Estudos atuais sobre medicamentos para combater a COVID-19.
PDF

Palavras-chave

Tratamento
Terapêutica
Farmacologia
Medicamentos
Covid-19

Como Citar

Coelho Paraguassu, E. ., & Celis de Cárdenas , A. M. . (2020). Estudos atuais sobre medicamentos para combater a COVID-19. Brazilian Journal of Implantology and Health Sciences, 2(11), 01–09. https://doi.org/10.36557/2674-8169.2020v2n11p01-09

Resumo

Uma campanha de triagem em grande escala rendeu dezenas de estruturas cristalinas de pequenos fragmentos de moléculas que se ligam à protease principal do SARS-CoV-2. A comunidade de pesquisa global é encorajada a persegui-los como pontos de partida para a descoberta de medicamentos para COVID-19.

https://doi.org/10.36557/2674-8169.2020v2n11p01-09
PDF

Referências

Douangamath, A. et al. Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease. Nat. Commun. https://doi.org/10.1038/s41467-020-18709-w (2020).

Zhang, L. et al. Alpha-ketoamides as broad-spectrum inhibitors of coronavirus and enterovirus replication: structure-based design, synthesis, and activity assessment. J. Med. Chem. 63, 4562–4578 (2020).

Jin, Z. et al. Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors. Nature 582, 289–293 (2020).

Dai, W. et al. Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease. Science 368, 1331–1335 (2020).

Erlanson, D. A., Fesik, S. W., Hubbard, R. E., Jahnke, W. & Jhoti, H. Twenty years on: the impact of fragments on drug discovery. Nat. Rev. Drug Discov. 15, 605–619 (2016).

Resnick, E. et al. Rapid covalent-probe discovery by electrophile-fragment screening. J. Am. Chem. Soc. 141, 8951–8968 (2019).

Abdeldayem, A., Raouf, Y. S., Constantinescu, S. N., Moriggl, R. & Gunning, P. T. Advances in covalent kinase inhibitors. Chem. Soc. Rev. 49, 2617–2687 (2020).

Mons, E. et al. The alkyne moiety as a latent electrophile in irreversible covalent small molecule inhibitors of cathepsin K. J. Am. Chem. Soc. 141, 3507–3514 (2019).

Di Lello, P. et al. Discovery of small-molecule inhibitors of ubiquitin specific protease 7 (USP7) using integrated NMR and in silico techniques. J. Med. Chem. 60, 10056–10070 (2017).

Gavory, G. et al. Discovery and characterization of highly potent and selective allosteric USP7 inhibitors. Nat. Chem. Biol. 14, 118–125 (2018).

Oltersdorf, T. et al. An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature 435, 677–681 (2005).

Tsai, J. et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc. Natl Acad. Sci. USA 105, 3041–3046 (2008).

Sreeramulu, S. et al. NMR quality control of fragment libraries for screening. J. Biomol. NMR https://doi.org/10.1007/s10858-020-00327-9 (2020).

Irie, T. & Sawa, M. 7-azaindole: a versatile scaffold for developing kinase inhibitors. Chem. Pharm. Bull. (Tokyo) 66, 29–36 (2018).

Erlanson, D. A., de Esch, I. J. P., Jahnke, W., Johnson, C. N. & Mortenson, P. N. Fragment-to-lead medicinal chemistry publications in 2018. J. Med. Chem. 63, 4430–4444 (2020).

Tron, A. E. et al. Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia. Nat. Commun. 9, 5341 (2018).

Creative Commons License
Este trabalho está licenciado sob uma licença Creative Commons Attribution 4.0 International License.

Copyright (c) 2020 Eber Coelho Paraguassu, Anneli Mercedes Celis de Cárdenas