Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Cyclodipeptides from fungi and bacteria are often modified by different tailoring enzymes. They display various biological and pharmacological activities, and some derivatives are used as drugs. In a previous study, we elucidated the function of the silent guatrypmethine gene cluster from containing a cyclodipeptide synthase (CDPS) core gene and four genes for tailoring enzymes. The latter are used in this study for the design of modified cyclodipeptides by genetic engineering. Addition of six different cyclodipeptides to the transformant harboring led to the detection of different pathway products. Coexpression of five CDPS genes from four strains with resulted in the formation of diketopiperazine derivatives, differing in their modification stages. Our results demonstrate the potential of rational gene combination to increase structural diversity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/acssynbio.3c00115 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Diketopiperazines with anti-skin inflammation from marine-derived endophytic fungus Aspergillus sp. and configurational reassignment of aspertryptanthrins.
Chin J Nat Med
August 2025
State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai 200237, China; Marine Biomedical Science and Technology Innovation Platform of Lin-gang Special Area, Shanghai 201306, China. Electronic address:
Two novel diketopiperazines (1 and 5), along with ten known compounds (2-4, 6-12) demonstrating significant skin inflammation inhibition, were isolated from a marine-derived fungus identified as Aspergillus sp. FAZW0001. The structural elucidation and configurational reassessments of compounds 1-5 were established through comprehensive spectral analyses, with their absolute configurations determined via single crystal X-ray diffraction using Cu Kα radiation, Marfey's method, and comparison between experimental and calculated electronic circular dichroism (ECD) spectra.
View Article and Find Full Text PDFMolecular networking derived from untargeted LC-MS/MS analysis to discover inhibitors of RANKL-induced osteoclastogenesis from Egyptian marine sponge-associated fungi.
Sci Rep
July 2025
Chemistry of Natural and Microbial Products Department, National Research Centre, 33 El-Bohouth St., Dokki, Giza, 12622, Egypt.
In continuous search for RANKL induced osteoclastogenesis inhibitors, twenty-six fungal isolates were obtained from ten Red Sea marine sponges collected from Egypt and the ethyl acetate fractions of their cultures' methanol extracts were assessed in RAW264 macrophages. Active fractions were profiled via LC-MS/MS, followed by untargeted molecular networking, leading to the tentative identification of eight unreported compounds (1, A2, C1, C2, C4-C7), and thirteen known compounds. The two active fungi were identified and deposited in GenBank with accession numbers PQ423742 and PQ423748 for Aspergillus flavus and Cladosporium colombiae, respectively.
View Article and Find Full Text PDFThe Novel Diketopiperazine Derivative, Compound 5-3, Selectively Inhibited the Proliferation of FLT3-ITD Mutant Acute Myeloid Leukemia (AML) Cells.
Mar Drugs
July 2025
Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 5 Yushan Rd, Qingdao 266003, China.
The internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) is associated with high recurrence and mortality rates in acute myeloid leukemia (AML), making it a critical target for anti-AML therapies. Plinabulin is a diketopiperazines derivative that exhibits extensive anti-cancer potency by targeting β-tubulin. We designed and synthesized a novel FLT3 inhibitor, namely , based on the structure of plinabulin and evaluated its effect on FLT3-ITD mutant AML cells.
View Article and Find Full Text PDFMolecular networking-guided isolation of linearly fused prenylated indole diketopiperazine alkaloids from a marine-derived fungus Aspergillus sp. MG35-18 and their anti-inflammatory effects.
Fitoterapia
September 2025
Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy/State Key Laboratory of Bioactive Molecules and Druggability Assessment/International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Ministry of Education (MOE
This study described the isolation and structural characterization of four novel linearly fused prenylated indole diketopiperazine alkaloids (1-4) alongside four known analogues from the marine-derived fungus Aspergillus sp. MG35-18, guided by LC-MS/MS-based molecular networking. These compounds are characterized with a rare [3,2-f] indole-pyrano fused ring system.
View Article and Find Full Text PDFAntiosteoclastogenic Indole Alkaloids from the Mangrove Endophytic Fungus GXIMD 02511.
J Nat Prod
July 2025
Guangxi Key Laboratory of Marine Drugs, University Engineering Research Center of High-efficient Utilization of Marine Traditional Chinese Medicine Resources, Guangxi, Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, China.
Eight new prenylated indole alkaloids, brefeldindoles A-F (-), G (), and H (), together with 17 known analogues, were obtained from the Beibu Gulf mangrove-derived fungal strain GXIMD 02511. Their structures, including absolute configurations, were determined by analysis of spectroscopic data and electronic circular dichroism (ECD) calculations. Brefeldindoles A-F (-) are characterized as a rare class of indole-diterpenoid derivatives with uncommon 3-methyl-3-hydroxybutyl substituents in the benzene ring.
View Article and Find Full Text PDF