• One protein, Gpr4, shares limited sequence identity with the Dictyostelium discoideum cAMP receptor cAR1 and the Aspergillus nidulans GPCR protein GprH and also shares structural similarity with the Saccharomyces cerevisiae receptor Gpr1. (elsevier.com)
  • The human beta-2 adrenergic receptor in complex with the partial inverse agonist carazolol . (wikipedia.org)
  • Natural estrogens such as 17β-estradiol, a nonselective agonist of ERα, ERβ, and GPER, 8 modulate vasoconstrictor prostanoid activity and the expression of TP receptors and prostanoid synthases. (ahajournals.org)
  • The company's lead program is a best-in-class sphingosine-1-phosphate receptor (S1P1) small molecule agonist candidate for autoimmune indications, including multiple sclerosis, that will enter a Phase 1 clinical trial in early 2011. (businesswire.com)
  • To explore the importance of receptor regulation, we engineered a series of Gi-coupled receptors that differ in signal length, degree of agonist-induced internalization, and ability to induce adenylyl cyclase superactivation. (sigmaaldrich.com)
  • Replacement of the C-terminus of the RASSL with the corresponding portion of the mu opioid receptor eliminated the induction of AC superactivation, without disrupting agonist-induced desensitization or internalization. (sigmaaldrich.com)
  • However, the receptor still signals and desensitizes in response to agonist, indicating normal G-protein coupling and partial membrane expression. (sigmaaldrich.com)
  • While each of these processes is initiated by the exposure of receptors to agonist, they proceed at different rates and can be dissociated on this basis. (scielo.br)
  • ORG27569 also decreases basal signaling, acting as an inverse agonist for the G protein-mediated signaling pathway. (pubmedcentralcanada.ca)
  • Therefore, both the efficacy and the potency of norepinephrine increase ∼10-fold over a few seconds of agonist stimulation, which illustrates that receptor and G-protein signaling and signal amplification are highly time-dependent phenomena. (aspetjournals.org)
  • By what pathway, or pathways, do drugs enter and exit the receptor binding pocket? (pnas.org)
  • Arrestins activated by interaction with phosphorylated receptors can also mediate G-protein-independent signalling by serving as adaptors to link receptors to numerous signalling pathways 4 . (nature.com)
  • Spinophilin knockout mice were more sensitive than wild-type mice to sedation elicited by stimulation of α 2 adrenergic receptors, whereas arrestin 3 knockout mice were more resistant, indicating that the signal-promoting, rather than the signal-terminating, roles of arrestin are more important for certain response pathways. (sciencemag.org)
  • The identification of this family of receptors should rekindle the investigation of the roles of trace amines in mammalian nervous systems and may potentially lead to the development of novel therapeutics for a variety of indications. (pnas.org)
  • Examples are the receptors of the olfactory epithelium that bind odorants and receptors of the neurotransmitter serotonin in the mammalian brain . (statemaster.com)
  • There are eight mammalian P2Y receptors known to date ( P2Y1 , P2Y2 , P2Y4 , P2Y6 , P2Y11 , P2Y12 , P2Y13 and P2Y14 ) and they are found in most human tissues. (atlasgeneticsoncology.org)
  • The problem of automatic protein classification using only their primary structures plays an important role in modern bioinformatics research, especially for proteins whose 3-D structures are yet unknown. (upc.edu)
  • A better understanding of the GPER, its role in breast cancer, and the interactions with the ER and epidermal growth factor receptor will be beneficial for the disease management and prevention in the future. (mdpi.com)
  • This class constitutes about 20 distinct, highly diverged protein receptors that are specific for peptide pheromones. (news-medical.net)
  • Here we report the crystal structure of β-arrestin-1 (also called arrestin-2) in complex with a fully phosphorylated 29-amino-acid carboxy-terminal peptide derived from the human V2 vasopressin receptor (V2Rpp). (nature.com)