Related references
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Article
Biochemistry & Molecular Biology
Yin Kwan Chung et al.
Summary: G protein-coupled receptors (GPCRs) are important drug targets, and signals from these receptors are primarily transduced via two functional components of G proteins, with increasing focus on the role of G beta gamma dimers. These dimers play a key role in regulating cellular physiology and are implicated in various diseases, although there is a bias in detecting G beta gamma signals from specific types of receptors.
Review
Biochemistry & Molecular Biology
Antara A. Banerjee et al.
Summary: The follicle-stimulating hormone receptor (FSHR) is a crucial G protein-coupled receptor in mammalian reproduction. This review covers the entire life cycle of FSHR, from its formation to internalization and degradation, highlighting important functional aspects and signaling pathways associated with this receptor. Unresolved questions and challenges in FSHR research are also presented for exploration.
Review
Biochemistry & Molecular Biology
Alexey Bondar et al.
Summary: Heterotrimeric G proteins play a central role in cellular signal transduction by mediating signals from G protein-coupled receptors to downstream effectors. Various optical sensors for G protein localization and function have been developed and applied in living systems since their discovery. This minireview provides an overview of existing G protein-based sensors, experimental approaches, recent advances, challenges, and future directions in the field of G protein sensor development.
Review
Biochemistry & Molecular Biology
Necla Birgul Iyison et al.
Summary: The urgent need for developing next-generation pesticides due to increasing human population and inefficiency of available pesticides is highlighted. Targeting invertebrate GPCRs has great potential in pesticide development, but further genomic and transcriptomic data are necessary for a full utilization of this strategy.
Article
Biochemistry & Molecular Biology
Anthony H. Nguyen et al.
Summary: G protein-coupled receptors (GPCRs) are a major class of cell-surface receptors involved in cellular signaling, traditionally thought to signal through G proteins or β-arrestin. However, recent studies have shown that some receptors are capable of sustained signaling even after internalization, challenging previous understanding. This new mechanism of sustained signaling presents new research directions and challenges.
Review
Biochemistry & Molecular Biology
Praachi Tiwari et al.
Summary: Early adversity significantly affects the development of neurocircuits regulating emotionality, leading to increased risk of adult anxiety and depression. Disruption of G protein-coupled receptor signaling may play a central role in programming persistent changes at molecular, cellular, functional, and behavioral levels as a consequence of early adversity.
Review
Biochemistry & Molecular Biology
Andreas Bock et al.
Summary: Bias agonism in GPCRs is likely a result of preferential allosteric coupling from the ligand binding pocket to a specific transducer, leading to selective activation of desired signaling pathways and potentially reducing side effects.
Review
Biochemistry & Molecular Biology
Yasmin Aydin et al.
Summary: Arrestins are multifunctional cytosolic adaptors that bind to active and phosphorylated GPCRs via a versatile interface, stopping G protein signaling and triggering other pathways. Recent studies have provided a wealth of information about the key determinants and dynamic insights into the arr-GPCR interaction, but questions about the functional consequences of structural details and interaction dynamics remain open for further investigation. Techniques such as mutagenesis studies, cross-linking studies, conformational probes, and sensors have been used to explore arr structure, function, and dynamics, offering valuable insights into the process of arr binding and the outcomes of different binding modes.
Review
Biochemistry & Molecular Biology
Mark Soave et al.
Summary: GPCRs, the largest family of membrane receptors, are major drug targets approved by the FDA. Recent advances in genome editing and fluorescent ligand design have provided new possibilities for studying GPCRs in their native environment. This review discusses the technical advances used to study the localization and ligand binding characteristics of genome-edited and endogenously expressed GPCRs.
Review
Biochemistry & Molecular Biology
Jeffrey S. Smith et al.
Summary: Recent discoveries have shown direct interactions between G proteins and beta-arrestins, essential for signaling and physiological events. Only members of the Gαi subtype family can form direct interactions with beta-arrestin, while other Gα subtypes do not possess this characteristic.
Review
Biochemistry & Molecular Biology
Anastasios Lymperopoulos et al.
Summary: The autonomic nervous system exerts its effects on the human myocardium through distinct G protein-coupled receptors on the plasma membranes of cardiac cells. Neurotransmitters like NE/Epi and ACh mediate these effects by activating specific adrenergic or muscarinic receptors. Other neurotransmitters/hormones also play a role in regulating cardiac function by utilizing different GPCRs in the heart.
Review
Biochemistry & Molecular Biology
Nicola J. Smith et al.
Summary: The class C G protein-coupled sweet taste receptor (STR) is responsible for sweet taste perception and has potential for pharmacotherapeutic modulation. Research focuses on regulation of STR surface expression and signal transduction, as well as exploitation of biased agonists. However, mechanisms controlling STR and the impact of receptor polymorphisms remain unclear.
Review
Biochemistry & Molecular Biology
Luiz F. Barella et al.
Summary: As the incidence of obesity and type 2 diabetes continues to rise globally, there is a growing need for more effective therapies. G protein-coupled receptors (GPCRs) have emerged as important drug targets for these chronic diseases, with research focusing on their role in regulating glucose metabolism and energy homeostasis.
Review
Biochemistry & Molecular Biology
Ning Ma et al.
Summary: GPCRs are membrane-bound proteins that play a critical role in mediating multiple signaling pathways. They possess a dynamic nature and exist in an equilibrium between inactive and active states, with ligands selectively stabilizing specific conformations to shift the equilibrium. This ligand-selective effect is achieved through allosteric communication between the ligand binding site and G protein or beta-arrestin coupling site, allowing for the design of selective ligands and mutants with specific interactions.
Review
Biochemistry & Molecular Biology
Arundhasa Chandrabalan et al.
Summary: Proteinase-activated receptors (PARs) are a family of receptors crucial in regulating physiological responses and implicated in various pathological conditions. PAR1 and PAR4 are essential for platelet function, while PAR2 drives inflammatory responses. Recent advancements in understanding the molecular mechanisms of PAR activation, signaling, and the involvement of different proteolytic enzymes as PAR regulators have been key in PAR-targeted drug development.
Review
Biochemistry & Molecular Biology
Daniel Hilger
Summary: G protein-coupled receptors (GPCRs) are crucial for human physiology regulation and recent research has revealed their high dynamics and ability to sample multiple conformational states in response to different ligands, impacting complex signaling behavior.
