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. 2022 May 10;53:102331. doi: 10.1016/j.redox.2022.102331

Table 2.

Summary of the effects of various pharmacological CBS inhibitors in cancer models.

CBS inhibitor compound Name hCBS IC50 Characteristics Effects in cancer models
Image 1 AOAA 8 μM PLP-dependent covalent inhibitor; inhibits multiple other enzymes as well Efficacy in a cellular model in vitro and in murine models in vivo
AOAA methyl ester
AOAA isopropyl ester		 YD0171YD0251 8 μM (with better cell uptake) After hydrolysis by esterases, it yields AOAA and exerts similar effects as AOAA at lower concentrations/doses. Efficacy in a cellular model in vitro and in murine models in vivo
Image 2 CH004 2 μM Competitive inhibitor, identified by HTS, has known or likely off-target effects Efficacy in a cellular model in vitro and in murine models in vivo
Image 3 Sikokianin C 3 μM Competitive inhibitor, identified by HTS, has known off-target effects, not druggable Efficacy in a cellular model in vitro and in a murine model in vivo
Image 4 Benserazide 30 μM PLP-dependent covalent inhibitor; known clinically used drug – may be a possible candidate for drug repurposing Efficacy in a cellular model in vitro and in murine models in vivo
Image 5 Disulfiram 1 μM (after conversion to CuDCC) Covalent inhibitor via copper; known clinically used drug with multiple MOA's – may be a possible candidate for drug repurposing; currently in several cancer clinical trials (but the proposed mechanism of action that is unrelated to CBS) Efficacy in a cellular model in vitro and in murine models in vivo
  Various polyphenols [Multiple] 5–30 μM Multiple targets, most of them natural compounds No information
Image 6 NSC11041
NSC67078		 4–10 μM Partially characterized compounds from various HTS campaigns; CBS selectivity and cell uptake insufficiently characterized No information