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. 2022 Dec 16;13:1067652. doi: 10.3389/fphar.2022.1067652

TABLE 1.

Potential pharmacological targets and inhibitors targeting lipid uptake.

Drug target Notable inhibitors Inhibitor description IC50 Development status Related diseases Chemical structure References
FATP2 Lipofermata 4.84 μM Preclinical Stage Melanoma graphic file with name FPHAR_fphar-2022-1067652_wc_tfx1.jpg Zhang et al. (2018)
CD36 ABT-510 TSP-1 mimetic drug Phase 2 Melanoma; Renal cell carcinoma, Lymphoma; Glioblastoma; Brain Tumor graphic file with name FPHAR_fphar-2022-1067652_wc_tfx2.jpg Campbell et al. (2010), Markovic et al. (2007), Nabors et al. (2010)
MAGL ABX-1431 An first-in-class irreversible inhibitor 8 nM Phase 2 Neurological disorders graphic file with name FPHAR_fphar-2022-1067652_wc_tfx3.jpg Cisar et al. (2018)
MAGL MJN110 Irreversible 9.1 nM Preclinical Stage Diabetes; Neuropathy graphic file with name FPHAR_fphar-2022-1067652_wc_tfx4.jpg Wilkerson et al. (2016)
MAGL JNJ-42226314 Highly selective; Non-covalent; Reversible 1.13 nM (Hela cells) Preclinical Stage Neuropathic and inflammatory pain graphic file with name FPHAR_fphar-2022-1067652_wc_tfx5.jpg Wyatt et al. (2020)
MAGL JZL184 The first selective MAGL inhibitor 8 nM Preclinical Stage T2D; Glioblastoma graphic file with name FPHAR_fphar-2022-1067652_wc_tfx6.jpg Taib et al. (2019), Walenna et al. (2020)
NPC1L1 Ezetimibe a selective inhibitor; Oral FDA approved Primary hyperlipidemia; Familial cholesterolemia graphic file with name FPHAR_fphar-2022-1067652_wc_tfx7.jpg Long et al. (2021), Rocha et al. (2022)

The chemical information of small molecules is collected from Pubchem database (https://pubchem.ncbi.nlm.nih.gov), and 2D structures in the above diagram were drawn by Chemdraw software. IC50, half maximal inhibitory concentration.