Development and evolution of therapies targeted to the estrogen receptor for the treatment and prevention of breast cancer

VC Jordan, AMH Brodie - Steroids, 2007 - Elsevier
… (aromatase inhibitors) … inhibitor 4-hydroxyandrostenedione (known as formestane) pioneered
the development of a range of oral aromatase inhibitors that are either suicide inhibitors

Cytochrome p450 retinoic acid 4-hydroxylase inhibitors: potential agents for cancer therapy

VCO Njar - Mini reviews in medicinal chemistry, 2002 - ingentaconnect.com
… levels of endogenous ATRA by inhibiting the cytochrome P450-dependent ATRA-4-hydroxylase
enzyme(s) responsible for ATRA metabolism. These inhibitors are also referred to as …

Improving and repurposing biocatalysts via directed evolution

CA Denard, H Ren, H Zhao - Current opinion in chemical biology, 2015 - Elsevier
hydroxylation activity (only ω-1, ω-2 and ω-3 products), but several of the evolved variants
catalyzed the terminal hydroxylation … and minimal product inhibition of the evolved enzyme …

Protein hydroxylation by hypoxia-inducible factor (HIF) hydroxylases: unique or ubiquitous?

MJ Strowitzki, EP Cummins, CT Taylor - Cells, 2019 - mdpi.com
… is important in order to fully elucidate the pharmacology of hydroxylase inhibitors (PHI). …
Because of the absolute reliance on a continuous supply of O 2 , animals have evolved a …

The evolving landscape in the development of isocitrate dehydrogenase mutant inhibitors

J Chen, J Yang, P Cao - Mini reviews in medicinal chemistry, 2016 - ingentaconnect.com
… describes known inhibitors with … evolving landscape of IDH mutant inhibitors provides
us an outlook on the discovery of novel, safer, and more effective cancer treatment strategies

Biocatalytic strategies for the asymmetric synthesis of α-hydroxy ketones

P Hoyos, JV Sinisterra, F Molinari… - Accounts of chemical …, 2010 - ACS Publications
… are found in some antidepressants, in selective inhibitors of amyloid-β protein production
(for Alzheimer’s disease treatment), in farnesyl transferase inhibitors Kurasoin A and B, in …

Directed evolution of oxygenases: screening systems, success stories and challenges

K Lan Tee, U Schwaneberg - Combinatorial chemistry & high …, 2007 - ingentaconnect.com
… industrial use of oxygenases inhibition by molar substrate/… Examples are a fluorometric assay
for steroid hydroxylation [… and lack of universal directed evolution strategies. We hope that …

Drug strategies targeting CYP51 in neglected tropical diseases

JY Choi, LM Podust, WR Roush - Chemical Reviews, 2014 - ACS Publications
… Research Institute collection of vitamin D hydroxylase inhibitors singled out two structurally
related compounds, 55 and 56 (VNF), as strong inhibitors of CYP51 catalytic function (Figure …

From nonsteroidal aromatase inhibitors to multifunctional drug candidates: classic and innovative strategies for the treatment of breast cancer

S Gobbi, A Cavalli, A Bisi… - Current topics in …, 2008 - ingentaconnect.com
… particular hydroxylation of the 7-position on the A ring could enhance the inhibitory potency,
whereas a methoxy group in the same position would be less favorable, and hydroxylation

Novel therapeutic strategies targeting HIV integrase

PK Quashie, RD Sloan, MA Wainberg - BMC medicine, 2012 - Springer
inhibition of viral integration are being explored in numerous preclinical studies, which include
inhibition … the clinical development of HIV integrase inhibitors, the development of antiviral …