life-threatening mosquito-borne blood disease …
pharmacological characteristics. Malaria is a life-threatening mosquito-borne blood disease …
[HTML][HTML] Chemoproteomics validates selective targeting of Plasmodium M1 alanyl aminopeptidase as an antimalarial strategy
New antimalarial drug candidates that act via novel mechanisms are urgently needed to
combat malaria drug resistance. Here, we describe the multi-omic chemical validation of …
combat malaria drug resistance. Here, we describe the multi-omic chemical validation of …
Identification of a potent and selective LAPTc inhibitor by RapidFire-Mass Spectrometry, with antichagasic activity
Background Chagas disease is caused by the protozoan parasite Trypanosoma cruzi and
leads to~ 10,000 deaths each year. Nifurtimox and benznidazole are the only two drugs …
leads to~ 10,000 deaths each year. Nifurtimox and benznidazole are the only two drugs …
Advances in drug discovery based on genomics, proteomics and bioinformatics in malaria
Malaria is one of the neglected infectious diseases, and drugs are the first line of action
taken against the onset of malaria as therapeutics. The drugs can be of either natural or …
taken against the onset of malaria as therapeutics. The drugs can be of either natural or …
Genetic and chemical validation of Plasmodium falciparum aminopeptidase PfA-M17 as a drug target in the hemoglobin digestion pathway
RCS Edgar, G Siddiqui, K Hjerrild, TR Malcolm… - Elife, 2022 - elifesciences.org
Plasmodium falciparum, the causative agent of malaria, remains a global health threat as
parasites continue to develop resistance to antimalarial drugs used throughout the world …
parasites continue to develop resistance to antimalarial drugs used throughout the world …
Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases
NB Vinh, N Drinkwater, TR Malcolm… - Journal of medicinal …, 2018 - ACS Publications
There is an urgent clinical need for antimalarial compounds that target malaria caused by
both Plasmodium falciparum and Plasmodium vivax. The M1 and M17 …
both Plasmodium falciparum and Plasmodium vivax. The M1 and M17 …
Biochemical and cellular characterisation of the Plasmodium falciparum M1 alanyl aminopeptidase (PfM1AAP) and M17 leucyl aminopeptidase (PfM17LAP)
The Plasmodium falciparum M1 alanyl aminopeptidase and M17 leucyl aminopeptidase, Pf
M1AAP and Pf M17LAP, are potential targets for novel anti-malarial drug development …
M1AAP and Pf M17LAP, are potential targets for novel anti-malarial drug development …