Ask about this productRelated genes to: UGT1A1 Blocking Peptide
- Gene:
- UGT1A1 NIH gene
- Name:
- UDP glucuronosyltransferase family 1 member A1
- Previous symbol:
- UGT1, GNT1
- Synonyms:
- UGT1A
- Chromosome:
- 2q37.1
- Locus Type:
- complex locus constituent
- Date approved:
- 1989-02-13
- Date modifiied:
- 2019-04-23
Related products to: UGT1A1 Blocking Peptide
Related articles to: UGT1A1 Blocking Peptide
- Bilirubin encephalopathy (BE) is a severe neurological complication of neonatal hyperbilirubinemia, but the molecular mechanisms underlying bilirubin-induced brain injury remain unclear. We investigated whether UDP-glucuronosyltransferase 1A1 (UGT1A1) regulates neuronal ferroptosis in BE and whether this process is controlled by ten-eleven translocation methylcytosine dioxygenase 1 (TET1)-mediated demethylation. - Source: PubMed
Publication date: 2026/09/21
Yang XiaolingDuan QingmingaiLei BeibeiYan Jun - Cholestasis is characterized by impaired bile flow and intracellular bile acid accumulation, leading to progressive liver injury driven by oxidative stress, inflammation, and hepatocellular apoptosis. Disruption of canalicular bile acid transport, particularly BSEP dysfunction, represents a central initiating event in cholestatic liver damage. α-Naphthyl isothiocyanate (ANIT) is widely used to model intrahepatic cholestasis; however, the mechanisms underlying selenium-mediated protection remain incompletely defined. - Source: PubMed
Publication date: 2026/09/28
Bolat İsmailÖzdemir SelçukÇomakli SelimSağlam Yavuz SelimTekin SametÇinar BurakBolat MerveOrhan BetülSağsöz Mustafa ErdemOkkay Ufuk - St. John's Wort (SJW; ) is widely used for mild-to-moderate depression and is known to induce certain cytochrome P450 enzymes (notably CYP3A4, with reported effects on CYP2C9 and CYP2C19) and intestinal P-glycoprotein, but its effects on UDP-glucuronosyltransferases (UGTs), the principal phase-II drug-metabolizing enzymes, remain largely uncharacterized. Using recombinant human UGTs with 4-methylumbelliferone as the probe substrate, we characterized inhibition by the two major SJW constituents, hypericin and hyperforin, across eleven isoforms, and combined AlphaFold2-based molecular docking, molecular dynamics, and MM/PBSA analyses with FDA 2020 static-model extrapolation (IVIVE) to predict drug-drug interaction (DDI) risk. Both compounds were broad-spectrum UGT inhibitors, with hyperforin the most potent (UGT1A1 = 1.46 μM; UGT2B7 = 6.70 μM). On the clinically critical UGT1A1, hyperforin and hypericin occupied the aglycone pocket through two structurally distinct binding modes that both produced noncompetitive kinetics. Under a complete-dissolution assumption, IVIVE flagged hyperforin as a high-risk intestinal UGT inhibitor ( = 69.49 for UGT1A1 and 15.93 for UGT2B7, far above the FDA threshold of 11); however, incorporating hyperforin's poor (∼2%) dissolution and acid instability lowered the corrected to ∼2.0-2.9 (UGT1A1) and ∼1.2-1.4 (UGT2B7), indicating a potential rather than definitive intestinal interaction whose magnitude depends on the SJW formulation. These findings provide mechanistic and quantitative support for reported clinical SJW-drug interactions and highlight intestinal glucuronidation as a previously underappreciated SJW-mediated DDI pathway. - Source: PubMed
Publication date: 2026/09/10
Chen JinqianZhang YanlongZhao XixiCui YatingXu TongLiu LingxiaZhao ZhenyuLi Xichuan - A woman in her 50 s presented with invasive mucinous adenocarcinoma of unknown primary origin 18 years after undergoing radical hysterectomy and two-dimensional chemoradiotherapy for FIGO stage IB1 cervical cancer. Over two decades, the patient developed chronic radiation-induced complications, including pelvic abscesses, enterocutaneous fistulas, and progressive renal impairment. These chronic changes formed a 'pelvic cocoon' that masked the development of a secondary malignancy. Diagnosis was achieved through random biopsies of the fistula site, whilst repeated endoscopies were negative. Management required complex decision-making, resulting in the selection of a modified 'folinic acid, fluorouracil, and irinotecan' regimen due to severe renal dysfunction (creatinine clearance < 20 mL/min) and UGT1A1*28/*28 homozygosity, adhering to stringent European safety standards. This case illustrates delayed recognition of secondary malignancy arising from chronic inflammatory and post-treatment changes, emphasising the need for a high index of clinical suspicion and individualised therapeutic strategies in long-term cancer survivors. - Source: PubMed
Publication date: 2026/08/26
Motomura YusukeAoki YuFunakoshi ShinsukeOhashi Toshio - TROP2-directed antibody-drug conjugates (trophoblast antigen 2-directed ADCs) are becoming increasingly integrated into breast cancer treatment across multiple disease settings. Their expanding use makes a detailed understanding of agent-specific toxicities, underlying mechanisms and practical management strategies increasingly important. - Source: PubMed
Publication date: 2026/09/18
Malagutti BiancaMalvezzi GiuliaZagami Paola