Combining activity profiling with advanced annotation to accelerate the discovery of natural products targeting oncogenic signaling in melanoma

T Hell, A Rutz, L Dürr, M Dobrzyński… - Journal of natural …, 2022 - ACS Publications
The discovery of bioactive natural products remains a time-consuming and challenging task.
The ability to link high-confidence metabolite annotations in crude extracts with activity …

Targeting Oncogenic Gαq/11 in Uveal Melanoma

D Lapadula, JL Benovic - Cancers, 2021 - mdpi.com
Simple Summary Uveal melanoma is a deadly form of eye cancer with a high rate of
metastasis. Once metastasis occurs, patients are often left with a short survival time, since …

New insights into in mycotoxins production in Alternaria infected apple during postharvest storage

X Mao, A Chen, J Qu, P Luo, Y You, Y Gao… - Postharvest Biology and …, 2023 - Elsevier
As an apple fruit rot disease related fungus, Alternaria spp. could bring severe hazardous
risk to apple fruits during postharvest storage. In this research, cold treatment is investigated …

Structural response of G protein binding to the cyclodepsipeptide inhibitor FR900359 probed by NMR spectroscopy

C Bonifer, W Hanke, J Mühle, F Löhr… - Chemical …, 2024 - pubs.rsc.org
The cyclodepsipeptide FR900359 (FR) and its analogs are able to selectively inhibit the
class of Gq proteins by blocking GDP/GTP exchange. The inhibitor binding site of Gq has …

Promoter‐Driven Overexpression in Chromobacterium vaccinii Facilitates Access to FR900359 and Yields Novel Low Abundance Analogs

D Pistorius, K Buntin, E Weber… - … A European Journal, 2022 - Wiley Online Library
Access to the cyclic depsipeptide FR900359 (FR), a selective Gq/11 protein inhibitor of high
pharmacological interest and a potential lead molecule for targeted therapy of cancers with …

Recommended Tool Compounds: Application of YM-254890 and FR900359 to Interrogate Gαq/11-Mediated Signaling Pathways

JH Voss - ACS Pharmacology & Translational Science, 2023 - ACS Publications
The macrocyclic depsipeptides YM-254890 (YM) and FR900359 (FR) are natural products,
which inhibit heterotrimeric Gαq/11 proteins with high potency and outstanding selectivity …

Structure-affinity and structure-residence time relationships of macrocyclic Gαq protein inhibitors

JH Voss, M Crüsemann, CRO Bartling, S Kehraus… - Iscience, 2023 - cell.com
The macrocyclic depsipeptides YM-254890 (YM) and FR900359 (FR) are potent inhibitors of
Gα q/11 proteins. They are important pharmacological tools and have potential as …

Targeted Isolation of Dolabellane Diterpenoids from the Soft Coral Clavularia viridis Using Molecular Networking

X Dong, J Wu, H Jia, S Cen, W Cheng, W Lin - ACS omega, 2023 - ACS Publications
LC–MS/MS-based molecular networking annotation coupled 1H NMR detection allowed the
depiction of the soft coral Clavularia viridis to produce a profile of dolabellane-type …

Das Cyclodepsipeptid FR900359: Ein Insektizid mit neuem Wirkmechanismus aus Cand. Burkholderia crenata und Chromobacterium vaccinii

W Hanke - 2024 - bonndoc.ulb.uni-bonn.de
The cyclic depsipeptide FR900359: An insecticide with a novel mode of action from Cand.
Burkholderia crenata and Chromobacterium vaccinii Secondary metabolites (SM) are known …

Biochemical Pharmacology Structure-Affinity and Structure-Residence Time Relationships of Macrocyclic Gα q Protein Inhibitors

JH Voss, M Crüsemann, C Bartling, S Kehraus… - Available at SSRN … - papers.ssrn.com
The natural macrocyclic depsipeptides YM-254890 (YM) and FR900359 (FR), produced by
bacteria, are potent and selective inhibitors of Gαq/11 proteins. These compounds have …