Table 1.

Selected cargo types delivered by pH-low insertion peptides (pHLIP).

Cargo Type	Cargo	Tumor Model	Vehicle
Small Molecules
Antiproliferative agents	Phallodin [19]	HeLa, JC, M4A4, HT1080 *	WT pHLIP-K(rho)
	α-Amanitin [20]	HeLa, U2OS, M4A4, MDA-MB-231 *	WT pHLIP
	Doxorubicin [21]	MCF-7, MCF-7/ADR *	WT pHLIP
	microtubule inhibitor monomethyl auristatin E (MMAE) [22]	HeLa, A431, MDA-MB-23 * NCRr nu/nu mice bearing HeLa or A431 tumors **	WT pHLIP pHLIP-D25E pHLIP-P20G pHLIP-D14Gla:D25Aad
	Paclitaxel [13]	A549 *	WT pHLIP pHLIP-D14Gla:D25Aad
Imaging agents	Alexa750, Cy5.5 [6,7]	BALB/c nude mice bearing HeLa and NM2C5 tumors, TRAMP mice bearing M4A4 tumors ** CRL-2116 tumor bearing C3D2F1 mice **	WT pHLIP
	Alexa488, Alexa546, Alexa647, IR680 [23]	4T1 * BALB/c mice bearing 4T1 tumors and MMTV-PyMT mice **	WT pHLIP Var3 pHLIP Var7 pHLIP
	Indocyanin green (ICG) [24]	HMEpC * BALB/c mice bearing 4T1, MDA-MB-231, A549, LLC, M4A4, HeLa, UM-UC3 and LNCaP tumors **	Var3 pHLIP
	64Cu, 18F-AlF [9]	BALB/c mice bearing 4T1 tumors **	WT pHLIP Var3 pHLIP Var7 pHLIP
	99mTC [25]	LLC tumor bearing C57BL/6 mice, PC-3 and LNCaP tumor bearing SCID mice **	WT pHLIP
Nanoparticles
Antiproliferative agents	Doxorubicin encapsulated MCM-41 nanoparticles [26]	MCF-7, MCF-7/ADR *	WT pHLIP
	Ceramide encapsulated liposomes [27]	A549, HeLa *	WT pHLIP
	Gramicidin A encapsulated liposomes [28]	A549, HeLa, M4A4 *	WT pHLIP
Genetic material	Plasmid DNA encapsulated dendrigraft poly lysine nanoparticles [29]	Bel-7402 * BALB/c nude mice bearing Bel-7402 tumors **	WT pHLIP
Metallic nanoparticles	Gold nanoparticles [30,31,32]	HeLa, A549, JC BALB/c nude mice bearing HeLa tumors and BALB/c mice bearing JC tumors **	WT pHLIP
	Gadolinium nanoparticles [33]	A549 * EMT6 tumors in BALB/c mice **	WT pHLIP
Peptide Nucleic Acids (PNAs)
Anti-miRNA	Anti-miR-155 [34]	A549, KB, DLBCL * Nude mice bearing neoplastic B cells derived from enlarged spleens of miR-155LSLtTA mice and mice bearing KB tumors **	WT pHLIP
	Anti-miR-21 [34,35]	A549 * Orthotopic and heterotopic LLC tumors in C57BL6 mice **	WT pHLIP Var3 pHLIP
Anti-lncRNA	HOX transcript antisense RNA targeting PNA [36]	A2780P, A2780_CR5, KURAMOCHI, SKBR-3, MCF-7, MDA-MB-231 * BALB/c-nu/nu mice bearing A2780_CR5 tumors **	WT pHLIP
Antisense	αKU80 [37]	A549, DLD1-BRCA2KO, EMT-6 * BALBc/Rw mice bearing EMT-6 tumors, athymic nu/nu mice bearing DLD1-BRCA2KO tumors **	WT pHLIP

* In vitro studies, ** In vivo studies.