Advances in the discovery of exosome inhibitors in cancer

Figures & data

Table 1. RAB27A inhibitors.

Compound	Structure	EC50(μM)	Reference
Tipifarnib		1.0	[14,15]
Neticonazole		8.0	[16]
Climbazole		10.0	[16]
Ketoconazole		5.0	[17]
Nexinhib20		2.6	[18]
Nexinhib4		10.0	[18]

Table showing the exosome inhibitors that target RAB27A, their potency and their structures.

Figure 1. The interactions between Tipifarnib and RAB27A from molecular docking. (A) The pocket is shown in electrostatics representation. (B) The two-dimensional schematic representation of the Rab27a and Tipifarnib complex interactions. Red, yellow, blue and white ribbons: RAB27A. The binding surfaces are identified in grey. The molecular structures of Tipifarnib is displayed by purple ball-and-stick models. Green lines indicate pi-pi stacking interactions, and purple dashed arrows represent sidechain hydrogen bond interactions. Polar and hydrophobic residues are depicted with green and pink circles, respectively.

Figure 2. The interactions between GW4869 and nSMase from molecular docking. (A) The pocket is shown in electrostatics representation. (B) The two-dimensional schematic representation of the nSMase and GW4869 complex interactions. Red, yellow, blue and white ribbons: nSMase. The binding surfaces are identified in grey. The molecular structures of GW4869 is displayed by purple ball-and-stick models. Green lines indicate pi-pi stacking interactions, and purple dashed arrows represent sidechain hydrogen bond interactions. Polar and hydrophobic residues are depicted with green and pink circles, respectively.

Table 2. nSMase inhibitors.

Compound	Structure	EC50(μM)	Reference
GW4869		1.0	[22,25,26]
Manumycin A		0.25	[27,28]
Spiroepoxide		2.0	[29,30]
Cambinol		5.0	[31]
Scyphostatin		N/A	[32,33]
DPTIP		2.0	[34]

Table showing the exosome inhibitors that target nSMase, their potency and their structures.

Table 3. Other inhibitors.

Compound	Structure	EC50(μM)	Reference
Lansoprazole		N/A	[43]
Omeprazole		10	[44]
Esomeprazole		70	[44]
Pantoprazole		N/A	[44]
SLC-0111		0.2	[45,46]
Cannabidiol		5.0	[47,48]
Ketotifen		10.0	[49,50]
Simvastatin		1.0	[51]
Sulphisoxazole		50.0	[52]

Table showing the exosome inhibitors that target other proteins, their potency and their structures.

Figure 3. The interactions between Sulphisoxazole and endothelin receptor A from molecular docking. (A) The pocket is shown in electrostatics representation. (B) The two-dimensional schematic representation of the endothelin receptor A and Sulphisoxazole complex interactions. Red, yellow, blue and white ribbons: endothelin receptor A. The binding surfaces are identified in grey. The molecular structures of Sulphisoxazole is displayed by purple ball-and-stick models. Green lines indicate pi-pi stacking interactions, and purple dashed arrows represent sidechain hydrogen bond interactions. Polar and hydrophobic residues are depicted with green and pink circles, respectively.

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