Synthesis and Biological Evaluation of Colibactin Derivatives.
1/5 보강
Colibactin is a pseudo--symmetric gut microbiome metabolite that induces DNA interstrand cross-links and plays a causal role in colorectal cancer.
APA
Airan Y, Fedorova O, et al. (2026). Synthesis and Biological Evaluation of Colibactin Derivatives.. ACS chemical biology, 21(1), 26-36. https://doi.org/10.1021/acschembio.5c00639
MLA
Airan Y, et al.. "Synthesis and Biological Evaluation of Colibactin Derivatives.." ACS chemical biology, vol. 21, no. 1, 2026, pp. 26-36.
PMID
41419211 ↗
Abstract 한글 요약
Colibactin is a pseudo--symmetric gut microbiome metabolite that induces DNA interstrand cross-links and plays a causal role in colorectal cancer. Since efforts to isolate colibactin have not been successful, we developed colibactin 742 () as a stable colibactin mimetic. However, colibactin 742 () exists as a mixture of ring and chain isomers, which complicates analysis of its activity. We report here the discovery of colibactin 686 () as a superior colibactin mimetic. Colibactin 686 () is more potent than colibactin 742 () and recapitulates the bacterial genotoxic phenotype. Colibactin 686 () possesses a -symmetric structure, which will expedite its synthesis, and is incapable of ring-chain isomerization, which will simplify analysis of its biological activity. We additionally establish that colibactins do not passively diffuse into cells, and are substrates for monocarboxylate transporter pumps. These latter findings have implications for trafficking of natural colibactin, which remains poorly understood.
🏷️ 키워드 / MeSH 📖 같은 키워드 OA만
📖 전문 본문 읽기 PMC JATS · ~34 KB · 영문
Supplementary Material
Supplementary Material
Supplementary MaterialThe Supporting Information is available free of charge at https://pubs.acs.org/doi/10.1021/acschembio.5c00639.
Detailed experimental procedures and characterization data (1H and 13C NMR, IR, HRMS) for all new compounds. Detailed experimental methods for biological assays. (PDF)
Supplementary MaterialThe Supporting Information is available free of charge at https://pubs.acs.org/doi/10.1021/acschembio.5c00639.
Detailed experimental procedures and characterization data (1H and 13C NMR, IR, HRMS) for all new compounds. Detailed experimental methods for biological assays. (PDF)
출처: PubMed Central (JATS). 라이선스는 원 publisher 정책을 따릅니다 — 인용 시 원문을 표기해 주세요.
🏷️ 같은 키워드 · 무료전문 — 이 논문 MeSH/keyword 기반
- A Phase I Study of Hydroxychloroquine and Suba-Itraconazole in Men with Biochemical Relapse of Prostate Cancer (HITMAN-PC): Dose Escalation Results.
- Self-management of male urinary symptoms: qualitative findings from a primary care trial.
- Clinical and Liquid Biomarkers of 20-Year Prostate Cancer Risk in Men Aged 45 to 70 Years.
- Diagnostic accuracy of Ga-PSMA PET/CT versus multiparametric MRI for preoperative pelvic invasion in the patients with prostate cancer.
- Comprehensive analysis of androgen receptor splice variant target gene expression in prostate cancer.
- Clinical Presentation and Outcomes of Patients Undergoing Surgery for Thyroid Cancer.