Related Experiment Video
Updated: Dec 27, 2025
10:12
Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
Published on: September 19, 2022
2.6K
Conformationally constrained peptides for drug delivery
Gaurav Jerath1, Ruchika Goyal1, Vishal Trivedi2
1Molecular Informatics and Design Laboratory, Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati, Guwahati, India.
Summary
New cationic helical amphipathic peptides (CHAPs) show promise for targeted drug delivery. These cell-penetrating peptides (CPPs) effectively deliver methotrexate to cancer cells, enhancing toxicity while sparing healthy cells.
Area of Science:
- Nanomedicine
- Biochemistry
- Drug Delivery
Background:
- Peptides serve as versatile carriers in nanomedicine for targeted drug delivery.
- Cell-penetrating peptides (CPPs) facilitate cellular uptake via multiple mechanisms.
- Many CPPs transition from disordered to helical structures upon cell membrane interaction, crucial for penetration.
Purpose of the Study:
- To design and evaluate novel cationic helical amphipathic peptides (CHAPs) as drug delivery platforms.
- To assess the cancer cell penetration and drug delivery capabilities of CHAPs.
- To investigate the therapeutic efficacy and selectivity of CHAP-drug conjugates.
Main Methods:
- Synthesis of topologically constrained helical cationic amphipathic peptides (CHAPs).
- Evaluation of cellular uptake of CHAPs in cervical and breast cancer cell lines.
- Assessment of drug delivery efficiency using methotrexate (MTX) as a model drug, forming CHAP-MTX conjugates.
- Comparative toxicity studies of CHAP-MTX conjugates versus free MTX on cancer and normal cell lines (HEK-293).
Main Results:
- CHAP peptides demonstrated temperature and energy-independent cellular uptake.
- The peptides exhibited biocompatibility in bovine serum.
- CHAP-MTX conjugates successfully delivered functional methotrexate into cancer cells.
- CHAP-MTX conjugates showed enhanced toxicity against cancer cells compared to MTX alone.
- CHAP-MTX conjugates exhibited reduced toxicity towards HEK-293 cells, indicating cancer cell selectivity.
Conclusions:
- Cationic helical amphipathic peptides (CHAPs) are effective carriers for targeted drug delivery in nanomedicine.
- CHAP-MTX conjugates offer a promising strategy for enhanced cancer therapy with improved selectivity.
- The design of constrained helical peptides represents a viable approach for developing advanced drug delivery systems.
Related Concept Videos
01:25Protein Folding
10.7K
Proteins are chains of amino acids linked together by peptide bonds. Upon synthesis, a protein folds into a three-dimensional conformation, critical to its biological function. Interactions between its constituent amino acids guide protein folding, and hence the protein structure is primarily dependent on its amino acid sequence.
Protein Structure Is Critical to Its Biological Function
Proteins perform a wide range of biological functions such as catalyzing chemical reactions, providing...
Protein Structure Is Critical to Its Biological Function
Proteins perform a wide range of biological functions such as catalyzing chemical reactions, providing...
10.7K
02:43Peptide Bonds
81.5K
A peptide bond covalently attaches amino acids through a dehydration reaction. One amino acid's carboxyl group and another amino acid's amino group combine, releasing a water molecule. The resulting bond is the peptide bond. The products that such linkages form are peptides. As more amino acids join this growing chain, the resulting chain is a polypeptide. Each polypeptide has a free amino group at one end. This end has the N-terminal, or the amino-terminal, and the other end has a free...
81.5K
01:49Conserved Binding Sites
5.0K
Many proteins’ biological role depends on their interactions with their ligands, small molecules that bind to specific locations on the protein known as ligand-binding sites. Ligand-binding sites are often conserved among homologous proteins as these sites are critical for protein function.
Binding sites are often located in large pockets, and if their location on a protein’s surface is unknown, it can be predicted using various approaches. The energetic method computationally...
Binding sites are often located in large pockets, and if their location on a protein’s surface is unknown, it can be predicted using various approaches. The energetic method computationally...
5.0K