Related Experiment Video
Updated: Jan 18, 2026
07:41
A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
9.4K
Physiological functions and structural features of Gα12/13 proteins.
Sabriye Aydoğdu1, Anna Pepanian1, Dhruv C Rathod1
1Pharmaceutical Biochemistry and Bioanalytics, Pharmaceutical Institute, University of Bonn, Bonn 53121, Germany.
Biomedicine & Pharmacotherapy = Biomedecine & Pharmacotherapie
|September 7, 2025
Summary
Heterotrimeric G proteins (GPCRs) are key signal transducers. This review focuses on the understudied Gα12/13 family, highlighting its role in cell functions and disease pathogenesis.
Area of Science:
- Molecular Biology
- Cell Signaling
- Biochemistry
Background:
- Heterotrimeric G proteins mediate cellular responses to extracellular signals via G protein-coupled receptors (GPCRs).
- G protein signaling is diverse, with Gα subunits classifying into four families: Gαs/olf, Gαi/o, Gαq/11, and Gα12/13.
- The Gα12/13 family's signaling pathways are less understood compared to other Gα families.
Purpose of the Study:
- To review current knowledge on the Gα12/13 signaling pathways and structural properties.
- To emphasize the importance of further research into the Gα12/13 family for understanding its physiological roles.
- To identify knowledge gaps concerning the Gα12/13 family's signaling mechanisms and structure.
Main Methods:
- Literature review of existing research on Gα12/13 proteins.
- Analysis of studies investigating Gα12/13 interactions with Rho GTPases.
- Synthesis of findings related to Gα12/13 involvement in physiological processes and disease.
Main Results:
- The Gα12/13 family regulates critical cellular functions including cell migration, adhesion, and cytoskeletal dynamics.
- Dysregulation of Gα12/13 is linked to diseases such as asthma, cardiovascular disorders, and cancer.
- Significant gaps remain in understanding the detailed signaling cascades and structural characteristics of Gα12/13.
Conclusions:
- The Gα12/13 family plays a vital role in numerous physiological processes and disease pathogenesis.
- Further investigation into Gα12/13 signaling and structure is crucial for therapeutic target identification.
- Comprehensive characterization of Gα12/13 is essential for advancing drug discovery efforts.
Related Concept Videos
01:22Activation and Inactivation of G Proteins
11.1K
Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high...
11.1K
01:30Transducer Mechanism: G Protein–Coupled Receptors
4.0K
G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
GPCRs are also called heptahelical,...
4.0K
01:30Assembly of Signaling Complexes
6.5K
Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
6.5K
01:15G Protein-coupled Receptors
16.6K
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
16.6K
01:21G-protein Coupled Receptors
131.6K
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
131.6K
01:21G-Protein Gated Ion Channels
5.6K
GPCRs are primarily responsible for our sense of smell, taste, and vision. The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
Sensory...
5.6K