EJE AWARD 2020: Signalling by G protein-coupled receptors: why space and time matter

نویسندگان

چکیده

G protein-coupled receptors (GPCRs) are the largest family of membrane and major drug targets. They play a fundamental role in endocrine system, where they mediate effects several hormones neurotransmitters. As result, alterations GPCR signalling cause disorders such as congenital hypothyroidism or Cushing’s syndrome. My group develops innovative optical methods fluorescence resonance energy transfer (FRET) single-molecule microscopy, which allow us to investigate living cells with unprecedented spatiotemporal resolution. Using this approach, we have contributed elucidate some long-debated questions about mechanisms their involvement human disease. Among other findings, these studies led unexpected discovery that GPCRs not only at cell surface, previously assumed, but also various intracellular sites. This has important implications understand how neurotransmitters produce specific responses our might pave way treatments for common diseases like diabetes heart failure.

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Regulatory mechanisms that modulate signalling by G-protein-coupled receptors.

The large and functionally diverse group of G-protein-coupled receptors includes receptors for many different signalling molecules, including peptide and non-peptide hormones and neuro-transmitters, chemokines, prostanoids and proteinases. Their principal function is to transmit information about the extracellular environment to the interior of the cell by interacting with the heterotrimeric G-...

متن کامل

Sphingosine kinase-mediated Ca2+ signalling by G-protein-coupled receptors.

Formation of inositol 1,4,5-trisphosphate (IP3) by phospholipase C (PLC) with subsequent release of Ca2+ from intracellular stores, is one of the major Ca2+ signalling pathways triggered by G-protein-coupled receptors (GPCRs). However, in a large number of cellular systems, Ca2+ mobilization by GPCRs apparently occurs independently of the PLC-IP3 pathway, mediated by an as yet unknown mechanism...

متن کامل

Signalling between G-protein-coupled receptors and TASK1 channels.

The superfamily of two pore-domain K+ (K2P) channels has a least 15 members, of which mainly TASK1 is expressed in cardiac myocytes. TASK1 gating is voltage independent, but the channel is acid sensitive, being activated by alkalotic conditions. Ion currents carried by TASK1 likely contribute to the cardiac action potential duration (APD), and pharmacological inhibition of TASK1 lengthens the A...

متن کامل

G-protein-coupled receptors: evolving views on physiological signalling: symposium on G-protein-coupled receptors: evolving concepts and new techniques.

Introduction In 1967, Earl Sutherland described the simplest possible model for signalling through heptahelical receptors when he wrote, “It seems likely that in most, and perhaps all, tissues the receptor and adenylyl cyclase are the same” (Robison et al, 1967). Within ten years, Rodbell and Gilman had disproved this model by showing that heterotrimeric guanine nucleotide-binding proteins (G p...

متن کامل

G Protein-coupled receptors

G protein-coupled receptors and heterotrimeric G proteins can diffuse laterally in the plasma membrane such that one receptor can catalyze the activation (GDP/GTP exchange) of multiple G proteins. In some cases, these processes are fast enough to support molecular signal amplification, where a single receptor maintains the activation of multiple G proteins at steady-state. Amplification in cell...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: European journal of endocrinology

سال: 2021

ISSN: ['1479-683X', '0804-4643']

DOI: https://doi.org/10.1530/eje-20-0890