Role of CAR and PXR in xenobiotic sensing and metabolism
Introduction: The xenobiotic detoxification system, which protects the human body from external
chemicals, comprises drug-metabolizing enzymes and transporters whose expressions …
chemicals, comprises drug-metabolizing enzymes and transporters whose expressions …
Novel pyrrolopyrimidine-based α-helix mimetics: cell-permeable inhibitors of protein− protein interactions
There is considerable interest in developing non-peptidic, small-molecule α-helix mimetics
to disrupt α-helix-mediated protein−protein interactions. Herein, we report the design of a …
to disrupt α-helix-mediated protein−protein interactions. Herein, we report the design of a …
[HTML][HTML] SPA70 is a potent antagonist of human pregnane X receptor
Many drugs bind to and activate human pregnane X receptor (hPXR) to upregulate drug-metabolizing
enzymes, resulting in decreased drug efficacy and increased resistance. This …
enzymes, resulting in decreased drug efficacy and increased resistance. This …
Small-molecule modulators of PXR and CAR
Two nuclear receptors, the pregnane X receptor (PXR) and the constitutive androstane receptor
(CAR), participate in the xenobiotic detoxification system by regulating the expression of …
(CAR), participate in the xenobiotic detoxification system by regulating the expression of …
[HTML][HTML] Blocking an N-terminal acetylation–dependent protein interaction inhibits an E3 ligase
N-terminal acetylation is an abundant modification influencing protein functions. Because ∼80%
of mammalian cytosolic proteins are N-terminally acetylated, this modification is …
of mammalian cytosolic proteins are N-terminally acetylated, this modification is …
Pregnane X receptor and drug-induced liver injury
Introduction: The liver plays a central role in transforming and clearing foreign substances.
The continuous exposure of the liver to xenobiotics sometimes leads to impaired liver function…
The continuous exposure of the liver to xenobiotics sometimes leads to impaired liver function…
Piperine activates human pregnane X receptor to induce the expression of cytochrome P450 3A4 and multidrug resistance protein 1
Activation of the pregnane X receptor (PXR) and subsequently its target genes, including those
encoding drug transporters and metabolizing enzymes, while playing substantial roles in …
encoding drug transporters and metabolizing enzymes, while playing substantial roles in …
A current structural perspective on PXR and CAR in drug metabolism
Introduction: Pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) are
two members of the nuclear receptor superfamily that play major roles in the expression of …
two members of the nuclear receptor superfamily that play major roles in the expression of …
E3 ligase autoinhibition by C-degron mimicry maintains C-degron substrate fidelity
…, CT Gee, R Kalathur, J Li, N Purser, A Nourse, SC Chai… - Molecular Cell, 2023 - cell.com
E3 ligase recruitment of proteins containing terminal destabilizing motifs (degrons) is
emerging as a major form of regulation. How those E3s discriminate bona fide substrates from …
emerging as a major form of regulation. How those E3s discriminate bona fide substrates from …
One protein, two enzymes revisited: a structural entropy switch interconverts the two isoforms of acireductone dioxygenase
T Ju, RB Goldsmith, SC Chai, MJ Maroney… - Journal of molecular …, 2006 - Elsevier
Acireductone dioxygenase (ARD) catalyzes different reactions between O 2 and 1,2-dihydroxy-3-oxo-5-(methylthio)pent-1-ene
(acireductone) depending upon the metal bound in the …
(acireductone) depending upon the metal bound in the …