Regulators of G protein Signaling (RGS) proteins (version 2020.4) in the IUPHAR/BPS Guide to Pharmacology Database

Regulator of G protein Signaling, or RGS, proteins serve an important regulatory role in signaling mediated by G protein-coupled receptors (GPCRs). They all share a common RGS domain that directly interacts with active, GTP-bound Gα subunits of heterotrimeric G proteins. RGS proteins stabilize the transition state for GTP hydrolysis on Gα and thus induce a conformational change in the Gα subunit that accelerates GTP hydrolysis, thereby effectively turning off signaling cascades mediated by GPCRs. This GTPase accelerating protein (GAP) activity is the canonical mechanism of action for RGS proteins, although many also possess additional functions and domains. RGS proteins are divided into four families, R4, R7, R12 and RZ based on sequence homology, domain structure as well as specificity towards Gα subunits. For reviews on RGS proteins and their potential as therapeutic targets, see e.g. [160, 377, 411, 415, 416, 512, 519, 312, 6]

Regulators of G protein Signaling (RGS) proteins in GtoPdb v.2021.2

Regulator of G protein Signaling, or RGS, proteins serve an important regulatory role in signaling mediated by G protein-coupled receptors (GPCRs). They all share a common RGS domain that directly interacts with active, GTP-bound Gα subunits of heterotrimeric G proteins. RGS proteins stabilize the transition state for GTP hydrolysis on Gα and thus induce a conformational change in the Gα subunit that accelerates GTP hydrolysis, thereby effectively turning off signaling cascades mediated by GPCRs. This GTPase accelerating protein (GAP) activity is the canonical mechanism of action for RGS proteins, although many also possess additional functions and domains. RGS proteins are divided into four families, R4, R7, R12 and RZ based on sequence homology, domain structure as well as specificity towards Gα subunits. For reviews on RGS proteins and their potential as therapeutic targets, see e.g. [225, 529, 578, 583, 584, 742, 753, 444, 10]

The Concise Guide to PHARMACOLOGY 2023/24:Introduction and Other Protein Targets

The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and about 6000 interactions with about 3900 ligands. There is an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes almost 500 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.16176. In addition to this overview, in which are identified 'Other protein targets' which fall outside of the subsequent categorisation, there are six areas of focus: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2023, and supersedes data presented in the 2021/22, 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.</p

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Introduction and Other Protein Targets.

The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes over 500 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/bph.15537. In addition to this overview, in which are identified 'Other protein targets' which fall outside of the subsequent categorisation, there are six areas of focus: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2021, and supersedes data presented in the 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate

An exploration of gossip as an intrasexual competition strategy

"A thesis for the degree of Doctor of Philosophy in the Department of Psychology"Bibliography: pages 386-464.Chapter 1. A review of reputation-based gossip -- Chapter 2. Variables influencing reputation-based gossip -- Chapter 3. The role of gossip in mate poaching -- Chapter 4. Consequences of hearing gossip about one's partner -- Chapter 5. Gossip from the perspective of the derogated -- Chapter 6. General discussion.The research presented in this dissertation investigated whether gossip is useful as a strategy for intrasexual competition in both traditional and non-traditional mate attraction settings. The variables that influence engagement in, and the success of, reputation-based gossip were explored from the perspective of all three members of the mate competition triad; the individual, the romantic target, and the romantic competitor. Chapter 1 provides aliterature review of gossip research, particularly focusing on the role of gossip in mate competition. The historical context of gossip is initially provided, leading to a discussion of gossip as a strategy for intrasexual competition. The variables that influence reputation-based gossip are discussed and directions for future research outlined. Chapter 2 presents a study that investigated the demographic variables influencing a woman’s tendency to gossip. The results showed that age, relationship status, and parental status all influence gossip tendencies and gossip content. In line with predictions from evolutionary psychology, parental status was found to be the best predictor of both a woman’s overall tendency to gossip in addition to her tendency to focus on physical appearance and social information gossip content. Chapter 3 presents two studies that explored willingness to gossip in a mate poaching context. Crossculturally, men and women were found to be willing to share derogatory gossip about a competitor in order to poach the competitor’s partner. However, as the consequences for sharing this gossip increased, men became more willing to gossip than women and participants from collectivistic cultures became more willing to gossip than participants from individualistic cultures. The study detailed in Chapter 4 investigated reputation-based gossip from the perspective of the target utilising a qualitative methodology. In this study, the target was asked to describe the impact that hearing negative gossip about their partner’s sexual reputation would have on their perceptions of their partner and their relationship. Hearing this gossip was found to lead to a variety of negative relational consequences for the target, ranging from expressions of negative affect and distributive communication, to relationship dissolution. Despite this, targets generally reported being unwilling to retaliate aggressively against the gossiper, preferring to focus their attentions on their partners and their relationships. Chapter 5 presents a two-part study that explored the intrasexual and intersexual retention tactics the derogated competitor engages in as a result of hearing derogatory gossip about their reputation. The results of this study indicated that men and women were generally unwilling to retaliate aggressively against the gossiper, with social norms thought to constrain engagement in aggressive behaviour. Rather, derogated individuals reported they would preferentially focus their attentions on their romantic partners through engagement in intersexual retention tactics. Chapter 6 is a summation providing an overview and analysis of the empirical findings obtained throughout the studies conducted for this dissertation. Limitations of the current research are discussed, as are avenues for future research, before final conclusions conferred. The findings from this dissertation suggest that gossip is a low-risk intrasexual competition strategy, particularly effective when used strategically in mate poaching contexts.Mode of access: World wide web1 online resource (viii, 197 pages) illustrations, chart

Hearing the marginalised voices

[Extract] In this chapter, we explore how we might hear marginalised voices in the practice discourse. We propose (after Taylor, 2010) that Bakhtin's (1981, 1984) notions of dialogical rhetoric, heteroglossia, polyphony and carnival are helpful in conceptualising how these voices might be heard. We examine these theories and how they might relate to the focus of this chapter and draw on the work of Sparkes (1997, 2007),Cash (2007) and Francis and Hey (2009) for insights into how marginalised voices might be represented, speak out and speak back from within and beyond the margins of the primary discourse. The particular form of this book, using marginalia, allows us to juxtapose marginalised and dominant voices in the text and bring together disparate perspectives, opening up opportunities for a mutual construction of "truth" about professional practice. We considered that, by using Bakhtin's (1984, 1987) theories of language and discourse, this chapter could be presented as a dialogic interaction of multiple voices by writing in and from the margins of the primary discourse

The Concise Guide to PHARMACOLOGY 2023/24: Introduction and Other Protein Targets.

Publication status: PublishedThe Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and about 6000 interactions with about 3900 ligands. There is an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes almost 500 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.16176. In addition to this overview, in which are identified 'Other protein targets' which fall outside of the subsequent categorisation, there are six areas of focus: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2023, and supersedes data presented in the 2021/22, 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate