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 …

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 …

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 …

Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity

D Malfacini, J Patt, S Annala, K Harpsøe… - Journal of Biological …, 2019 - ASBMB
Transmembrane signals initiated by a range of extracellular stimuli converge on members of
the Gq family of heterotrimeric G proteins, which relay these signals in target cells. Gq family …

Bicyclic peptide library screening for the identification of Gαi protein modulators

A Pepanian, FA Binbay, S Roy… - Journal of Medicinal …, 2023 - ACS Publications
Noncanonical G protein activation and inactivation, particularly for the Gαi/s protein
subfamilies, have long been a focus of chemical research. Combinatorial libraries were …

Heterotrimeric G proteins as therapeutic targets in drug discovery

J Li, Y Ge, JX Huang, K Strømgaard… - Journal of medicinal …, 2019 - ACS Publications
Heterotrimeric G proteins are molecular switches in GPCR signaling pathways and regulate
a plethora of physiological and pathological processes. GPCRs are efficient drug targets …

Recent achievements in developing selective Gq inhibitors

H Zhang, AL Nielsen… - Medicinal research …, 2020 - Wiley Online Library
G proteins are key mediators of G protein‐coupled receptor (GPCR) signaling, facilitating a
plethora of important physiological processes. The role of G proteins is much less …

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 …

Unraveling binding mechanism and kinetics of macrocyclic Gαq protein inhibitors

JH Voss, J Nagel, M Rafehi, R Guixà-González… - Pharmacological …, 2021 - Elsevier
G proteins represent intracellular switches that transduce signals relayed from G protein-
coupled receptors. The structurally related macrocyclic depsipeptides FR900359 (FR) and …

Identification of promising compounds from curry tree with cyclooxygenase inhibitory potential using a combination of machine learning, molecular docking, dynamics …

PN Pandya, SP Kumar, K Bhadresha… - Molecular …, 2020 - Taylor & Francis
ABSTRACT Murraya koenigii (Linn.) Spreng, commonly known as curry leaf tree, is popular
as a condiment and spice among Asian countries. Ethnobotanical studies suggest that …