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Table 1 Preclinical studies with drugs targeting HIF-1, angiogenesis or vasculogenic mimicry in cutaneous melanoma

From: Hypoxia-dependent drivers of melanoma progression

Drug

Involved Pathways

References

Transferrin-polyethylenimine-HIF-1α–short-hairpin RNA complex

Prevention of cell proliferation and induction of cell apoptosis; Downregulation of HIF-1α

Liu Y et al Mol Ther 2009 [119]

Isoliquiritigenin

Reduced expression of HIF-1α and glycolysis enzymes (GLUT 1/4, hexokinase 2, pyruvate kinase M2 and LDHA)

Wang Y et al Recent Pat Anticancer Drug Discov 2016 [120]

Luteolin

Reduced EMT, angiogenesis and metastasis through downregulation of HIF-1α, p-Akt, VEGF-A, p-VEGFR-2, MMP2, and MMP9

Li C et al Phytother Res 2019 [122]

Vanillin

Inhibition of cell migration by repressing STAT3-mediated HIF-1α mRNA expression

Park EJ et al Int J Mol Sci 2017 [123]

Anti-human VEGFR-1 monoclonal antibodies, D16F7

Inhibition of angiogenesis and endothelial cell migration in vitro; in vivo increased activity of immune checkpoint inhibitors

Lacal PM et al Pharmacol Res 2018 [124]

Lacal PM et al Pharmacol Res 2020 [126]

Sorafenib analogs

In vitro antiproliferative effect; in vivo anti-tumor activity; inhibitory activities against both EGFR and VEGFR-2

Sun S et al Molecules 2017 [127]

FAK inhibitor

In vitro inhibition of cell proliferation; in vivo reduced angiogenesis and lymphatic vessel density through disruption of FAK-VEGFR-3 complex

Kurenova E et al Cell Cycle 2014 [128]

Cordyceps militaris extract

Apoptosis induction, reduced VEGF secretion, decreased Akt1 and GSK-3β activation

Ruma IMW et al Int J Oncol 2014 [129]

16-kDa N-terminal fragment of prolactin complexed with liposomes

Reduced in vivo tumor growth and angiogenesis

Kinet V et al Cancer Lett 2009 [130]

Kinase C inhibitor

Inhibition of angiogenesis, vasculogenic mimicry, cell migration and colony formation

Fu Y et al Exp Cell Res 2020 [131]

Lupeol

Inhibition of vasculogenic mimicry

Bhattacharyya S et al Microvasc Res 2019 [132]

Apatinib

Inhibition of angiogenesis and vasculogenic mimicry by decreased expression of VEGFR-2, downregulation of the ERK1/2/PI3K/MMP2 signalling cascade

Liu ZJL et al PLoS One 2018 [133]

Copper (II) complex CPT8

Reduced vasculogenic mimicry through downregulation of MMP2

Shi X et al Dalton Trans 2018 [134]

Nicotinamide

Inhibition of vasculogenic mimicry through downregulation of VE-Cadherin

Itzhaki O et al PLoS One 2013 [135]

Lycorine hydrochloride

Reduced vasculogenic mimicry by decreasing VE-cadherin

Liu F et al Pigment Cell Melanoma Res 2012

Phenyl-quinoline derivative (CVM-1118)a

Inhibition of vasculogenic mimicry, antiproliferative and proapoptotic activity; inhibition of stem cell-associated genes and VEGF-A gene

Hendrix MJC et al Pharmacol Ther 2016 [137]

  1. aIn this article the use of Cutaneous Melanoma or Uveal Melanoma cells is not specified