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GPCRs Regulate Adenylyl Cylase Activity

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...

Diversity in Cell Signaling Responses

Diversity in Cell Signaling Responses

The physiological function of a cell and cellular communication are outcomes of a range of extrinsic signals, intracellular signaling pathways, and cellular responses. No two cell types express the same repertoire of signaling components. Receptors are highly selective for their cognate ligands, but once activated, they can alter multiple cellular processes such as DNA transcription, protein synthesis, and metabolic activity.
Graded and Abrupt Responses
Some signaling systems generate...

GPCR Desensitization

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...

Assembly of Signaling Complexes

Assembly of Signaling Complexes

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,...

G-protein Coupled Receptors

G-protein Coupled Receptors

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.

G-protein Coupled Receptors

G-protein Coupled Receptors

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.

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Updated: May 9, 2026

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

Published on: September 10, 2016

GPCRシグナル伝達における精度と柔軟性

Matthias Elgeti¹, Alexander S Rose, Franz J Bartl

¹Institut für Medizinische Physik und Biophysik (CC2), Charité-Universitätsmedizin Berlin, Charitéplatz 1, 10117 Berlin, Germany. matthias.elgeti@charite.de

Journal of the American Chemical Society

|July 26, 2013

まとめ

この要約は機械生成です。

ロドプシン (Rhodopsin) とはロドプシン (Rhodopsin) とはロドプシン (Rhodopsin) とは

さらに関連する動画

Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay

Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay

Published on: March 10, 2020

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

関連する実験動画

Last Updated: May 9, 2026

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

Published on: September 10, 2016

Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay

Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay

Published on: March 10, 2020

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

科学分野:

バイオケミストリーバイオケミストリー
分子生物学は分子生物学である.
構造生物学構造生物学とは

背景:

ロドプシンのようなGタンパク質結合受容体 (GPCR) は,信号伝達に不可欠です.
ロドプシンの光活性化状態は,網膜の棒細胞における迅速かつ正確な信号伝達を可能にします.

研究の目的:

ロドプシンとトランスデューシンとの相互作用の構造動態を調査する.
ロドプシンからトランスデューシンへの高速で高精度な信号伝達のメカニズムを解明する.

主な方法:

フーリエ変換赤外線 (FTIR) スペクトロスコーピーは,タンパク質の構成状態を研究するために使用されます.
膜環境でロドプシンをモデル化するための全原子分子動力学 (MD) シミュレーション.
合成GtγおよびGtαサブユニットのC端ペプチドがロドプシン構成に及ぼす影響の分析.

主要な成果:

FTIRは,保存されたモチーフ (E(D) RYとYx7K(R)) が,ロドプシンの不活性および活性状態を調節することを明らかにしました.
MDシミュレーションでは,本質的に構造化されていないループ (CL3) とコンフォメーションサブステートが特定されました.
GγCTはCL3の柔軟性を保ちながら活性状態を安定させ,GαCTは螺旋型のCL3置換物を安定させました.

結論:

ロドプシン/トランスデューシンを素早く,正確に結合させるためのメカニズムが提案され,段階的な形状的空間縮小を伴う.
保存されたアミノ酸残基は,このメカニズムにおいて重要な役割を果たします.
提案されたメカニズムは,他のGPCR/Gタンパク質相互作用に一般化することができる.