Results 21 to 30 of about 830,364 (264)

The role of ECL2 in CGRP receptor activation: a combined modelling and experimental approach [PDF]

, 2013
The calcitonin gene-related peptide (CGRP) receptor is a complex of a calcitonin receptor-like receptor (CLR), which is a family B G-protein-coupled receptor (GPCR) and receptor activity modifying protein 1.
Alex C. Conner, Barwell J, Bruck Taddese, Christopher A. Reynolds, Conner AC, David R. Poyner, Debbie L. Hay, Harriet A. Watkins, James Barwell, Kevin J. Smith, Michael. J. Woolley, Urano D, Watkins HA, Z. Gamze Karakullukcu   +13 more
core   +2 more sources

Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]

, 2009
We describe a general application of the nonsense suppression methodology for unnatural amino acid incorporation to probe drug–receptor interactions in functional G protein-coupled receptors (GPCRs), evaluating the binding sites of both the M2 muscarinic
Ballesteros, Cho, D. A. Dougherty, Dougherty, Dougherty, Dougherty, Doupnik, Gallivan, H. A. Lester, Hibert, Hopkins, Huang, Huang, K. S. Bower, Klabunde, Kofuji, Krapivinsky, Lagerstrom, Lu, Lu, M. M. Torrice, Ma, Mark, Nemeth, Nowak, Palczewski, Rasmussen, Schwartz, Warne, Xiu, Zacharias, Zhong   +31 more
core   +3 more sources

Thrombin Protease-activated Receptor-1 Signals through Gq- and G13-initiated MAPK Cascades Regulating c-Jun Expression to Induce Cell Transformation [PDF]

, 2003
Although the ability of G protein-coupled receptors to stimulate normal and aberrant cell growth has been intensely investigated, the precise nature of the molecular mechanisms underlying their transforming potential are still not fully understood.
Gutkind, J. Silvio, Marinissen, Maria Julia, Offermanns, Stefan, Servitja, Joan-Marc, Simon, Melvin I.   +4 more
core   +1 more source

Molecular architecture of Gαo and the structural basis for RGS16-mediated deactivation [PDF]

, 2008
Heterotrimeric G proteins relay extracellular cues from heptahelical transmembrane receptors to downstream effector molecules. Composed of an α subunit with intrinsic GTPase activity and a βγ heterodimer, the trimeric complex dissociates upon receptor ...
Berman, C.-K. Chen, Chan, Chen, Chen, Chen, Coleman, De Vries, Grafstein-Dunn, He, Heximer, K. C. Slep, Kimple, Koelle, Kozasa, Kozasa, Kudlacek, Lodowski, M. A. Kercher, M. I. Simon, McIntire, Neubig, Noel, P. B. Sigler, Slep, Snow, Sondek, Sunahara, T. Wieland, Tesmer, Tesmer, Valenzuela, Wang, Wilkie, Willars   +34 more
core   +4 more sources

Crystallization of G Protein-Coupled Receptors [PDF]

, 2013
Oligomerization is one of several mechanisms that can regulate the activity of G protein-coupled receptors (GPCRs), but little is known about the structure of GPCR oligomers. Crystallography and NMR are the only methods able to reveal the details of receptor-receptor interactions at an atomic level, and several GPCR homodimers already have been ...
David, Salom, Pius S, Padayatti, Krzysztof, Palczewski   +2 more
openaire   +2 more sources

Structural and Functional Analysis of a β2-Adrenergic Receptor Complex with GRK5. [PDF]

, 2017
The phosphorylation of agonist-occupied G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) functions to turn off G-protein signaling and turn on arrestin-mediated signaling.
Adams, Christopher M., Benovic, Jeffrey L., Betz, Robin M., Chung, Ka Young, Dror, Ron O., Du, Yang, Duc, Nguyen Minh, Kobilka, Brian K., Komolov, Konstantin E., Leib, Ryan D., Patra, Dhabaleswar, Rodrigues, João P.G.L.M., Skiniotis, Georgios   +12 more
core   +2 more sources

G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]

, 2017
It is widely appreciated that G protein-coupled receptors have been the most successfully exploited class of targets for the development of small molecule medicines. Despite this, to date, less than 15% of the non-olfactory G protein-coupled receptors in
Milligan, Graeme
core   +1 more source

G‐protein‐coupled receptors and melanoma [PDF]

Pigment Cell & Melanoma Research, 2008
SummaryG‐protein‐coupled receptors (GPCR) are the largest family of receptors with over 500 members. Evaluation of GPCR gene expression in primary human tumors identified over‐expression of GPCR in several tumor types. Analysis of cancer samples in different disease stages also suggests that some GPCR may be involved in early tumor progression and ...
Hwa Jin, Lee, Brian, Wall, Suzie, Chen
openaire   +2 more sources

GPCR-OKB: the G protein coupled receptor oligomer knowledge base [PDF]

, 2010
Rapid expansion of available data about G Protein Coupled Receptor (GPCR) dimers/oligomers over the past few years requires an effective system to organize this information electronically.
Bouvier, M., Camacho-Artacho, M., Campagne, F., Devi, L.A., Dorff, K., Filizola, M., George, S.R., Javitch, J.A., Khelashvili, G., Lohse, M.J., Milligan, G., Neubig, R.R., Palczewski, K., Parmentier, M., Pin, J.-P., Shan, J., Skrabanek, L., Vriend, G., Vroling, B.   +18 more
core   +3 more sources

Plasmodium falciparum gametogenesis essential protein 1 (GEP1) is a transmission‐blocking target

FEBS Letters, EarlyView.
This study shows Plasmodium falciparum GEP1 is vital for activating sexual stages of malarial parasites even independently of a mosquito factor. Knockout parasites completely fail gamete formation even when a phosphodiesterase inhibitor is added. Two single‐nucleotide polymorphisms (V241L and S263P) are found in 12%–20% of field samples.
Frederik Huppertz, Milagros Siebeck Caturelli, Lina S. Lehmann, Florian Kurth, Alexander G. Maier, Kai Matuschewski   +5 more
wiley   +1 more source