+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

G protein-coupled receptors--recent advances

, : G protein-coupled receptors--recent advances. Acta Biochimica Polonica 59(4): 515-529

The years 2000 and 2007 witnessed milestones in current understanding of G protein-coupled receptor (GPCR) structural biology. In 2000 the first GPCR, bovine rhodopsin, was crystallized and the structure was solved, while in 2007 the structure of β(2)-adrenergic receptor, the first GPCR with diffusible ligands, was determined owing to advances in microcrystallization and an insertion of the fast-folding lysozyme into the receptor. In parallel with those crystallographic studies, the biological and biochemical characterization of GPCRs has advanced considerably because those receptors are molecular targets for many of currently used drugs. Therefore, the mechanisms of activation and signal transduction to the cell interior deduced from known GPCRs structures are of the highest importance for drug discovery. These proteins are the most diversified membrane receptors encoded by hundreds of genes in our genome. They participate in processes responsible for vision, smell, taste and neuronal transmission in response to photons or binding of ions, hormones, peptides, chemokines and other factors. Although the GPCRs share a common seven-transmembrane α-helical bundle structure their binding sites can accommodate thousands of different ligands. The ligands, including agonists, antagonists or inverse agonists change the structure of the receptor. With bound agonists they can form a complex with a suitable G protein, be phosphorylated by kinases or bind arrestin. The discovered signaling cascades invoked by arrestin independently of G proteins makes the GPCR activating scheme more complex such that a ligand acting as an antagonist for G protein signaling can also act as an agonist in arrestin-dependent signaling. Additionally, the existence of multiple ligand-dependent partial activation states as well as dimerization of GPCRs result in a 'microprocessor-like' action of these receptors rather than an 'on-off' switch as was commonly believed only a decade ago.


PMID: 23251911

Other references

Hooper-McGrevy, K.E.; Giguere, S.; Wilkie, B.N.; Prescott, J.F., 2001: Evaluation of equine immunoglobulin specific for Rhodococcus equi virulence-associated proteins A and C for use in protecting foals against Rhodococcus equi-induced pneumonia. The objective of the study is to determine whether purified equine immunoglobulin specific for R. equi virulence-associated proteins A and C (VapA and VapC) can confer passive protection against R. equi-induced pneumonia in foals. Seven foals rece...

Wagner, G., 1999: Political distribution problems of social security. The ongoing change of demographic and economic structures does not undermine employment (as many believe), but this change indeed induces problems with the mandatory old-age security system in Germany. This paper discusses some popular reform prop...

van Pesch, V.; Sindic, C.J.M., 2013: Vitamin D supplementation in multiple sclerosis patients in 2012: hype or reality as an adjunctive therapy?. Acta Neurologica Belgica 112(4): 325-325

Enoz, M.; Kiyak, E.; Katircioglu, S.; Gulluoglu, M., 2007: Abrikossoff tumor of the larynx. Case report about laryngeal localization of a granular cell tumor in a 38 years old female without recurrence over an observation period of two years.

Hefetz, A.K.onenberg, S.P.leg, B.; Bar-Zakay, I., 1988: Mating disruption of the California red scale Aonidiella aurantii (Homoptera: Diaspididae). Citriculture: proceedings of the Sixth International Citrus Congress: Middle East Tel Aviv Israel March 6-11-1988 scientific editors R Goren and K Mendel editor N Goren: -1127

Abramson, D.H.; Ellsworth, R.M.; Rozakis, G.W., 1982: Cryotherapy for retinoblastoma. Cryotherapy was applied to 138 intraocular retinoblastoma tumors from 113 patients who were followed up for a mean of 40 months (four to 144 months). Overall, 70% of tumors were cured with cryotherapy and 93% of patients treated with cryotherapy s...

Harboe, Z.B.; Valentiner-Branth, P.; Benfield, T.L.; Christensen, J.Jørgen.; Hjuler, T.; Kaltoft, M.; Krogfelt, K.A.; Lambertsen, L.; Konradsen, H.B., 2008: Estimated effect of pneumococcal conjugate vaccination on invasive pneumococcal disease and associated mortality, Denmark 2000-2005. In order to provide an estimation of the direct and indirect benefits of pneumococcal vaccination with three protein-conjugate pneumococcal vaccines (PCV) we described the epidemiology and mortality from invasive pneumococcal disease (IPD) in Denm...

Smith, C.A.; Massie, L.B.; Gilpatrick, J.D.; Seem, R.C., 1976: Electronic disease monitoring. In field trials in apples, an electronic device to record leaf wetting periods gave good results when used in conjunction with standard recording thermographs to estimate apple scab (Venturia inaequalis) infection periods. The device compared favo...

Elmannai, W.; Elleithy, K., 2017: Sensor-Based Assistive Devices for Visually-Impaired People: Current Status, Challenges, and Future Directions. The World Health Organization (WHO) reported that there are 285 million visuallyimpaired people worldwide. Among these individuals, there are 39 million who are totally blind. There have been several systems designed to support visually-impaired p...

Chen, D.; Yang, T-Chuan., 2014: The pathways from perceived discrimination to self-rated health: an investigation of the roles of distrust, social capital, and health behaviors. Although there has been extensive research on the adverse impacts of perceived discrimination on health, it remains unclear how perceived discrimination gets under the skin. This paper develops a comprehensive structural equation model (SEM) by in...