Skip to content
DraconiticResearch
Search Sources API
194,161 studies31 sourcesUpdated 55 min ago
Peer-reviewedCC BY-NC-ND 4.0ACS Omega

FBMN-Guided Discovery of Cyanogrisides from Mutant Strain CRM005 and Structural Diversification

  • Yukang Gao1
  • Yun Luo1
  • Qingyun Wen1
  • Linmeng Chen1
  • Guoliang Zhu2
  • Peng Fu1,3
  • Peipei Liu1
  • Weiming Zhu1,3
  1. 1Ocean University of China , , ,
  2. 2East China University of Science and Technology , , ,
  3. 3Qingdao Marine Science and Technology Center , , ,
Read full textPDFDOICite

Abstract

Through genome mining and metabolomic analysis of the mutant strain CRM005, combined with feature-based molecular networking (FBMN) deduplication, five novel natural cyanogrisides (1–5) were selectively isolated and characterized, alongside six previously reported analogs (6–11). Antiproliferative assays demonstrated that cyanogriside K (8) exhibited potent and selective cytotoxicity against HCT-116 cells, with an IC50 value of 0.70 μM. In an effort to maximize the reutilization of natural product resources, the major aglycone caerulomycin H (11) was utilized to develop a glycosylation system, affording a small panel of nine glycosylated derivatives (13–21). Subsequent antiproliferative evaluations facilitated a preliminary structure–activity relationship analysis focused on variations in the glycosyl groups. Notably, the synthetic compound 13 displayed submicromolar-level activity against the human glioblastoma cell line SF-126 (IC50 0.49 μM), surpassing the activity of doxorubicin (IC50 0.78 μM). These findings position compound 13 as a promising cytotoxic hit derived from a small semisynthetic library and offer preliminary insight into how glycosyl modification impacts antiproliferative activity.

Related

  1. Multiobjective V H H discovery through integrated high-throughput screening and AlphaFold3-guided structural prioritization
    Max D. Overath, Suthimon Thumtecho, Esperanza Rivera-de-Torre +12
    Science AdvancesPeer-reviewedCC BYMedical imaging & radiologyCrossref
  2. Molecular Mechanisms and Therapeutic Advances in KRAS G12C‐Mutant Non‐Small Cell Lung Cancer: Toward Mechanism‐Guided Longitudinal Management
    Haiying Wang, Hanxiao Chen, Sheng Li +1
    Cancer innovationPeer-reviewedCC BYFull textGeneral medicineEurope PMC
  3. DNA-Encoded Library-Guided Discovery of a First-in-Class Molecular Glue of the NOS1AP-SCRIB Complex in Alzheimer's Disease Patient-Derived Neurons
    B. Kaur, A. Abdo, S. Cho +1
    bioRxivPreprintAll rights reservedFull textPharmacology & toxicologybioRxiv
  4. Genome Mining-Guided Discovery of Polyketide-Tropolone Hybrids Reveals Their Biosynthetic Logic and Antitumor Activity
    Changzheng Wu, Yanfu Wang, Daixi Liu +7
    ChemRxivPreprintCC BY-NC-NDFull textPharmacology & toxicologyChemRxiv
  5. Antibody discovery from phage libraries lacking clear target-cell-selective enrichment through NGS-guided search space definition and cloning-free binding screening
    Koichi Wada, Takeharu Watanabe, Yu Nishida +1
    Scientific ReportsPeer-reviewedCC BY 4.0Full textMedical imaging & radiologyCrossref

Cite

BibTeXRIS
BibTeX
@article{gao2026fbmnguided,
  title = {{FBMN-Guided Discovery of Cyanogrisides from Mutant Strain CRM005 and Structural Diversification}},
  author = {Yukang Gao and Yun Luo and Qingyun Wen and Linmeng Chen and Guoliang Zhu and Peng Fu and Peipei Liu and Weiming Zhu},
  journal = {ACS Omega},
  year = {2026},
  month = oct,
  doi = {10.1021/acsomega.6c04357},
  url = {https://pubs.acs.org/acsodf/article/11/41/62728/5444931/FBMN-Guided-Discovery-of-Cyanogrisides-from-Mutant},
  note = {CC BY-NC-ND 4.0},
}
RIS
TY  - JOUR
TI  - FBMN-Guided Discovery of Cyanogrisides from Mutant Strain CRM005 and Structural Diversification
AU  - Yukang Gao
AU  - Yun Luo
AU  - Qingyun Wen
AU  - Linmeng Chen
AU  - Guoliang Zhu
AU  - Peng Fu
AU  - Peipei Liu
AU  - Weiming Zhu
PY  - 2026
DA  - 2026/10/06
JO  - ACS Omega
DO  - 10.1021/acsomega.6c04357
UR  - https://pubs.acs.org/acsodf/article/11/41/62728/5444931/FBMN-Guided-Discovery-of-Cyanogrisides-from-Mutant
AB  - Through genome mining and metabolomic analysis of the mutant strain CRM005, combined with feature-based molecular networking (FBMN) deduplication, five novel natural cyanogrisides (1–5) were selectively isolated and characterized, alongside six previously reported analogs (6–11). Antiproliferative assays demonstrated that cyanogriside K (8) exhibited potent and selective cytotoxicity against HCT-116 cells, with an IC50 value of 0.70 μM. In an effort to maximize the reutilization of natural product resources, the major aglycone caerulomycin H (11) was utilized to develop a glycosylation system, affording a small panel of nine glycosylated derivatives (13–21). Subsequent antiproliferative evaluations facilitated a preliminary structure–activity relationship analysis focused on variations in the glycosyl groups. Notably, the synthetic compound 13 displayed submicromolar-level activity against the human glioblastoma cell line SF-126 (IC50 0.49 μM), surpassing the activity of doxorubicin (IC50 0.78 μM). These findings position compound 13 as a promising cytotoxic hit derived from a small semisynthetic library and offer preliminary insight into how glycosyl modification impacts antiproliferative activity.
SN  - 2470-1343
ER  -