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Table 2 Classification of tumor-targeting peptide in PDCs

From: Current progress and remaining challenges of peptide–drug conjugates (PDCs): next generation of antibody-drug conjugates (ADCs)?

Peptide sequence

Target

Payloads

Application

Ref.

cyclo (RGDfK); E[cyclo (RGDyK)]2;

integrins ανβ3,ανβ5

18F, 68Ga, Paclitaxel, Doxorubicin, Pt

PET imaging; breast cancer, ovarian cancer, melanoma, prostate

[41,42,43,44,45,46,47,48]

NGR; cyclo (NleNGRE); c[KNGRE]

CD13

Chlorambucil, 99m Tc, daunomycin, NSAID, human tumor necrosis factor (hTNF)

pleural mesothelioma, hepatocellular carcinoma; ovarian cancer; human fibrosarcoma

[49,50,51,52,53]

LS-7 (LQNAPRS)

CD133

Camptothecin

Treatment of lung cancer, melanoma, colon cancer, liver cancer or breast cancer.

[54]

QKRKRKKSRYKS

VEGFR

Lytic peptide

liver cancer

[55]

D-γ-E-γ-E-γ-E-E-OH

PSMA

Thapsigargin

hepatocellular carcinoma

[56, 57]

NYSKPTDRQYHF; CVRARTR

PD-L1

anti-miR-21 inhibitor, DOX

Melanoma, breast cancer

[58, 59]

RS17 (RRYKQDGGWSHWSPWSS); CkRFYVVMWKk, k = D analogue of lysine

CD47

pro-apoptotic VK30 peptide; gemcitabine

lung cancer, bladder cancer

[60, 61]

D-f-C-F-D-w-K-T-C-Thr(ol)

SST2 receptor

111In,99mTc, 68Ga, Paclitaxel, Doxorubicin, camptothecin

diagnosis of neuroendocrine tumors, treatment of breast or liver cancer,

[62,63,64,65,66,67,68]

Pyro-E-H-W-S-Y-D-K-L-R-P-G-NH2;

LH-RH receptor

vedotin (MC-VC-PABC-MMAE), Doxorubicin; sunitinib

Ovarian cancer, prostate cancer, breast cancer

[69,70,71,72,73]

MT1-MMP bicyclic binder (BT1718); MMP-2 inhibitors CCKIGLFRWR

Matrix metalloproteinase (MT1-MMP); MMP-2

DM1, Doxorubicin

metastatic liver cancers,

[74, 75]

ANG2: TFFYGGSRGKRNNFKTEEY IETP2:TFYGGRPKRNNFLRGIRSRGD; M1-RGD: TFYGGRPKRNNFLRGIRSRGD)

LRP1

Paclitaxel; Curcumin; Doxorubicin; morphine

Breast cancer with brain metastasis; noise-induced hearing impairment; central pain

[76,77,78]

EphA2 bicyclic binder); YSAYPDSVPMMS

EphA2

auristatin E; paclitaxel

fibrosarcoma, prostate cancer

[79,80,81]

YHWYGYTPQNVI; CMYIEALDKYAC; Cyclic[CQTPYYMNTC]; Cyclic (CHVPGSYIC); Cyclic (CVNAMQSYC)

EGFR

Doxorubicin; Lytic peptide; Proapoptotic Peptide; Epothilone Analogs; Camptothecin

TKI-resistant cancer, liver cancer, lung cancer, glioblastoma cell

[82,83,84]