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 …

Non-canonical amino acids in analyses of protease structure and function

P Goettig, NG Koch, N Budisa - International Journal of Molecular …, 2023 - mdpi.com
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 …

Asymmetric enzymatic synthesis of allylic amines: a sigmatropic rearrangement strategy

CK Prier, TK Hyster, CC Farwell… - Angewandte Chemie …, 2016 - Wiley Online Library
Sigmatropic rearrangements, while rare in biology, offer opportunities for the efficient and
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 …

Fingerprinting the Substrate Specificity of M1 and M17 Aminopeptidases of Human Malaria, Plasmodium falciparum

M Poreba, S McGowan, TS Skinner-Adams… - PLoS …, 2012 - journals.plos.org
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 …

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 …

[HTML][HTML] Chemoproteomics validates selective targeting of Plasmodium M1 alanyl aminopeptidase as an antimalarial strategy

D Creek, C Giannangelo, M Challis, G Siddiqui… - eLife, 2024 - elifesciences.org
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 …

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 …

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 …

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 …