Related Experiment Video
Updated: Feb 18, 2026

Constructing Thioether/Vinyl Sulfide-tethered Helical Peptides Via Photo-induced Thiol-ene/yne Hydrothiolation
Published on: August 1, 2018
Structure-based design for binding peptides in anti-cancer therapy
1Institute of Stem Cell and Translational Cancer Research, Chang Gung Memorial Hospital at Linkou, Chang Gung University, Taoyuan 333, Taiwan.
Abstract:
The conventional anticancer therapeutics usually lack cancer specificity, leading to damage of normal tissues that patients find hard to tolerate. Ideally, anticancer therapeutics carrying payloads of drugs equipped with cancer targeting peptides can act like "guided missiles" with the capacity of targeted delivery toward many types of cancers. Peptides are amenable for conjugation to nano drugs for functionalization, thereby improving drug delivery and cellular uptake in cancer-targeting therapies. Peptide drugs are often more difficult to design through molecular docking and in silico analysis than small molecules, because peptide structures are more flexible, possess intricate molecular conformations, and undergo complex interactions. In this review, the development and application of strategies for structure-based design of cancer-targeting peptides against GRP78 are discussed. This Review also covers topics related to peptide pharmacokinetics and targeting delivery, including molecular docking studies, features that provide advantages for in vivo use, and properties that influence the cancer-targeting ability. Some advanced technologies and special peptides that can overcome the pharmacokinetic challenges have also been included.
Insights
Developing targeted cancer therapies using peptides offers a promising "guided missile" approach. This review explores structure-based peptide design for enhanced drug delivery and specificity against GRP78, improving cancer treatment outcomes.
Area of Science:
- Oncology
- Drug Discovery
- Biotechnology
Background:
- Conventional anticancer therapeutics often lack specificity, causing damage to normal tissues and limiting patient tolerance.
- Targeted delivery systems, such as peptides conjugated to nano drugs, can improve specificity and efficacy in cancer treatment.
Purpose of the Study:
- To review strategies for the structure-based design of cancer-targeting peptides against GRP78.
- To discuss peptide pharmacokinetics, targeting delivery, and features advantageous for in vivo applications.
Main Methods:
- Exploration of structure-based design principles for peptide therapeutics.
- Analysis of molecular docking and in silico methods for peptide drug development.
- Review of pharmacokinetic properties and targeting capabilities of cancer-specific peptides.
Main Results:
- Peptides can be functionalized with nano drugs for improved drug delivery and cellular uptake in cancer cells.
- Structure-based design strategies are crucial for overcoming the complexities of peptide drug development.
- Advanced technologies and specialized peptides show potential in addressing pharmacokinetic challenges for in vivo use.
Conclusions:
- Structure-based design of cancer-targeting peptides, particularly against GRP78, is a viable strategy for developing more specific and effective anticancer therapeutics.
- Optimizing peptide pharmacokinetics and targeting delivery is essential for successful in vivo application and improved patient outcomes.
Related Concept Videos
Ligand Binding Sites
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...
Ligand Binding Sites
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
Conserved Binding Sites
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...
Targeted Cancer Therapies
There are several types of targeted therapies against...

