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Related Concept Videos

Amplifying Signals via Enzymatic Cascade01:22

Amplifying Signals via Enzymatic Cascade

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When a ligand binds to a cell-surface receptor, the receptor's intracellular domain changes shape, which may either activate its enzyme function or allow its binding to other molecules. The initial signal is amplified by most signal transduction pathways. This means that a single ligand molecule can activate multiple molecules of a downstream target. Proteins that relay a signal are most commonly phosphorylated at one or more sites, activating or inactivating the protein. Kinases catalyze...
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Assembly of Signaling Complexes01:30

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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,...
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Interactions Between Signaling Pathways01:19

Interactions Between Signaling Pathways

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Signaling cascades usually lack linearity. Multiple pathways interact and regulate one another, allowing cells to integrate and respond to diverse environmental stimuli.
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Signal Transduction: Overview01:26

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Cells respond to many types of information, often through receptor proteins positioned on the membrane. They respond to chemical signals, such as hormones, neurotransmitters, and other signaling molecules, initiating a series of molecular reactions to produce an appropriate response. This is called signal transduction. Cells also coordinate different responses elicited by the same signaling molecule via mediators, allowing molecular cross-talk.
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Intracellular Signaling Cascades01:24

Intracellular Signaling Cascades

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Once a ligand binds to a receptor, the signal is transmitted through the membrane and into the cytoplasm. The continuation of a signal in this manner is called signal transduction. Signal transduction only occurs with cell-surface receptors, which cannot interact with most components of the cell, such as DNA. Only internal receptors can interact directly with DNA in the nucleus to initiate protein synthesis. When a ligand binds to its receptor, conformational changes occur that affect the...
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Transducer Mechanism: Enzyme-Linked Receptors01:27

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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:
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Related Experiment Video

Updated: Dec 13, 2025

Mimicking the Function of Signaling Proteins: Toward Artificial Signal Transduction Therapy
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Mimicking the Function of Signaling Proteins: Toward Artificial Signal Transduction Therapy

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Targeting signal transduction with large combinatorial collections.

Douglas S Auld1, David Diller, Koc-Kan Ho

  • 1Pharmacopeia, Box 5350, Princeton, NJ 08543, USA. dauld@pharmacop.com

Drug Discovery Today
|January 28, 2003
PubMed
Summary

Combinatorial chemistry aids drug discovery by screening vast compound libraries against novel genomic targets. This review explores selecting effective compounds for signal transduction pathways.

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Area of Science:

  • Drug discovery and development
  • Medicinal chemistry
  • Genomics and proteomics

Background:

  • Combinatorial chemistry has been applied to drug discovery for over a decade.
  • The field faces a post-genomic era with numerous protein targets and massive compound libraries.
  • Drug screening paradigms have been significantly altered by these advancements.

Purpose of the Study:

  • To review the practices and applications of selecting specific compounds from large chemical libraries.
  • To focus on compounds targeting proteins involved in signal transduction pathways.

Main Methods:

  • Literature review of combinatorial chemistry applications in drug discovery.
  • Analysis of strategies for selecting compounds from large chemical libraries.
  • Examination of screening paradigms in the context of genomic targets.

Main Results:

  • The growth of chemical libraries and genomic targets necessitates new screening approaches.
  • The ability to screen millions of compounds against single targets presents both opportunities and challenges.
  • Effective selection of compounds targeting signal transduction pathways is crucial.

Conclusions:

  • The drug discovery industry must adapt to a complex post-genomic landscape.
  • Strategic compound selection is vital for identifying effective drug candidates.
  • Signal transduction pathways remain a key focus for therapeutic intervention.