Structure-Guided Development of Antifungal Protein Farnesyltransferase Inhibitors and DNA Polymerase Engineering

Y Wang - 2021 - search.proquest.com
Eukaryotic human pathogens present a serious threat to global health, causing hundreds of
millions of infections with high death rate each year. Fungi and protozoa are two major …

Crystal structures of the fungal pathogen Aspergillus fumigatus protein farnesyltransferase complexed with substrates and inhibitors reveal features for antifungal …

MF Mabanglo, MA Hast, NB Lubock… - Protein …, 2014 - Wiley Online Library
Species of the fungal genus Aspergillus are significant human and agricultural pathogens
that are often refractory to existing antifungal treatments. Protein farnesyltransferase (FTase) …

[HTML][HTML] Structures of Cryptococcus neoformans protein farnesyltransferase reveal strategies for developing inhibitors that target fungal pathogens

MA Hast, CB Nichols, SM Armstrong, SM Kelly… - Journal of Biological …, 2011 - ASBMB
Cryptococcus neoformans is a fungal pathogen that causes life-threatening infections in
immunocompromised individuals, including AIDS patients and transplant recipients. Few …

Structure-guided discovery of potent antifungals that prevent Ras signaling by inhibiting protein farnesyltransferase

Y Wang, F Xu, CB Nichols, Y Shi… - Journal of medicinal …, 2022 - ACS Publications
Infections by fungal pathogens are difficult to treat due to a paucity of antifungals and
emerging resistances. Next-generation antifungals therefore are needed urgently. We have …

Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: structure− activity relationships of ethylenediamine-analogue …

S Fletcher, CG Cummings, K Rivas… - Journal of medicinal …, 2008 - ACS Publications
New chemotherapeutics are urgently needed to combat malaria. We previously reported on
a novel series of antimalarial, ethylenediamine-based inhibitors of protein …

Advantages and challenges of phenotypic screens: the identification of two novel antifungal geranylgeranyltransferase I inhibitors

V Pries, S Cotesta, R Riedl, T Aust… - Journal of …, 2016 - journals.sagepub.com
Phenotypic screens are effective starting points to identify compounds with desirable
activities. To find novel antifungals, we conducted a phenotypic screen in Saccharomyces …

[HTML][HTML] Bacteria are new targets for inhibitors of human farnesyltransferase

L Weber, A Hagemann, J Kaltenhäuser… - Frontiers in …, 2021 - frontiersin.org
Farnesyltransferase inhibitors (FTIs) are focus for the treatment of several diseases,
particularly in the field of cancer therapy. Their potential, however, goes even further, as a …

[PDF][PDF] Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase

MA Hast, S Fletcher, CG Cummings, EE Pusateri… - Chemistry & biology, 2009 - cell.com
Protein farnesyltransferase (FTase) catalyzes an essential posttranslational lipid
modification of more than 60 proteins involved in intracellular signal transduction networks …

Protein farnesyltransferase inhibitors exhibit potent antimalarial activity

L Nallan, KD Bauer, P Bendale, K Rivas… - Journal of medicinal …, 2005 - ACS Publications
New therapeutics to combat malaria are desperately needed. Here we show that the
enzyme protein farnesyltransferase (PFT) from the malaria parasite Plasmodium falciparum …

Structurally Simple, Potent, Plasmodium Selective Farnesyltransferase Inhibitors That Arrest the Growth of Malaria Parasites

MP Glenn, SY Chang, C Hornéy, K Rivas… - Journal of medicinal …, 2006 - ACS Publications
Third world nations require immediate access to inexpensive therapeutics to counter the
high mortality inflicted by malaria. Here, we report a new class of antimalarial protein …