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Screening of metallohelices for enantioselective targeting SARS-CoV-2 RNA G-quadruplex

文献类型： 外文期刊

作者： Sun, Yue 1 ; Zhao, Chuanqi 1 ; Liu, Yan 1 ; Wang, Yibo 1 ; Zhang, Cheng 1 ; Yang, Jie 1 ; Qin, Geng 1 ; Song, Hualong 4 ; Postings, Miles 4 ; Scott, Peter 4 ; Ren, Jinsong 1 ; Qu, Xiaogang 1 ;

作者机构： 1.Chinese Acad Sci, Changchun Inst Appl Chem, Lab Chem Biol, Changchun 130022, Peoples R China

2.Changchun Inst Appl Chem, Chinese Acad Sci, State Key Lab Rare Earth Resource Utilizat, P, R China, Changchun 130022, Peoples R China

3.Univ Sci & Technol China, Sch Appl Chem & Engn, Hefei 230026, Peoples R China

4.Chinese Acad Agr Sci, Changchun Vet Res Inst, Changchun 130122, Peoples R China

5.Univ Warwick, Coventry CV4 7AL, England

期刊名称：NUCLEIC ACIDS RESEARCH （ 影响因子：13.1； 五年影响因子：16.8 ）

ISSN： 0305-1048

年卷期： 2025 年 53 卷 10 期

页码：

收录情况： SCI

摘要： The emergence of numerous variants of SARS-CoV-2 still presents the major challenges in the fight against this disease by reducing the efficacy of vaccines and drugs. RNA G-quadruplexes (G4s) in the SARS-CoV-2 genome are highly conserved and have thus been spotlighted as a promising therapeutic target to combat a wider range of variants. However, very few RNA G4 specific compounds have been reported. Here, a small library of 64 chiral metallohelices has been constructed for screening SARS-CoV-2 G4-specific binders. After screening, we found that one pair of the enantiomers showed the best enantioselectivity. The Lambda enantiomer can strongly stabilize SARS-CoV-2 G4s, inhibit the expression of virus protein, and reduce the SARS-CoV-2 RNA copies and viral titers in Vero E6 cells. In contrast, the Delta enantiomer has much weaker effects than the Lambda enantiomer under the same experimental conditions, showing an obvious enantioselectivity. Further studies indicate that the Lambda enantiomer prefers binding to SARS-CoV-2 G4s rather than binding to the single/double-stranded DNA and commonly reported human DNA G4s, indicating its selectivity to RNA G4s. This work provides the first example for enantioselectively targeting SARS-CoV-2 G4s, and will promote developing drug candidates for targeting virus G4s.

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