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Related Concept Videos

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.

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Related Experiment Video

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

Multivalent peptidomimetic conjugates: a versatile platform for modulating androgen receptor activity.

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
Summary

Researchers developed novel multivalent peptidomimetic conjugates to modulate androgen receptor (AR) activity. These conjugates show potent anti-proliferative effects in therapy-resistant prostate cancer models, offering new therapeutic strategies.

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08:47

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

Published on: March 6, 2019

Area of Science:

  • Medicinal Chemistry
  • Molecular Biology
  • Oncology

Background:

  • The androgen receptor (AR) is a key target in prostate cancer therapy.
  • Therapy-resistant prostate cancer remains a significant clinical challenge.
  • Developing novel AR modulators is crucial for improved treatment outcomes.

Purpose of the Study:

  • To design and synthesize novel multivalent peptidomimetic conjugates targeting the androgen receptor.
  • To evaluate the anti-proliferative activity of these conjugates in prostate cancer cells.
  • To elucidate the mechanism of action of the developed AR modulators.

Main Methods:

  • Conjugation of bioactive ethisterone ligands to sequence-specific peptoid oligomers.
  • Assessment of AR-mediated transcriptional activation.
  • Evaluation of anti-proliferative activity in LNCaP-abl cells (a model for therapy-resistant prostate cancer).
  • In vitro ligand-binding assays to determine competitive or non-competitive inhibition.

Main Results:

  • A family of multivalent peptidomimetic conjugates targeting the androgen receptor was successfully synthesized.
  • Certain conjugates demonstrated enhanced AR-mediated transcriptional activation.
  • A linear conjugate exhibited competitive inhibition of AR ligand binding and anti-proliferative activity.
  • A cyclic conjugate showed potent anti-proliferative activity via a non-competitive mechanism.

Conclusions:

  • The developed peptidomimetic conjugates represent a versatile platform for designing novel AR modulators.
  • Both competitive and non-competitive AR modulators with therapeutic potential were identified.
  • These findings offer promising strategies for targeting therapy-resistant prostate cancer.