Site-specific proteasome inhibitors
AF Kisselev - Biomolecules, 2021 - mdpi.com
Proteasome is a multi-subunit protein degradation machine, which plays a key role in the
maintenance of protein homeostasis and, through degradation of regulatory proteins, in the …
maintenance of protein homeostasis and, through degradation of regulatory proteins, in the …
Experimental structure based drug design (SBDD) applications for anti‐leishmanial drugs: A paradigm shift?
M Marín, M López, L Gallego‐Yerga… - Medicinal Research …, 2024 - Wiley Online Library
Leishmaniasis is a group of neglected tropical diseases caused by at least 20 species of
Leishmania protozoa, which are spread by the bite of infected sandflies. There are three …
Leishmania protozoa, which are spread by the bite of infected sandflies. There are three …
Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors
MG Thomas, K McGonagle, P Rowland… - Journal of Medicinal …, 2023 - ACS Publications
There is an urgent need for new treatments for Chagas disease, a parasitic infection which
mostly impacts South and Central America. We previously reported on the discovery of …
mostly impacts South and Central America. We previously reported on the discovery of …
Small molecules as kinetoplastid specific proteasome inhibitors for leishmaniasis: A patent review from 1998 to 2021
Introduction Leishmaniasis is a neglected tropical infectious disease. The available limited
therapeutic options for leishmaniasis are inadequate due to their poor pharmacokinetic …
therapeutic options for leishmaniasis are inadequate due to their poor pharmacokinetic …
Design, synthesis, and optimization of macrocyclic peptides as species-selective antimalaria proteasome inhibitors
With over 200 million cases and close to half a million deaths each year, malaria is a threat
to global health, particularly in developing countries. Plasmodium falciparum, the parasite …
to global health, particularly in developing countries. Plasmodium falciparum, the parasite …
Structures revealing mechanisms of resistance and collateral sensitivity of Plasmodium falciparum to proteasome inhibitors
The proteasome of the malaria parasite Plasmodium falciparum (Pf20S) is an advantageous
drug target because its inhibition kills P. falciparum in multiple stages of its life cycle and …
drug target because its inhibition kills P. falciparum in multiple stages of its life cycle and …
Targeting proteasomes in cancer and infectious disease: a parallel strategy to treat malignancies and microbes
JJ Ignatz-Hoover, EV Murphy… - Frontiers in Cellular and …, 2022 - frontiersin.org
Essential core pathways of cellular biology are preserved throughout evolution, highlighting
the importance of these pathways for both bacteria and human cancer cells alike. Cell …
the importance of these pathways for both bacteria and human cancer cells alike. Cell …
Discovery of highly selective inhibitors of the human constitutive proteasome β5c chymotryptic subunit
We describe our discovery and development of potent and highly selective inhibitors of
human constitutive proteasome chymotryptic activity (β5c). Structure–activity relationship …
human constitutive proteasome chymotryptic activity (β5c). Structure–activity relationship …
Susceptibilities of Ugandan Plasmodium falciparum isolates to proteasome inhibitors
S Garg, O Kreutzfeld, S Chelebieva… - Antimicrobial agents …, 2022 - Am Soc Microbiol
The proteasome is a promising target for antimalarial chemotherapy. We assessed ex vivo
susceptibilities of fresh Plasmodium falciparum isolates from eastern Uganda to seven …
susceptibilities of fresh Plasmodium falciparum isolates from eastern Uganda to seven …
The AAA+ ATPase p97 as a novel parasite and tuberculosis drug target
G Kobakhidze, A Sethi, S Valimehr, SA Ralph… - Trends in …, 2022 - cell.com
The multifunctional AAA+ ATPase p97 is an unfoldase/segregase involved in various
cellular processes and present in all kingdoms of life. In mammals and yeast, p97 functions …
cellular processes and present in all kingdoms of life. In mammals and yeast, p97 functions …