Jove
Visualize
お問い合わせ
JoVE
x logofacebook logolinkedin logoyoutube logo
JoVEについて
概要リーダーシップブログJoVEヘルプセンター
著者向け
出版プロセス編集委員会範囲と方針査読よくある質問投稿
図書館員向け
推薦の声購読アクセスリソース図書館諮問委員会よくある質問
研究
JoVE JournalMethods CollectionsJoVE Encyclopedia of Experimentsアーカイブ
教育
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab Manual教員リソースセンター教員サイト
利用規約
プライバシーポリシー
ポリシー

関連する概念動画

Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
The Two-State Receptor Model01:29

The Two-State Receptor Model

The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with one...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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...
Internal Receptors01:31

Internal Receptors

Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
Drug-Receptor Interactions01:29

Drug-Receptor Interactions

Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.

こちらも読む

関連記事

共著者、ジャーナル、引用グラフによってこの研究に関連する記事。

並び替え
Same author

<i>In Vivo</i> Activity of Antimicrobial Peptoid Oligomers against HSV-1 in a Mouse Model of Herpes Labialis.

ACS infectious diseases·2026
Same author

MDM2 suppresses c-Myc synthesis by binding to the 5' mRNA translation regulatory sequence.

Proceedings of the National Academy of Sciences of the United States of America·2026
Same author

YAP/TAZ inhibition refines TGF-β signaling to prevent laryngeal fibrosis.

bioRxiv : the preprint server for biology·2026
Same author

Quantitative holographic agglutination assay for immunoglobulin A.

Biomedical optics express·2026
Same author

Structural and Positional Effects of Peptoid Residues on Triple Helix Stability.

Biomacromolecules·2026
Same author

Native Chemical Ligation of Peptoid Oligomers.

Biochemistry·2026

関連する実験動画

Updated: May 23, 2026

Initial Evaluation of Antibody-conjugates Modified with Viral-derived Peptides for Increasing Cellular Accumulation and Improving Tumor Targeting
11:58

Initial Evaluation of Antibody-conjugates Modified with Viral-derived Peptides for Increasing Cellular Accumulation and Improving Tumor Targeting

Published on: March 8, 2018

多価ペプチドミメティック結合体:アンドロゲン受容体の活性を調節するための多用途のプラットフォーム.

Paul M Levine1, Keren Imberg, Michael J Garabedian

  • 1Department of Chemistry, New York University, New York, New York 10003, USA.

Journal of the American Chemical Society
|April 19, 2012
PubMed
まとめ

研究者らは,アンドロゲン受容体 (AR) の活性を調節する新しい多価ペプチドミメティック結合体を開発した. これらの結合体は,治療に抵抗する前立腺がんのモデルにおいて強力な抗増殖効果を示し,新しい治療戦略を提供している.

さらに関連する動画

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
10:36

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues

Published on: March 21, 2017

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
08:47

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates

Published on: March 6, 2019

関連する実験動画

Last Updated: May 23, 2026

Initial Evaluation of Antibody-conjugates Modified with Viral-derived Peptides for Increasing Cellular Accumulation and Improving Tumor Targeting
11:58

Initial Evaluation of Antibody-conjugates Modified with Viral-derived Peptides for Increasing Cellular Accumulation and Improving Tumor Targeting

Published on: March 8, 2018

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
10:36

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues

Published on: March 21, 2017

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
08:47

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates

Published on: March 6, 2019

科学分野:

  • 薬用化学 薬用化学について
  • 分子生物学は分子生物学である.
  • 腫瘍学 腫瘍学

背景:

  • アンドロゲン受容体 (AR) は前立腺がん治療の重要な標的である.
  • 治療に抵抗性のある前立腺がんは,依然として重要な臨床的課題です.
  • 新種のAR調節器の開発は,治療結果の改善に不可欠です.

研究 の 目的:

  • アンドロゲン受容体を標的とする新しい多価ペプチドミメティック結合体を設計・合成する.
  • 前立腺がん細胞におけるこれらの結合体の抗増殖活性を評価する.
  • 開発されたAR調節器の作用メカニズムを解明する.

主な方法:

  • 生物活性エチステロンリガンドを配列固有のペプトイドオリゴーマーに結合する.
  • AR媒介による転写活性化の評価.
  • LNCaP-abl細胞 (治療に抵抗性のある前立腺がんのモデル) の抗増殖活性の評価.
  • 競争的または非競争的阻害を決定するためのインビトロリガンド結合測定法.

主要な成果:

  • アンドロゲン受容体を標的にする多価ペプチドミメティック結合体の一族が成功裏に合成されました.
  • 特定のコンジュガートは,AR媒介によるトランスクリプション活性化の強化を示した.
  • 線形結合剤は,ARリガンド結合と抗増殖活性に対する競争的阻害を示した.
  • 周期性コンジュガートは,非競争的メカニズムを通じて強力な反増殖活性を示した.

結論:

  • 開発されたペプチドミメティック結合体は,新しいAR調節器を設計するための汎用性のあるプラットフォームを表しています.
  • 治療的可能性のある競争力のあるAR調節剤と非競争力のあるAR調節剤の両方が特定されました.
  • これらの発見は,治療に抵抗する前立腺がんを標的とした有望な戦略を提供します.