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The COVID-19 outbreak has rapidly spread on a global scale, affecting the economy and public health systems throughout the world. In recent years, peptide-based therapeutics have been widely studied and developed to treat infectious diseases, including viral infections. Herein, the antiviral effects of the lysine linked dimer des-Cys 11 , Lys 12 ,Lys 13 -(pBthTX-I) 2 K ( (pBthTX-I) 2 K) ) and derivatives against SARS-CoV-2 are reported. The lead peptide (pBthTX-I) 2 K and derivatives showed attractive inhibitory activities against SARS-CoV-2 (EC 50 = 28-65 µM) and mostly low cytotoxic effect (CC 50 &gt; 100 µM). To shed light on the mechanism of action underlying the peptides' antiviral activity, the Main Protease (M pro ) and Papain-Like protease (PL pro ) inhibitory activities of the peptides were assessed. The synthetic peptides showed PL pro inhibition potencies (IC 50 s = 1.0-3.5 µM) and binding affinities ( K  d = 0.9-7 µM) at the low micromolar range but poor inhibitory activity against M pro (IC 50 &gt; 10 µM). The modeled binding mode of a representative peptide of the series indicated that the compound blocked the entry of the PL pro substrate toward the protease catalytic cleft. Our findings indicated that non-toxic dimeric peptides derived from the Bothropstoxin-I have attractive cellular and enzymatic inhibitory activities, thereby suggesting that they are promising prototypes for the discovery and development of new drugs against SARS-CoV-2 infection.

Non-Toxic Dimeric Peptides Derived from the Bothropstoxin-I Are Potent SARS-CoV-2 and Papain-like Protease Inhibitors