Receptor-ligand interactions for optimized endocytosis in targeted therapies

Yejin Sung1, Youngjin Choi1, Eun Sun Kim2

  • 1Medicinal Materials Research Center, Biomedical Research Institute, Korea Institute of Science and Technology (KIST), Seoul 02792, Republic of Korea.

Insights

Receptor-mediated endocytosis is key for drug development, controlling how therapies enter cells. Understanding receptor-ligand interactions allows precise control over cellular trafficking for enhanced therapeutic efficacy.

Area of Science:

  • Cell biology
  • Pharmacology
  • Drug development

Background:

  • Receptor-mediated endocytosis is vital for drug delivery and efficacy.
  • Ligand binding to receptors initiates cellular uptake and intracellular trafficking.
  • Endosomal sorting determines if complexes are degraded or recycled, impacting therapy outcomes.

Purpose of the Study:

  • To review receptor-ligand interactions as modulators of endocytosis.
  • To emphasize their role in therapeutic design and efficacy.
  • To bridge endocytosis mechanisms with innovative therapeutic strategies.

Main Methods:

  • Review of scientific literature on receptor-mediated endocytosis.
  • Analysis of receptor-ligand interactions in therapeutic contexts.
  • Examination of advanced therapeutic platforms utilizing endocytosis.

Main Results:

  • Receptor-ligand interactions precisely control endocytosis, influencing therapeutic design.
  • Optimized ligands enable tailored control over internalization and trafficking.
  • Strategies like ADCs and TPD platforms leverage endocytosis for enhanced efficacy.

Conclusions:

  • Understanding endocytosis mechanisms is crucial for advancing precision medicine.
  • Targeted control of endosomal sorting can improve therapeutic outcomes.
  • Future drug development can be significantly enhanced by leveraging receptor-mediated endocytosis insights.

Related Concept Videos

Receptor-mediated Endocytosis01:20

Receptor-mediated Endocytosis

Receptor-mediated endocytosis is when bulk amounts of specific molecules are imported into a cell after binding to cell surface receptors. The molecules bound to these receptors are taken into the cell through inward folding of the cell surface membrane, which is eventually pinched off into a vesicle within the cell. Structural proteins, such as clathrin, coat the budding vesicle.
Clathrin-Mediated Endocytosis of LDL
One well-characterized example of receptor-mediated endocytosis is the...
6.0K
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:
2.3K
Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
12.7K
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....
4.8K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
7.4K
The Early Endosome: Endocytosis of Transferrin01:28

The Early Endosome: Endocytosis of Transferrin

Essential proteins such as insulin or low-density lipoprotein (LDL) and micronutrients such as iron enter a eukaryotic cell through receptor-mediated endocytosis. Subsequently, the early endosomes fuse with the vesicles containing such receptor-ligand complexes and play a vital role in sorting the incoming ligands and receptors. While the ligands are either degraded inside the vesicle or released into the cytosol, their receptors are returned to the plasma membrane for further rounds of...
3.2K