Heterotrimeric Gq proteins as therapeutic targets?
E Kostenis, EM Pfeil, S Annala - Journal of Biological Chemistry, 2020 - ASBMB
Heterotrimeric G proteins are the core upstream elements that transduce and amplify the
cellular signals from G protein–coupled receptors (GPCRs) to intracellular effectors. GPCRs …
cellular signals from G protein–coupled receptors (GPCRs) to intracellular effectors. GPCRs …
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 …
metastasis. Once metastasis occurs, patients are often left with a short survival time, since …
Functional characterization of uveal melanoma oncogenes
J Ma, L Weng, BC Bastian, X Chen - Oncogene, 2021 - nature.com
Uveal melanoma (UM) is a currently untreatable form of melanoma with a 50% mortality rate.
Characterization of the essential signaling pathways driving this cancer is critical to develop …
Characterization of the essential signaling pathways driving this cancer is critical to develop …
Thioesterase-mediated side chain transesterification generates potent Gq signaling inhibitor FR900359
C Hermes, R Richarz, DA Wirtz, J Patt, W Hanke… - Nature …, 2021 - nature.com
The potent and selective Gq protein inhibitor depsipeptide FR900359 (FR), originally
discovered as the product of an uncultivable plant endosymbiont, is synthesized by a …
discovered as the product of an uncultivable plant endosymbiont, is synthesized by a …
Pharmacological Gq inhibition induces strong pulmonary vasorelaxation and reverses pulmonary hypertension
A Seidinger, R Roberts, Y Bai, M Müller… - EMBO Molecular …, 2024 - embopress.org
Pulmonary arterial hypertension (PAH) is a life-threatening disease with limited survival.
Herein, we propose the pharmacological inhibition of Gq proteins as a novel concept to …
Herein, we propose the pharmacological inhibition of Gq proteins as a novel concept to …
Agonist-Dependent Coupling of the Promiscuous Adenosine A2B Receptor to Gα Protein Subunits
The adenosine A2B receptor (A2BAR) belongs to the rhodopsin-like G protein-coupled
receptor (GPCR) family. It is upregulated under hypoxic conditions, in inflammation and …
receptor (GPCR) family. It is upregulated under hypoxic conditions, in inflammation and …
Discovery of P2Y2 Receptor Antagonist Scaffolds through Virtual High-Throughput Screening
A Neumann, I Attah, H Al-Hroub… - Journal of chemical …, 2022 - ACS Publications
The human ATP-and UTP-activated P2Y2 receptor (P2Y2R) is a Gq protein-coupled
receptor involved in several pathophysiological conditions including acute and chronic …
receptor involved in several pathophysiological conditions including acute and chronic …
The Bacterial Gq Signal Transduction Inhibitor FR900359 Impairs Soil-Associated Nematodes
W Hanke, J Alenfelder, J Liu, P Gutbrod… - Journal of chemical …, 2023 - Springer
The cyclic depsipeptide FR900359 (FR) is derived from the soil bacterium Chromobacterium
vaccinii and known to bind Gq proteins of mammals and insects, thereby abolishing the …
vaccinii and known to bind Gq proteins of mammals and insects, thereby abolishing the …
The chromodepsins–chemistry, biology and biosynthesis of a selective Gq inhibitor natural product family
C Hermes, GM König, M Crüsemann - Natural product reports, 2021 - pubs.rsc.org
Covering: up to April 2021 The bacterial cyclic depsipeptides FR900359 (FR) and YM-
254890 (YM) were shown to selectively inhibit Gαq proteins with high potency and selectivity …
254890 (YM) were shown to selectively inhibit Gαq proteins with high potency and selectivity …
Unraveling binding mechanism and kinetics of macrocyclic Gαq protein inhibitors
G proteins represent intracellular switches that transduce signals relayed from G protein-
coupled receptors. The structurally related macrocyclic depsipeptides FR900359 (FR) and …
coupled receptors. The structurally related macrocyclic depsipeptides FR900359 (FR) and …