Today's challenges to de-risk and predict drug safety in human “mind-the-gap”

RJ Weaver, JP Valentin - Toxicological Sciences, 2019 - academic.oup.com
Current gaps in drug safety sciences can result from the inability (1) to identify hazard across
multiple target organs,(2) to predict and risk assess with certainty against drug safety …

Mechanisms and in vitro models of drug-induced cholestasis

E Gijbels, V Vilas-Boas, N Deferm, L Devisscher… - Archives of …, 2019 - Springer
Cholestasis underlies one of the major manifestations of drug-induced liver injury. Drug-
induced cholestatic liver toxicity is a complex process, as it can be triggered by a variety of …

In-depth proteome analysis highlights HepaRG cells as a versatile cell system surrogate for primary human hepatocytes

G Tascher, A Burban, S Camus, M Plumel, S Chanon… - Cells, 2019 - mdpi.com
Of the hepatic cell lines developed for in vitro studies of hepatic functions as alternatives to
primary human hepatocytes, many have lost major liver-like functions, but not HepaRG cells …

Exploration of the molecular basis of forsythia fruit in the prevention and treatment of cholestatic liver injury through network pharmacology and molecular docking

K Fu, Y Li, S Dai, Y Li - Nutrients, 2023 - mdpi.com
Forsythia fruit, edible fruit of Forsythia suspensa (Thunb.) Vahl, which has been found to be
effective in treating cholestasis. However, its key component for alleviating cholestasis has …

Identification of flucloxacillin-haptenated HLA-B* 57: 01 ligands: evidence of antigen processing and presentation

JC Waddington, X Meng, PT Illing, A Tailor… - Toxicological …, 2020 - academic.oup.com
Flucloxacillin is a β-lactam antibiotic associated with a high incidence of drug-induced liver
reactions. Although expression of human leukocyte antigen (HLA)-B* 57: 01 increases …

Endoplasmic reticulum stress precedes oxidative stress in antibiotic-induced cholestasis and cytotoxicity in human hepatocytes

A Burban, A Sharanek, C Guguen-Guillouzo… - Free Radical Biology …, 2018 - Elsevier
Endoplasmic reticulum (ER) stress has been associated with various drug–induced liver
lesions but its participation in drug-induced cholestasis remains unclear. We first aimed at …

Specific roles of HSP27 S15 phosphorylation augmenting the nuclear function of HER2 to promote trastuzumab resistance

SY Hwang, SK Choi, SH Seo, H Jo, JH Shin, Y Na… - Cancers, 2020 - mdpi.com
Trastuzumab (TZMB) is widely used as first line therapy for breast cancer (BC) patients
overexpressing human epidermal growth factor receptor 2 (HER2). Despite its clinical …

In vitro prediction of drug-induced cholestatic liver injury: a challenge for the toxicologist

M Vinken - Archives of toxicology, 2018 - Springer
Cholestasis is derived from the Greek words chole meaning bile and stasis indicating halting
(Noor 2015), and denotes any situation of impaired bile secretion with concomitant …

Identification of flucloxacillin-modified hepatocellular proteins: implications in flucloxacillin-induced liver injury

SE Ali, JC Waddington, A Lister… - Toxicological …, 2023 - academic.oup.com
Flucloxacillin is a β-lactam antibiotic associated with a high incidence of drug-induced liver
injury. Although expression of HLA-B* 57: 01 is associated with increased susceptibility, little …

Mechanisms of drug-induced cholestasis

E Gijbels, M Vinken - Experimental Cholestasis Research, 2019 - Springer
Cholestasis can be defined as any situation of impaired bile secretion with concomitant
accumulation of bile acids in the liver or in the systemic circulation. A variety of factors may …