Adenylyl cyclase ≈ Adenylyl cyclase
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cAMP signalling in insulin and glucagon secretion Open
The “second messenger” archetype cAMP is one of the most important cellular signalling molecules with central functions including the regulation of insulin and glucagon secretion from the pancreatic β‐ and α‐cells, respectively. cAMP is ge…
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Deletion of Type 3 Adenylyl Cyclase Perturbs the Postnatal Maturation of Olfactory Sensory Neurons and Olfactory Cilium Ultrastructure in Mice Open
Type 3 adenylyl cyclase (Adcy3) is localized to the cilia of olfactory sensory neurons (OSNs) and is an essential component of the olfactory cyclic adenosine monophosphate (cAMP) signaling pathway. Although the role of this enzyme in odor …
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Emerging Role of cAMP/AMPK Signaling Open
The 5′-Adenosine monophosphate (AMP)-activated protein kinase (AMPK) is a natural energy sensor in mammalian cells that plays a key role in cellular and systemic energy homeostasis. At the cellular level, AMPK supports numerous processes r…
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Cyclic di‐AMP mediates biofilm formation Open
Summary Cyclic di‐ AMP (c‐di‐ AMP ) is an emerging second messenger in bacteria. It has been shown to play important roles in bacterial fitness and virulence. However, transduction of c‐di‐ AMP signaling in bacteria and the role of c‐di‐ A…
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The Lactate Receptor HCAR1 Modulates Neuronal Network Activity through the Activation of G<sub>α</sub> and G<sub>βγ</sub> Subunits Open
The discovery of a G-protein-coupled receptor for lactate named hydroxycarboxylic acid receptor 1 (HCAR1) in neurons has pointed to additional nonmetabolic effects of lactate for regulating neuronal network activity. In this study, we char…
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A<sub>3</sub>Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy Open
The A 3 adenosine receptor (A 3 AR) subtype is a novel, promising therapeutic target for inflammatory diseases, such as rheumatoid arthritis (RA) and psoriasis, as well as liver cancer. A 3 AR is coupled to inhibition of adenylyl cyclase a…
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The structure of a membrane adenylyl cyclase bound to an activated stimulatory G protein Open
The architecture of a signaling hub Adenylyl cyclases (ACs) respond to a variety of inputs to generate the signaling molecule cyclic adenosine monophosphate. ACs are regulated by G proteins, which are activated by upstream receptors. Qi et…
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G-Protein–Coupled Receptor MrgD Is a Receptor for Angiotensin-(1–7) Involving Adenylyl Cyclase, cAMP, and Phosphokinase A Open
Angiotensin (Ang)-(1–7) has cardiovascular protective effects and is the opponent of the often detrimental Ang II within the renin–angiotensin system. Although it is well accepted that the G-protein–coupled receptor Mas is a receptor for t…
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The Role of Zinc in Male Fertility Open
Several studies proposed the importance of zinc ion in male fertility. Here, we describe the properties, roles and cellular mechanisms of action of Zn2+ in spermatozoa, focusing on its involvement in sperm motility, capacitation and acroso…
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Global and local missions of cAMP signaling in neural plasticity, learning, and memory Open
The fruit fly Drosophila melanogaster has been a popular model to study cAMP signaling and resultant behaviors due to its powerful genetic approaches. All molecular components (AC, PDE, PKA, CREB, etc) essential for cAMP signaling have bee…
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Olfactory Receptors in Non-Chemosensory Organs: The Nervous System in Health and Disease Open
Olfactory receptors (ORs) and down-stream functional signaling molecules adenylyl cyclase 3 (AC3), olfactory G protein α subunit (Gαolf), OR transporters receptor transporter proteins 1 and 2 (RTP1 and RTP2), receptor expression enhancing …
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Controlling fertilization and cAMP signaling in sperm by optogenetics Open
Optogenetics is a powerful technique to control cellular activity by light. The light-gated Channelrhodopsin has been widely used to study and manipulate neuronal activity in vivo, whereas optogenetic control of second messengers in vivo h…
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Physiological roles of mammalian transmembrane adenylyl cyclase isoforms Open
Adenylyl cyclases (ACs) catalyze the conversion of ATP to the ubiquitous second messenger cAMP. Mammals possess nine isoforms of transmembrane ACs, dubbed AC1–9, that serve as major effector enzymes of G protein-coupled receptors (GPCRs). …
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Endothelial CD99 signals through soluble adenylyl cyclase and PKA to regulate leukocyte transendothelial migration Open
CD99 is a critical regulator of leukocyte transendothelial migration (TEM). How CD99 signals during this process remains unknown. We show that during TEM, endothelial cell (EC) CD99 activates protein kinase A (PKA) via a signaling complex …
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The Molecular Basis for Specificity at the Level of the Protein Kinase a Catalytic Subunit Open
Assembly of multi enzyme complexes at subcellular localizations by anchoring- and scaffolding proteins represents a pivotal mechanism for achieving spatiotemporal regulation of cellular signaling after hormone receptor targeting [for revie…
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Serotonin activates glycolysis and mitochondria biogenesis in human breast cancer cells through activation of the Jak1/STAT3/ERK1/2 and adenylate cyclase/PKA, respectively Open
