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Halofuginone is a Molecular Glue Degrader of Integrin β4

Advanced Science, EarlyView.
Integrin β4 overexpression is linked to aggressive tumors and poor prognosis, but targeted therapies are lacking. We identified halofuginone (HF) as a molecular glue degrader that promotes integrin β4 degradation via the CRL4BWDR18 E3 ligase. HF suppresses tumor progression in vitro and in vivo, offering a new strategy for targeting oncogenic ...
Wei Gong, Di Yang, Junrui Tian, Yufei Chai, Tiantian Yu, Qingnan Wu, Yan Wang, Weimin Zhang, Qimin Zhan   +8 more
wiley   +1 more source

Signalling mechanisms used by the orexin-1 receptor [PDF]

Peltonen, Hanna
core  

Regulation of G protein-coupled receptor kinase subtypes by calcium sensor proteins

Biochimica Et Biophysica Acta - Molecular Cell Research, 2000
Michele Sallese, Luisa Iacovelli, Loredana Capobianco   +2 more
exaly   +2 more sources

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Regulation of G Protein-Coupled Receptor Kinases

Trends in Cardiovascular Medicine, 2000
G protein-coupled receptor kinases (GRKs) specifically interact with the agonist-activated form of G protein-coupled receptors (GPCRs) to effect receptor phosphorylation and desensitization. Recent studies demonstrate that GRK function is a highly regulated process, and it is perhaps in this manner that a handful of GRKs (7 have been identified to date)
R B, Penn, A N, Pronin, J L, Benovic
openaire   +2 more sources

G-protein-coupled receptor regulation: role of G-protein-coupled receptor kinases and arrestins

Canadian Journal of Physiology and Pharmacology, 1996
G-protein-coupled receptors (GPCRs) represent a large family of proteins that transduce extracellular signals to the interior of cells. Signalling through these receptors rapidly desensitized primarily as the consequence of receptor phosphorylation, but receptor sequestration and downregulation can also contribute to this process.
S S, Ferguson, L S, Barak, J, Zhang, M G, Caron   +3 more
openaire   +2 more sources

Selective Regulation of Gq Signaling by G Protein-Coupled Receptor Kinase 2: Direct Interaction of Kinase N Terminus with Activated Gαq

Molecular Pharmacology, 2000
In this study, we investigated the regulation of different G protein-coupled receptor (GPCR)-stimulated signaling pathways by GPCR kinase 2 (GRK2). We used thyrotropin receptor, which is coupled to different G proteins, to investigate the regulation of ...
M. Sallese, S. Mariggiò, Etrusca D'Urbano, L. Iacovelli, A. Blasi   +4 more
semanticscholar   +1 more source

G protein—coupled receptor kinases

Cell, 1993
G protein‐coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein‐coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization.
openaire   +2 more sources

Characterization of G protein-coupled receptor kinases

2002
Publisher Summary A basic feature of most cells is the ability to dynamically regulate their responsiveness to extracellular stimuli. Numerous stimuli transmit their signals via interaction with cell surface G protein-coupled receptors (GPCRs). GPCRs are subject to three principal modes of regulation: (1) desensitization, the process by which a ...
Alexey N, Pronin, Robert P, Loudon, Jeffrey L, Benovic   +2 more
openaire   +2 more sources

G-protein-coupled receptor kinases and the heart

Trends in Cardiovascular Medicine, 1995
The family of G-protein-coupled receptors includes many well-studied members, such as the adrenergic and the muscarinic acetylcholine receptors. These receptors are regulated by multiple mechanisms that serve to adapt their expression and their function to a rapidly changing environment.
openaire   +2 more sources

Targeting G protein-coupled receptor kinases to their receptor substrates

Journal of Membrane Biology, 1997
Membrane association is essential for GRK function and because of this the GRKs have evolved complex regulatory mechanisms for associating with the membrane. Although the GRKs are highly homologous, each kinase utilizes a distinct mechanism for associating with the membrane, which makes it unique within the family.
R H, Stoffel, J A, Pitcher, R J, Lefkowitz   +2 more
openaire   +2 more sources