Related Experiment Video
Updated: May 25, 2026
06:01
Extracellular Protein Microarray Technology for High Throughput Detection of Low Affinity Receptor-Ligand Interactions
Published on: January 7, 2019
Peptide-receptor ligands and multivalent approach.
Paolo Ruzza1, Anna Marchiani, Nicola Antolini
1Institute of Biomolecular Chemistry of CNR, Padova Unit, via Marzolo 1, 35131 Padova, Italy. paolo.ruzza@unipd.it
Anti-Cancer Agents in Medicinal Chemistry
|February 2, 2012
Summary
Targeting peptide ligands, overexpressed in tumors, offer promising cancer imaging and therapy. Advances in peptide synthesis and radiolabeling enable development of targeted radiopharmaceuticals for improved cancer treatment.
Area of Science:
- Oncology
- Radiopharmaceutical Chemistry
- Molecular Imaging
Background:
- Overexpressed peptide receptors on human tumors present therapeutic and diagnostic targets.
- Peptide-ligands are attractive for targeted cancer imaging and therapy.
- Radiopharmaceuticals combine bioactive peptides with radionuclides for targeted delivery.
Purpose of the Study:
- To review principal receptor-binding peptides and their tumor cell overexpression.
- To discuss advantages and challenges in developing multivalent peptide-based ligands.
- To summarize design strategies and applications of peptide-based ligands in oncology.
Main Methods:
- Review of scientific literature on receptor-binding peptides.
- Analysis of peptide synthesis, phage display, and combinatorial chemistry techniques.
- Examination of bifunctional chelating agents and radiolabeling methods.
Main Results:
- Identified key receptor-binding peptides overexpressed on various tumor cells.
- Highlighted advancements in peptide-based ligand development through modern synthesis and display technologies.
- Demonstrated the utility of radiolabeled peptides in diagnostic imaging and therapeutic applications.
Conclusions:
- Peptide-ligands are valuable tools for targeted cancer diagnostics and therapeutics.
- Multivalent peptide designs offer enhanced targeting but present development challenges.
- Continued research in peptide chemistry and radiolabeling will advance targeted cancer medicine.
More Related Videos
Related Concept Videos
01:27Transducer 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:
Major types that are helpful drug targets include:
01:29The 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...
The binding affinity of a drug determines its interaction with one...
01:15G 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...
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...
01:30Spare Receptors
Some receptors remain unoccupied even when an agonist produces a maximal response. Such empty ones are called spare receptors. In presence of spare receptors the maximum effect of an agonist drug is achieved with fewer than 100% of the receptors being occupied. To determine the presence of spare receptors, scientists often compare the concentration of the drug needed to produce 50% of the maximum effect (EC50) with the concentration of the drug needed to occupy 50% of the receptors (Kd). If the...
02:40Ligand 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...
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...
00:49Ligand Binding and Linkage
Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked. In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence the...