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 …

[HTML][HTML] Larixol is not an inhibitor of Gαi containing G proteins and lacks effect on signaling mediated by human neutrophil expressed formyl peptide receptors

L Björkman, H Forsman, L Bergqvist, C Dahlgren… - Biochemical …, 2024 - Elsevier
Neutrophils express several G protein-coupled receptors (GPCRs) connected to intracellular
Gα i or Gα q containing G proteins for down-stream signaling. To dampen GPCR mediated …

[HTML][HTML] 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 …

Bioactive Peptides and Proteins in Medicinal Chemistry

R Abdel-Jalil, R Stoll - Current Medicinal Chemistry, 2022 - ingentaconnect.com
Proteins and peptides play a crucial role in every aspect of cell structure and function, as
evidenced by their diversity and abundance. More than half of the dry weight of cells is made …

Investigating Chemical Pollutants at the 'Druggable'GPCRome: A Nexus of Pollutant Toxicity and Predictive Risk Assessment

JC Wilkinson - 2024 - search.proquest.com
Many synthetic chemicals used in industrial and consumer applications inevitably pollute
our food, water, and air. Much evidence has established these chemical pollutants as a …

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 …