Table 3.

Small molecules targeting DBHS family proteins and their tumour-suppressive effects.

Small molecule	Target DBHS family protein	Binding site on target DBHS family protein	Effects on target DBHS family protein	Tumor-suppressive effects	Clinical application
No. 10–3 (7,8-dihydroxy-4- (4-methoxyphenyl) chromen-2-one)	SFPQ	The groove between coiled-coil domain and RNA-binding domain of SFPQ	Inhibits RNA binding of SFPQ	Suppresses in vitro proliferation of 22 Rv1 CRPC model cells and tamoxifen-resistant breast cancer cells [15] Impairs in vivo tumour growth of CRPC mouse models [15]	–
C-65 (4-[2-(3H-Imidazol[4,5-b] pyridib-2-ylsulfanyl) -acetylamino]-benzonic acid isopropyl ester)	SFPQ	Unknown	Inhibits RNA binding of SFPQ	Suppresses in vitro proliferation of 22 Rv1 CRPC model cells and tamoxifen-resistant breast cancer cells [16] Impairs in vivo tumour growth of CRPC mouse models [16]	–
Auranofin (1-Thio-β-D-glucopyranosatotriethylphosphine gold-2,3,4,6-tetraacetate)	NONO	Unknown	Decreases NONO expression level	Suppresses in vitro proliferation of MDA-MB-231 triple-negative breast cancer cells and glioblastoma cells [17,18] Impairs in vivo tumour growth of glioblastoma mouse models [18]	a treatment of rheumatoid arthritis [138]
(R)-SKBG-1 ((R)-4-(2-chloroacetyl) -N-(4-methoxybenzyl) −1-((4-methoxyphenyl) sulfonyl)piperazine-2 -carboxamide)	NONO	Cysteine 145 on NONO (covalent binding)	Enhances RNA binding of NONO	Suppresses in vitro proliferation of 22 Rv1 CRPC model cells and ER-positive MCF-7 breast cancer cells [19]	–

CRPC, castration-resistant prostate cancer; DBHS, Drosophila behavior and human splicing; ER, oestrogen receptor; NONO, non-POU domain-containing octamer-binding protein; SFPQ, splicing factor proline/glutamine rich.