Drug delivery explores the utilization of technologies that transport drugs to theirintended target site.
Compared with small molecules and proteins, peptides offer improved
biocompatibility, reduced cost, tunable bioactivity, specific targeting, ease ofsynthesis and modification, making them highly promising for the development ofnovel drug delivery systems[1, 2].

To achieve the desired therapeutic effects, various aspects of peptides have been
introduced into drug delivery systems, such as targeting peptides, cell-penetrating
peptides, and responsive peptides. Peptide-based drug delivery systems have gainedwidespread uses in the form of peptide-drug conjugates, injectable biodegradable
particles, and depots for effectively delivering therapeutic agents[2].

Figure 1. Mechanisms of cellular delivery of three
typical peptide-based drug delivery systems[2].

CS Products
Category

Product Name

Description(Arg)9 Acetate

A cell-penetrating peptide made up of 9
arginine residues.

TAT (48-57)

A cell-penetrating peptide derived from HIV-1
transactivator of transcription (Tat) protein
residue 48-57.

Penetratin

A cell-penetrating peptide derived from theamphiphilic Drosophila Antennapedia
homeodomain.

Melittin TFA

A peptide can bind to and penetrate theenterocyte brush border, causing leakage into
the cytosol and increased paracellular
passage into the lamina propria.

Cell-penetratingPeptides

A peptide-based delivery agent that combines
TAT-HA2
the pH-sensitive HA2 fusion peptide fromFusion Peptide Influenza and the cell-penetrating peptide TATfrom HIV.
Targeting Peptides
CyclicsomatostatiniRGD peptide

A peptide acts as an inhibitor of endocrine andexocrine secretion via the activation of fiveG-protein-coupled receptors, namedSSTR1-5.

A peptide triggers tissue penetration of agentsby initially binding to av integrins, thenproteolytically cleaved within the tumor toproduce CRGDK/R, which interact swith
neuropilin-1. This peptide exhibits both tumortargeting and tumor-penetrating properties.
Cyclo(RGDyK) A potent and selective αVβ3 integrin inhibitor.
RGD peptide(GRGDNP)

A peptide competitively inhibits α5β1 binding
with extracellular matrix (ECM).

NGR peptideTFAA peptide containing Asn-Gly-Arg (NGR) motifthat can bind to APN/CD13, is usuallyconjugated to drugs for tumor imaging.

DgHBP-2

A 26-amino-acid-long peptide derived fromhistidine-rich beak protein-2 can be used infabricated glucose-responsive insulin deliverysystems.

pH-Low
Insertion
PeptideA pH-sensitive peptide that serves as a
specific ligand, targeting the acidic
microenvironment of tumor during early andmetastatic stages.

KLD-12

A 12-residue self-assembling peptide that canform peptide hydrogel with β-sheet structure.

RAD16-Ihydrochloride

A self-assembling nano-fibrous peptide with
biocompatible and biodegradable properties,
can be used to encapsulate cells.

Stimuli-responsive
PeptidesSelf-assembling
PeptidesChemScene — Master of Bioactive Molecules• CS offers 5,000+ catalog peptides: which are continuously updated.
• Unlimited custom service is available peptides, PDCs, ADCs, etc.

References:[1] Molecules. 2019, 24(2): 351.
[2] Medicina. 2021, 57(11): 1209.

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Products are for research use only and are not intended for human use. We do not sell to patients.