ABC transporters are essential for cellular physiology. Humans have 48 ABC genes
organized into seven distinct families. Of these genes, 44 (in five distinct families) encode for …

Background Drug-induced liver injury (DILI) is the most challenging and thought-provoking
liver problem for hepatologists owing to unregulated medication usage in medical practices …

Peptides and proteins are not orally bioavailable in mammals, although a few peptides are
intestinally absorbed in small amounts. Polypeptides are generally too large and polar to …

Lipids, phospholipids and cholesterol in particular, are the predominant components of the
plasma membrane, wherein multidrug efflux transporters of the ATP-binding cassette (ABC) …

ABCG2 is a constitutively expressed ATP-binding cassette (ABC) transporter that protects
many tissues against xenobiotic molecules. Its activity affects the pharmacokinetics of …

Drug discovery for difficult targets that have large and flat binding sites is often better suited
to compounds beyond the “rule of 5”(bRo5). However, such compounds carry higher …

Transporters in proximal renal tubules contribute to the disposition of numerous drugs.
Furthermore, the molecular mechanisms of tubular secretion have been progressively …

Angiotensin‐I‐converting enzyme (ACE) inhibitory peptides are able to inhibit the activity of
ACE, which is the key enzymatic factor mediating systemic hypertension. ACE‐inhibitory …

Glucuronidation and sulfation are the most typical phase II metabolic reactions of drugs. The
resulting glucuronide and sulfate conjugates are generally considered inactive and safe …

The kidney is a vital organ for the elimination of therapeutic drugs and their metabolites.
Renal drug transporters, which are primarily located in the renal proximal tubules, play an …