The L-Type Amino Acid Transporter LAT1—An Emerging Target in Cancer

Häfliger, Pascal; Charles, Roch‐Philippe

doi:10.3390/ijms20102428

Cited by 151 publications

(156 citation statements)

References 117 publications

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“…It is overexpressed in some NET, such as pheochromocytoma, medullary thyroid carcinoma, and NET of the lungs. Its overexpression was proven in many types of solid tumours [11][12][13]. Our patient was diagnosed with grade I NET; however, in a study by Kaira et al [13], all 10 patients diagnosed with grade I NET of the lung did not express LAT-1.…”

Section: Discussion/conclusionmentioning

confidence: 54%

Incidental Accumulation of Fluciclovine in Neuroendocrine Tumour in a Patient with Oncological Duplicity

Balážová

Černý

Vyškovský³

2020

Case Rep Oncol

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18F-fluciclovine is a PET radiopharmaceutical used for the detection of recurrent prostate cancer in adult men after primary curative treatment with suspicion of recurrence based on elevated prostate-specific antigen level. Several incidental uptakes of 18F-fluciclovine in other tumour types have been described in the literature so far -in breast cancer, hepatocellular carcinoma, and malignant melanoma. Our case report presents a patient with oncological duplicity (prostate gland carcinoma and newly diagnosed neuroendocrine tumour) and with accumulation of fluciclovine in pathologically proved neuroendocrine tumour, later imagined also by octreotide SPECT/CT. To our knowledge, this is the first case of fluciclovine accumulated in a neuroendocrine tumour described in the literature.In conclusion, incidental FCV uptake in cancer types other than prostate cancer has already been described, with our case report adding to this list. FCV PET is a tool to detect recurrent prostate cancer with rising PSA levels. In our case, the patient had low PSA levels and FCV uptake in metastases which were later proven to be NET. AcknowledgementWe would like to thank Dr. Pavel Veselý, PhD, clinical oncologist, for his help with the clinical data of the patient. Statement of EthicsWritten informed consent was obtained from the patient for the publication of this case report and accompanying images.

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Section: Discussion/conclusionmentioning

confidence: 54%

Incidental Accumulation of Fluciclovine in Neuroendocrine Tumour in a Patient with Oncological Duplicity

Balážová

Černý

Vyškovský³

2020

Case Rep Oncol

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“…Since overexpression of LAT‐1 is a hallmark of several cancers, [ 42 ] we hypothesized that the uptake of Nano‐pPAAM via LAT‐1 could be exploited to achieve selective targeting of cancer cells. To examine this possibility, we extended our in vitro screening regime to an additional panel of cancer cells such as MCF‐7 (breast cancer), MKN (gastric cancer), II‐4 (HaCaT ras clone), as well as noncancerous cells such as HaCaT (skin), HDF (skin), NCM‐460 (colon).…”

Section: Resultsmentioning

confidence: 99%

Potent‐By‐Design: Amino Acids Mimicking Porous Nanotherapeutics with Intrinsic Anticancer Targeting Properties

Lim

Tan

et al. 2020

Small

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Exogenous sources of amino acids are essential nutrients to fuel cancer growth. Here, the increased demand for amino acid displayed by cancer cells is unconventionally exploited as a design principle to replete cancer cells with apoptosis inducing nanoscopic porous amino acid mimics (Nano‐PAAM). A small library consisting of nine essential amino acids nanoconjugates (30 nm) are synthesized, and the in vitro anticancer activity is evaluated. Among the Nano‐PAAMs, l‐phenylalanine functionalized Nano‐PAAM (Nano‐pPAAM) has emerged as a novel nanotherapeutics with excellent intrinsic anticancer and cancer‐selective properties. The therapeutic efficacy of Nano‐pPAAM against a panel of human breast, gastric, and skin cancer cells could be ascribed to the specific targeting of the overexpressed human large neutral amino acid transporter SLC7A5 (LAT‐1) in cancer cells, and its intracellular reactive oxygen species (ROS) inducing properties of the nanoporous core. At the mechanistic level, it is revealed that Nano‐pPAAM could activate both the extrinsic and intrinsic apoptosis pathways to exert a potent “double‐whammy” anticancer effect. The potential clinical utility of Nano‐pPAAM is further investigated using an MDA‐MB‐231 xenograft in NOD scid gamma mice, where an overall suppression of tumor growth by 60% is achieved without the aid of any drugs or application of external stimuli.

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“…(Li and Zhao, 2019;Mohammed et al, 2019;Zhang et al, 2019). It is well known that the progression of the tumor requires a large amount of nutrients, including amino acids (AA), glucose, etc., which leads to overexpression of AA transporters and glucose transporters on the surface of tumor cells (Madunic et al, 2018;Hafliger and Charles, 2019;Ogawa et al, 2019;Sztandera et al, 2019). Moreover, transporter-mediated drug transport exhibited higher specificity and efficiency than receptor-ligand-mediated active targeting in terms of transport efficiency.…”

Section: Introductionmentioning

confidence: 99%

Lysine-mediated hydroxyethyl starch-10-hydroxy camptothecin micelles for the treatment of liver cancer

Zhao

2020

Drug Delivery

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Liver cancer is a malignant tumor with extremely high morbidity and mortality. At present, traditional chemotherapy is still the most commonly used therapeutic approach. However, serious side effects lead to the treatment of liver cancer is not ideal. Therefore, it is imperative to develop a new drug delivery system based on nanotechnology and liver cancer microenvironment. In this study, a pH/ reduction/a-amylase multi-sensitive hydroxyethyl starch-10-hydroxy camptothecin micelles (HES-10-HCPT-SS-Ly) targeting over-expressed amino acid (AA) transporters on the surface of liver cancer cell by applying lysine were successfully synthesized. The prepared micelles showed regular structure, suitable particle size, and intelligent drug release property. Compared with conventional HES-10-HCPT micelles and 10-HCPT injection, HES-10-HCPT-SS-Ly micelles demonstrated better in vitro anti-proliferative capability toward human liver cancer Hep-G2 cells and greater antitumor efficiency against nude mouse with Hep-G2 tumor. These findings suggest that HES-10-HCPT-SS-Ly micelles may be a promising nanomedicine for treatment of liver cancer.

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The L-Type Amino Acid Transporter LAT1—An Emerging Target in Cancer

Cited by 151 publications

References 117 publications

Incidental Accumulation of Fluciclovine in Neuroendocrine Tumour in a Patient with Oncological Duplicity

Incidental Accumulation of Fluciclovine in Neuroendocrine Tumour in a Patient with Oncological Duplicity

Potent‐By‐Design: Amino Acids Mimicking Porous Nanotherapeutics with Intrinsic Anticancer Targeting Properties

Lysine-mediated hydroxyethyl starch-10-hydroxy camptothecin micelles for the treatment of liver cancer

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