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Table1 Anticancer peptide function in four different cancers: breast, glioma, colorectal, and melanoma

From: Anti-cancer peptide-based therapeutic strategies in solid tumors

Cancer

Target, group

Peptide name

Function

Refs.

Breast cancer

Tumor suppressor

INK4 family

(p16INK4a

p15INK4b

p18INK4c

p19INK4d)

Using the proteins Cdk4 or Cdk6 to inhibit the action of cyclin D and block the progression of the cell cycle

[172]

  

CIP/KIP family

(p21cip1/waf1

p27kip1

p57 kip2)

CYCLIN–CDK complexes indirectly repress transcription

[173]

  

p16 (p16INK4a)

Slowing down the progression of the cell cycle by inactivating Cdk4/6

[174]

  

p21 (CIP1/WAF1)

Cell cycle arrest is caused by blocking the activity of cyclin–CDK2, cyclin–CDK1, and cyclin–CDK4/6 complexes

Competing for PCNA binding with DNA polymerase-δ, hence directly inhibiting DNA synthesis

[175]

  

p44

Activating p53 by phosphorylating serine 15, resulting in activating p21 protein, and thus inhibiting cell cycle progression

[176]

  

BRCA1

Involved in repairing damaged DNA

[177]

 

Cell death provoker

KCCYSL

Imaging the HER2-positive tumors with kd of 295 nM

[178]

  

BP-FFVLK-YCDGFYACYMDV

Once bound to the cell surface HER2, it transforms into nanofibrillar (NF) structures

[179]

  

Bcl-2 family

(Bax, Bak, and Bok)

Binding with interactions regulating mitochondrial outer membrane permeabilization, thereby releasing intermembrane space proteins

[180]

  

CT20

Promoting mitochondrial aggregation and cytoskeletal disruption

[181]

  

RRM-MV

Decreasing BCL-XL and d MCL-1, increasing Bax

[182]

  

VDAC1

Interacting with anti-apoptotic proteins

[183]

 

Cytolytic agents

RGD

Acting as an inhibitor of integrin–ligand interactions

Promoting cell adherence to the matrix, preventing cell apoptosis, and accelerating new tissue regeneration

[184]

  

Pleurocidin family (NRC-03 and NRC-07)

Using membranolytic mechanisms to kill breast cancer cells

[185]

  

L-K6

Interacting with MCF-7 cells, owing to negatively charged phosphatidylserine thereof

[186]

  

p28 peptide

Acting as a cancer-specific antiproliferative agent

[187]

  

SKACP003

Inducing dose-dependent cytotoxicity in all cell lines via hydrogenic interaction of the peptide with β-catenin

[179]

 

Peptide vaccine

E75

Eliciting a robust anti-HER2 immune response

[188]

Glioma

Cell-penetrating peptides

PepFect14 Transportan10

PepFect3

PepFect28

SynB3

Stearyl-SynB3

Delivery of splice-correcting oligonucleotides (SCOs) to the HeLa pLuc705 cell line

Delivering a large protein such as an antibody, oligonucleotide, or colloidal gold as cargo

[189] [190]

[191]

 

MDGI/FABP3 targeting peptide

CooP (CGLSGLGVA)

Recognizing tumor vessels and invading tumor satellites by interacting with MDGI/H-FABP/FABP3 in brain tumor tissue

[192]

 

Transferrin receptor

T7 (HAIYPRH)

Targeting transferrin receptors (TfRs) in a tumor-targeting nanodrug delivery system to enter cells easily without damaging the cells with transferrin (Tf)

[193]

  

T12 (THRPPMWSPVWP)

Binding to a different site on TfRs compared with transferrin

[194]

 

LRP targeting peptides

LRP-1

As a cellular penetration facilitator, uPA inhibits the activity of extracellular proteases that activate uPA

[195]

  

LRP-2

Mediating endocytosis of ligands leading to degradation in lysosomes or transcytosis

[196]

 

Interleukin-4 receptor

CRKRLDRNC

IL-4Ra-binding

[197]

Colorectal cancer

 

PepT 1 (SLC15A1)

Facilitating the cellular translocation of dipeptides and tripeptides and the absorption of numerous peptidomimetic drugs

[198]

  

HNP1–3

Mediating lysis of tumors in a concentration-dependent manner

Inducing the chemokine interleukin-8 (IL-8) and modulating cytokine expression, thereby modulating immune response and inflammation

[199]

  

TCP-1

Delivering fluorescein and anticancer medicines into CRC tissue

[200]

  

EphA2-derived peptide

EphA2-specific CTL

[201]

  

ABT-737

Inhibition of anti-apoptotic Bcl-2 family

[201]

  

Multipeptide cocktail: epitomes of HER2, MVF, GMP, and n-MDP

Inhibition of EGF-2

[201]

  

Endoglin

Inhibition of angiogenesis

[201]

  

CEA691

Induction of tumor-specific CTLs

[201]

  

CEA526–533, NP52–59

Activation of tumor-specific CTLs

[201]

Melanoma

 

M2pep

Binding preferentially to murine M2 macrophages and M2-like TAMs

[202]

  

LyP-1

Creating reagents that can specifically destroy tumor lymphatics could be one way to develop the treatment

[203]

  

CycMSH

Providing a large surface area for interacting with the target

[204]

  

RGD-SSL-Dox

Facilitating the DOX uptake into melanoma cells by integrin-mediated endocytosis

(205)