Asymmetric organocatalysis: an enabling technology for medicinal chemistry

B Han, XH He, YQ Liu, G He, C Peng… - Chemical Society Reviews, 2021 - pubs.rsc.org
The efficacy and synthetic versatility of asymmetric organocatalysis have contributed
enormously to the field of organic synthesis since the early 2000s. As asymmetric …

Azole fungicides–understanding resistance mechanisms in agricultural fungal pathogens

CL Price, JE Parker, AGS Warrilow… - Pest management …, 2015 - Wiley Online Library
Plant fungal pathogens can have devastating effects on a wide range of crops, including
cereals and fruit (such as wheat and grapes), causing losses in crop yield, which are costly …

Structural analyses of Candida albicans sterol 14α-demethylase complexed with azole drugs address the molecular basis of azole-mediated inhibition of fungal sterol …

TY Hargrove, L Friggeri, Z Wawrzak, A Qi… - Journal of Biological …, 2017 - ASBMB
With some advances in modern medicine (such as cancer chemotherapy, broad exposure to
antibiotics, and immunosuppression), the incidence of opportunistic fungal pathogens such …

Architecture of a single membrane spanning cytochrome P450 suggests constraints that orient the catalytic domain relative to a bilayer

BC Monk, TM Tomasiak, MV Keniya… - Proceedings of the …, 2014 - National Acad Sciences
Bitopic integral membrane proteins with a single transmembrane helix play diverse roles in
catalysis, cell signaling, and morphogenesis. Complete monospanning protein structures …

Fungal cytochrome P450 sterol 14α-demethylase (CYP51) and azole resistance in plant and human pathogens

R Becher, SGR Wirsel - Applied microbiology and biotechnology, 2012 - Springer
Azoles have been applied widely to combat pathogenic fungi in medicine and agriculture
and, consequently, loss of efficacy has occurred in populations of some species. Often, but …

Nitroheterocyclic compounds are more efficacious than CYP51 inhibitors against Trypanosoma cruzi: implications for Chagas disease drug discovery and …

CB Moraes, MA Giardini, H Kim, CH Franco… - Scientific reports, 2014 - nature.com
Advocacy for better drugs and access to treatment has boosted the interest in drug discovery
and development for Chagas disease, a chronic infection caused by the genetically …

Structure-functional characterization of cytochrome P450 sterol 14α-demethylase (CYP51B) from Aspergillus fumigatus and molecular basis for the development of …

TY Hargrove, Z Wawrzak, DC Lamb… - Journal of Biological …, 2015 - ASBMB
Aspergillus fumigatus is the opportunistic fungal pathogen that predominantly affects the
immunocompromised population and causes 600,000 deaths/year. The cytochrome P450 …

Design and optimization of highly-selective fungal CYP51 inhibitors

WJ Hoekstra, EP Garvey, WR Moore… - Bioorganic & medicinal …, 2014 - Elsevier
While the orally-active azoles such as voriconazole and itraconazole are effective antifungal
agents, they potently inhibit a broad range of off-target human cytochrome P450 enzymes …

Resistance to antifungals that target CYP51

JE Parker, AGS Warrilow, CL Price, JGL Mullins… - Journal of Chemical …, 2014 - Springer
Fungal diseases are an increasing global burden. Fungi are now recognised to kill more
people annually than malaria, whilst in agriculture, fungi threaten crop yields and food …

[HTML][HTML] Examination of multiple Trypanosoma cruzi targets in a new drug discovery approach for Chagas disease

I Beltran-Hortelano, V Alcolea, M Font… - Bioorganic & medicinal …, 2022 - Elsevier
Chagas disease (CD) is a centenarian neglected parasitosis caused by the protozoan
Trypanosoma cruzi (T. cruzi). Despite the continuous efforts of many organizations and …