Targeted covalent inhibitors for drug design

TA Baillie - Angewandte Chemie International Edition, 2016 - Wiley Online Library
In contrast to the traditional mechanism of drug action that relies on the reversible,
noncovalent interaction of a ligand with its biological target, a targeted covalent inhibitor …

Catalytic properties and biomedical applications of cerium oxide nanoparticles

C Walkey, S Das, S Seal, J Erlichman… - Environmental …, 2015 - pubs.rsc.org
Cerium oxide nanoparticles (nanoceria) have shown promise as catalytic antioxidants in the
test tube, cell culture models and animal models of disease. However given the reactivity …

The cysteinome of protein kinases as a target in drug development

A Chaikuad, P Koch, SA Laufer… - Angewandte Chemie …, 2018 - Wiley Online Library
Drugs that function through covalent bond formation represent a considerable fraction of our
repository of effective medicines but safety concerns and the complexity of developing …

[HTML][HTML] Animal models of drug-induced liver injury

MR McGill, H Jaeschke - Biochimica et Biophysica Acta (BBA)-Molecular …, 2019 - Elsevier
Drug-induced liver injury (DILI) presents unique challenges for consumers, clinicians, and
regulators. It is the most common cause of acute liver failure in the US. It is also one of the …

An FDA/CDER perspective on nonclinical testing strategies: Classical toxicology approaches and new approach methodologies (NAMs)

AM Avila, I Bebenek, JA Bonzo, T Bourcier… - Regulatory Toxicology …, 2020 - Elsevier
Nonclinical testing of human pharmaceuticals is conducted to assess the safety of
compounds to be studied in human clinical trials and for marketing of new drugs. Although …

Drug‐induced liver injury: advances in mechanistic understanding that will inform risk management

M Mosedale, PB Watkins - Clinical Pharmacology & …, 2017 - Wiley Online Library
Drug‐induced liver injury (DILI) is a major public health problem. Intrinsic (dose‐dependent)
DILI associated with acetaminophen overdose is the number one cause of acute liver failure …

[HTML][HTML] Acetaminophen-induced liver injury: from animal models to humans

H Jaeschke, Y Xie, MR McGill - Journal of clinical and translational …, 2014 - ncbi.nlm.nih.gov
Drug-induced liver injury is an important clinical problem and a challenge for drug
development. Whereas progress in understanding rare and unpredictable (idiosyncratic) …

Idiosyncratic drug-induced liver injury: mechanistic and clinical challenges

A Jee, SC Sernoskie, J Uetrecht - International journal of molecular …, 2021 - mdpi.com
Idiosyncratic drug-induced liver injury (IDILI) remains a significant problem for patients and
drug development. The idiosyncratic nature of IDILI makes mechanistic studies difficult, and …

Applications of covalent chemistry in targeted protein degradation

D Lu, X Yu, H Lin, R Cheng, EY Monroy, X Qi… - Chemical Society …, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are
currently two exciting strategies in the fields of chemical biology and drug discovery …

[HTML][HTML] Dissecting the molecular pathophysiology of drug-induced liver injury

H Ye, LJ Nelson, MG Del Moral… - World journal of …, 2018 - ncbi.nlm.nih.gov
Drug-induced liver injury (DILI) has become a major topic in the field of Hepatology and
Gastroenterology. DILI can be clinically divided into three phenotypes: hepatocytic …