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 …
Non-canonical amino acids in analyses of protease structure and function
All known organisms encode 20 canonical amino acids by base triplets in the genetic code.
The cellular translational machinery produces proteins consisting mainly of these amino …
The cellular translational machinery produces proteins consisting mainly of these amino …
Asymmetric enzymatic synthesis of allylic amines: a sigmatropic rearrangement strategy
Sigmatropic rearrangements, while rare in biology, offer opportunities for the efficient and
selective synthesis of complex chemical motifs. A “P411” serine‐ligated variant of …
selective synthesis of complex chemical motifs. A “P411” serine‐ligated variant of …
Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions
N Drinkwater, NB Vinh, SN Mistry, RS Bamert… - European journal of …, 2016 - Elsevier
Malaria remains a global health problem, and though international efforts for treatment and
eradication have made some headway, the emergence of drug-resistant parasites threatens …
eradication have made some headway, the emergence of drug-resistant parasites threatens …
Fingerprinting the Substrate Specificity of M1 and M17 Aminopeptidases of Human Malaria, Plasmodium falciparum
Background Plasmodium falciparum, the causative agent of human malaria, expresses two
aminopeptidases, Pf M1AAP and Pf M17LAP, critical to generating a free amino acid pool …
aminopeptidases, Pf M1AAP and Pf M17LAP, critical to generating a free amino acid pool …
Two-Pronged Attack: Dual Inhibition of Plasmodium falciparum M1 and M17 Metalloaminopeptidases by a Novel Series of Hydroxamic Acid-Based Inhibitors
SN Mistry, N Drinkwater, C Ruggeri… - Journal of medicinal …, 2014 - ACS Publications
Plasmodium parasites, the causative agents of malaria, have developed resistance to most
of our current antimalarial therapies, including artemisinin combination therapies which are …
of our current antimalarial therapies, including artemisinin combination therapies which are …
[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 …
Targeting the active sites of malarial proteases for antimalarial drug discovery: approaches, progress and challenges
KK Roy - International Journal of Antimicrobial Agents, 2017 - Elsevier
Malaria is an infectious disease causing vast mortality and morbidity worldwide. Although
antimalarial drugs are effective in several parts of the world, there is a serious threat to …
antimalarial drugs are effective in several parts of the world, there is a serious threat to …
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 …
Synthesis and Structure–Activity Relationships of Phosphonic Arginine Mimetics as Inhibitors of the M1 and M17 Aminopeptidases from Plasmodium falciparum
K Kannan Sivaraman, A Paiardini… - Journal of Medicinal …, 2013 - ACS Publications
The malaria parasite Plasmodium falciparum employs two metallo-aminopeptidases, Pf A-
M1 and Pf A-M17, which are essential for parasite survival. Compounds that inhibit the …
M1 and Pf A-M17, which are essential for parasite survival. Compounds that inhibit the …