Table 1.
Targeting of the amino acid transporters.
| Chemical Inhibition | |||||
|---|---|---|---|---|---|
| Transporter | Inhibitor | Experimental Model | Tissue Type | Refs | |
| SLC1A1 | 2-(furan-2-yl)-8-methyl-N-(o-tolyl)imidazo[1,2-a]pyridin-3-amine | In vitro (Cell line) | Human Embryonic Kidney cells | [161] | |
| SLC1A2 | Azo-TFB-TBOA | In vitro (Xenopus laevis oocytes) | Xenopus laevis oocytes | [162] | |
| SLC1A5, SLC38A2, SLC7A5 | V-9302 | In vitro (Cell line) | A panel of human cancer cell lines [163] Head and Neck Squamous Cell Carcinoma [29] | [29,163] | |
| In vivo (Cell line derived-xenograft) | patient-derived xenografts (PDX) model [163], Head and Neck Squamous Cell Carcinoma cell line xenograft [29] | ||||
| SLC1A5 | L-g-glutamyl-p-nitroanilide (GPNA) | In vitro (Cell line) | Colorectal Carcinoma [164], Endometrial Carcinoma [165] | [164,165] | |
| In vivo (Cell line derived-xenograft) | |||||
| SLC1A5 | Benzylserine (BenSer) | In vitro (Cell line) | Endometrial Carcinoma [165], Melanoma [166] | [165,166] | |
| SLC1A5 | Benzyloxybenzyl analogues | In vitro (Cell line) | Human Embryonic Kidney cells, C6 Rat cells | [167] | |
| SLC1A5 | KM8094 mAB | In vivo (Patient derived-xenograft) | Patient-derived Gastric cancer tissue | [168] | |
| SLC1A5 | KM4008 mAB | In vitro (Cell line) | A panel of cell lines | [169] | |
| SLC1A5 | KM4012 mAB | In vitro (Cell line) | A panel of cell lines | [169] | |
| SLC1A5 | KM4018 mAB | In vitro (Cell line) | A panel of cell lines | [169] | |
| SLC1A5 | Ab3-8 mAb | In vitro (Cell line) | Colorectal Carcinoma | [170] | |
| SLC1A5, SLC7A5 | Delta-tocotrienol (δT) | In vitro (Cell line) | Non-Small Cell Lung Cancer | [171] | |
| SLC6A1 | Photoswitchable inhibitor | In vitro (Cell line) | Human Embryonic Kidney cells and Dentate gyrus granule cells | [172] | |
| SLC6A14 | α-methyltryptophan | In vitro (Cell line) | Colon cancer [173], Pancreatic cancer [174,175] | [173,174,175] | |
| In vivo (Cell line derived-xenograft) | |||||
| SLC7A5 | SKN103 | In vitro (Cell line) | A panel of human cancer cell lines | [176] | |
| SLC7A5 | BCH | In vitro (Cell line) | Melanoma | [166] | |
| SLC7A5 | JPH203 | In vitro (Cell line) | Anaplastic thyroid cancer [177], Medulloblastoma [178], Head and Neck Squamous Cell Carcinoma [179], T-cell lymphoblastic lymphoma/T-cell acute lymphoblastic leukemia [180] |
[177,178,179,180] | |
| In vivo (Cell line derived-xenograft) | |||||
| SLC7A11 | Sulfasalazine (SSZ) | In vitro (Cell line) | Non-Small Cell Lung Cancer [181], A panel of human cancer cell lines [182], Lung Adenocarcinoma [183], Head and Neck Squamous Cell Carcinoma [184], Bladder Cancer [185], Lymphoma [186,187] | [181,182,183,184,185,186,187] | |
| In vivo (Cell line derived-xenograft) | |||||
| In vivo (KRAS Mouse model) | |||||
| In vivo (Murine metastasis model) | |||||
| SLC25A8 | Genipin | In vitro (Cell line) | Breast Cancer [188], Ovarian Cancer [189] | [189] | |
| SLC43A1 | ESK246 | In vitro (Cell line) | Prostate Cancer | [190] | |
| Drug Delivery | |||||
| Through which Transporter | Molecule | Delivery | Experimental Model | Tissue Type | Refs |
| SLC1A5 | GLN-CD (conjugation of Gln with β-cyclodextrin) | Doxorubicin | In vitro (Cell line) | Triple-negative Breast Cancer | [191] |
| SLC1A5 | Polyglutamine (PGS) | various agents including siRNAs | In vitro (Cell line) | Lung Cancer | [192] |