0000000000408247

AUTHOR

Christine Beemelmanns

0000-0002-9747-3423

showing 2 related works from this author

Modular Solid-Phase Synthesis of Antiprotozoal Barnesin Derivatives

2020

Here, we applied and optimized a solid support (SP)-based Horner-Wadsworth-Emmons reagent to prepare SP-bound vinylogous amino acids. Subsequent SP-based peptide synthesis, global deprotection, and chemical modifications yielded 14 lipodipeptides carrying vinylogous amino acids, including the natural product barnesin A (1). Biological evaluation revealed that several synthesized derivatives show micromolar to nanomolar inhibitory activity against papain-like cysteine proteases, human cathepsin L, and rhodesain.

medicine.drug_classAntiprotozoal AgentsChemistry Techniques Synthetic010402 general chemistry01 natural sciencesBiochemistrychemistry.chemical_compoundSolid-phase synthesisPeptide synthesismedicineSolid-Phase Synthesis TechniquesHumansPhysical and Theoretical ChemistrySolid-Phase Synthesis Techniqueschemistry.chemical_classificationNatural productMolecular Structure010405 organic chemistryOrganic ChemistryCombinatorial chemistry0104 chemical sciencesAmino acidCysteine EndopeptidaseschemistryReagentAntiprotozoalCysteineOrganic Letters
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GNPS-guided discovery of xylacremolide C and D, evaluation of their putative biosynthetic origin and bioactivity studies of xylacremolide A and B

2021

Targeted HRMS2-GNPS-based metabolomic analysis of Pseudoxylaria sp. X187, a fungal antagonist of the fungus-growing termite symbiosis, resulted in the identification of two lipopeptidic congeners of xylacremolides, named xylacremolide C and D, which are built from d-phenylalanine, l-proline and an acetyl-CoA starter unit elongated by four malonyl-CoA derived ketide units. The putative xya gene cluster was identified from a draft genome generated by Illumina and PacBio sequencing and RNAseq studies. Biological activities of xylacremolide A and B were evaluated and revealed weak histone deacetylase inhibitory (HDACi) and antifungal activities, as well as moderate protease inhibition activity …

Antifungal0303 health sciencesProteasesProteasemedicine.drug_classGeneral Chemical Engineeringmedicine.medical_treatmentGeneral ChemistryBiologyGenomeChemistry03 medical and health sciences0302 clinical medicineMetabolomicsBiochemistrySymbiosis030220 oncology & carcinogenesisGene clustermedicineHistone deacetylase030304 developmental biologyRSC Advances
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