Table 1 Examples of interference peptides, peptidomimetics, and small inhibitors utilized in preclinical and clinical studies

From: Precision medicine by designer interference peptides: applications in oncology and molecular therapeutics

Target/s	Name/s	Cancer model/s	In vitro	In vivo	Concentration/dose administered	In vivo mode of administration	Clinical trials	References
MYC	Int-H1-S6A,F8A	Breast cancer cell line MCF-7	✓	×	0–10 µM	N/A	No	[15]
	Pen-ELP-H1	Breast cancer cell line MCF-7	✓	×	0–18 µM	N/A	No	[80]
	CPP-ELP-H1	Rat glioma cell C6 allograft	✓	✓	200 mg/kg	Intravenously	No	[17]
	IIA4B20 IIA6B17	Myc-transformed chicken embryo fibroblasts	✓	×	0–75 µM and 0–125 µM	N/A	No	[108*]
	10058-F4	Myc-transduced rat Rat1a xenograft in mice	✓	✓	64 µM	Cells treated in vitro and then inoculated in mice	No	[181*]
		Human prostate PC-3 and DU145 xenografts	✓	✓	20 and 30 mg/kg	Intravenously	No	[128*]
	10074-G5	Human Daudi Burkitt’s lymphoma xenografts	✓	✓	20 mg/kg	Intravenously	No	[115*]
	3jc48–3	human promyelocytic leukemia and Daudi Burkitt’s lymphoma cell lines	✓	×	0–50 µM	N/A	No	[113*]
	KJ-Pyr-9	Human triple negative breast cancer MDA-MB-231 xenograft	✓	✓	10 mg/kg	Intraperitoneally	No	[130*]
	Mycro3	Human pancreatic ductal adenocarcinoma Panc1 and MiaPaCa2 xenografts	✓	✓	100 mg/kg	Orally	No	[166*]
	OmoMYC	Human non-small cell lung cancer A549 xenografts	✓	✓	5 × 10¹⁰ viral particles	Intratumoral	No	[23]
		OmoMYC transgenic mice developing skin papilloma	✓	✓	N/A	expression directed to suprabasal keratinocytes	No	[19]
						under the control of the human involucrin promoter
		Spontaneous multifocal invasive astrocytoma and human glioblastoma xenograft	✓	✓	N/A	TRE-Omomyc; CMVrtTA mouse model, in which Omomyc	No	[105*]
						Is widely expressed upon doxycycline administration
		KRas^LSL-G12D/+-induced lung adenocarcinoma	✓	✓	2.37 and 60/120 mg/kg	Intranasally	No	[25]
		Human non-small cell lung cancer H1975 xenograft	✓	✓	60 and 120 mg/kg	Intravenously	No	[25]
	FPPa-OmoMYC	Murine triple negative breast cancer T11 allograft	✓	✓	32.2 mg/kg	Intratumoral	No	[26]
HOX(1–8)	HXR9	Murine melanoma B16 allograft	✓	✓	10 mg/kg	Intravenously	No	[32]
		Human non-small cell lung cancer A549 xenografts	✓	✓	100 mg/kg	Intraperitoneally	No	[33]
		Human ovarian cancer SK-OV3 xenografts	✓	✓	100 mg/kg	Intravenously	No	[34]
		Human triple negative breast cancer MDA-MB-231 xenografts	✓	✓	100 mg/kg	Intratumorally	No	[37]
		Human prostate cancer LNCaP xenografts	✓	✓	100 mg/kg	Intratumorally	No	[38]
		Human Mesothelioma MSTO-211H xenografts	✓	✓	25 mg/kg	Intraperitoneally	No	[39]
		Human oral squamous cell carcinoma cells	✓	×	0–100 µM	N/A	No	[153*]
PBX1	EN1-iPep	Human and murine basal-like breast cancer cell lines	✓	×	0–100 µM	N/A	No	[45]
	EN1_act-iPep	Murine triple negative breast cancer T11 allograft	✓	✓	25 mg/kg	Intratumorally	No	[49]
	EN1_act-RGD₁	Murine triple negative breast cancer T11 allograft	✓	✓	25 mg/kg	Intravenously	No	[50]
KRAS	Peptide 49 Peptide 54	Human lung cancer cell line H441	✓	×	0−0.1 mM	N/A	No	[56]
KRAS	SAH-SOS1_A	Human pancreatic, colon and lung cancer cells bearing KRAS mutations	✓	×	0.625–40 µM	N/A	No	[57]
BCL2	ABT-737	Human small cell lung cancer H146 and H1963 xenografts	✓	✓	25, 50, 75, 100 mg/kg	Intraperitoneally	No	[64]
	SAHB_A	Human leukemia xenografts	✓	✓	10 mg/kg	Intravenously	No	[63]
	ABT-263	Human B-cell lymphoma, multiple myeloma and small cell lung cancer xenografts	✓	✓	100 mg/kg	Orally	Yes	[65]
	ABT-199	Human hematological tumor xenografts	✓	✓	100 mg/kg	Orally	Yes	[66]
HDM2	^DPMIα	Human glioma U87 xenograft	✓	✓	3, 4, 7.5, 10 mg/kg	Intravenously	No	[70]
HDM2 HDMX	SAH-p53–8	Human choriocarcinoma JEG-3 xenograft	✓	✓	10 mg/kg	Intravenously	No	[72]
	ATSP-7041	Human osteosarcoma SJSA-1 and breast cancer MCF-7 xenografts	✓	✓	15, 20, 30 mg/kg	Intravenously	No	[73]
	MCo-PMI	Human colon cancer HCT116 xenograft	✓	✓	40 mg/kg	Intravenously	No	[189*]
	ALRN-6924	Human acute myeloid leukemia xenografts	✓	✓	20 mg/kg	Intravenously	Yes	[74]

The name of the peptides, peptidomimetics, and small inhibitors, the cancer model, the application in vitro and in vivo, the concentration/dose administered, the in vivo mode of administration, the clinical trials designed and the related references are indicated. N/A not applicable; ✓ Yes; × Not. The references marked with an asterix can be found in Supplementary Information

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Table 1 Examples of interference peptides, peptidomimetics, and small inhibitors utilized in preclinical and clinical studies

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