Background Although produced by several types of tumours, the role of serotonin on cancer biology is yet to be understood. Methods The effects of serotonin (5-HT) on human breast cancer cells proliferation, signalling pathways and metaboli…
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Essential Control of the Function of the Striatopallidal Neuron by Pre-coupled Complexes of Adenosine A2A-Dopamine D2 Receptor Heterotetramers and Adenylyl Cyclase Open
The central adenosine system and adenosine receptors play a fundamental role in the modulation of dopaminergic neurotransmission. This is mostly achieved by the strategic co-localization of different adenosine and dopamine receptor subtype…
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Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor Open
Selective activation of dopamine D1 receptors (D1Rs) has been pursued for 40 years as a therapeutic strategy for neurologic and psychiatric diseases due to the fundamental role of D1Rs in motor function, reward processing, and cognition. A…
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Cyclic AMP signalling controls key components of malaria parasite host cell invasion machinery Open
Cyclic AMP (cAMP) is an important signalling molecule across evolution, but its role in malaria parasites is poorly understood. We have investigated the role of cAMP in asexual blood stage development of Plasmodium falciparum through condi…
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New perspectives in signaling mediated by receptors coupled to stimulatory G protein: the emerging significance of cAMP efflux and extracellular cAMP-adenosine pathway Open
G protein-coupled receptors (GPCRs) linked to stimulatory G (Gs) proteins (GsPCRs) mediate increases in intracellular cyclic AMP as consequence of activation of nine adenylyl cyclases , which differ considerably in their cellular distribut…
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Control of glutamate release by complexes of adenosine and cannabinoid receptors Open
Background It has been hypothesized that heteromers of adenosine A 2A receptors (A2AR) and cannabinoid CB 1 receptors (CB1R) localized in glutamatergic nerve terminals mediate the integration of adenosine and endocannabinoid signaling invo…
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Expression and functions of adenylyl cyclases in the CNS Open
Adenylyl cyclases (ADCYs), by generating second messenger cAMP, play important roles in various cellular processes. Their expression, regulation and functions in the CNS, however, remain largely unknown. In this review, we first introduce …
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The Orphan G Protein-coupled Receptor GPR17 Negatively Regulates Oligodendrocyte Differentiation via Gαi/o and Its Downstream Effector Molecules Open
Recent studies have recognized G protein-coupled receptors as important regulators of oligodendrocyte development. GPR17, in particular, is an orphan G protein-coupled receptor that has been identified as oligodendroglial maturation inhibi…
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Extracellular vesicles direct migration by synthesizing and releasing chemotactic signals Open
Chemotactic signals are relayed to neighboring cells through the secretion of additional chemoattractants. We previously showed in Dictyostelium discoideum that the adenylyl cyclase A, which synthesizes the chemoattractant cyclic adenosine…
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Structure and function of adenylyl cyclases, key enzymes in cellular signaling Open
The adenylyl cyclases (ACs) catalyze the production of the ubiquitous second messenger, cAMP, which in turns acts on a number of effectors and thus regulates a plethora of cellular functions. As the key enzymes in the highly evolutionarily…
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CBD Effects on TRPV1 Signaling Pathways in Cultured DRG Neurons Open
CBD at low doses corresponding to plasma concentrations observed physiologically inhibits or desensitizes neuronal TRPV1 signalling by inhibiting the adenylyl cyclase - cAMP pathway, which is essential for maintaining TRPV1 phosphorylation…
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Convergence of adenosine and GABA signaling for synapse stabilization during development Open
Synapse stabilization Early in brain development, neurons connect to each other enthusiastically. With development, an overabundance of synapses is winnowed down to refine efficiently connected circuits. Inactive synapses are prime targets…
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Neomorphic effects of recurrent somatic mutations in <i>Yin Yang 1</i> in insulin-producing adenomas Open
Significance The identical recurrent somatic heterozygous missense mutation in the DNA-binding domain of transcription factor YY1 is found in a third of insulin-secreting pancreatic tumors. This mutation alters sites involved in DNA contac…
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Discovery, Synthesis, and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ-Opioid Receptor Open
Allosteric modulators of G protein-coupled receptors (GPCRs) have a number of potential advantages compared to agonists or antagonists that bind to the orthosteric site of the receptor. These include the potential for receptor selectivity,…
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Sensing Positive versus Negative Reward Signals through Adenylyl Cyclase-Coupled GPCRs in Direct and Indirect Pathway Striatal Medium Spiny Neurons Open
Transient changes in striatal dopamine (DA) concentration are considered to encode a reward prediction error (RPE) in reinforcement learning tasks. Often, a phasic DA change occurs concomitantly with a dip in striatal acetylcholine (ACh), …