[HTML][HTML] 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 …

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 …

Design of ultrasensitive probes for human neutrophil elastase through hybrid combinatorial substrate library profiling

P Kasperkiewicz, M Poreba, SJ Snipas… - Proceedings of the …, 2014 - pnas.org
The exploration of protease substrate specificity is generally restricted to naturally occurring
amino acids, limiting the degree of conformational space that can be surveyed. We …

Discovery of 8-hydroxy-2-quinoline carbaldehyde derivatives as inhibitors for M1 aminopeptidase of leishmania donovani

J Kumar, R Qureshi, P Jagruthi, M Arifuddin… - International Journal of …, 2024 - Elsevier
M1 aminopeptidase is a metallopeptidase that plays a vital role in protein catabolism and
has been identified as a validated drug target in various parasites; however, our …

Emerging challenges in the design of selective substrates, inhibitors and activity‐based probes for indistinguishable proteases

P Kasperkiewicz, M Poreba, K Groborz… - The FEBS …, 2017 - Wiley Online Library
Proteases are enzymes that hydrolyze the peptide bond of peptide substrates and proteins.
Despite significant progress in recent years, one of the greatest challenges in the design …

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 …

A multilayer network approach for guiding drug repositioning in neglected diseases

AJ Berenstein, MP Magariños… - PLoS neglected …, 2016 - journals.plos.org
Drug development for neglected diseases has been historically hampered due to lack of
market incentives. The advent of public domain resources containing chemical information …

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 …

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 …

Biochemical and cellular characterisation of the Plasmodium falciparum M1 alanyl aminopeptidase (PfM1AAP) and M17 leucyl aminopeptidase (PfM17LAP)

R Mathew, J Wunderlich, K Thivierge, K Cwiklinski… - Scientific reports, 2021 - nature.com
The Plasmodium falciparum M1 alanyl aminopeptidase and M17 leucyl aminopeptidase, Pf
M1AAP and Pf M17LAP, are potential targets for novel anti-malarial drug development …