Natural Aromatic Compounds as Scaffolds to Develop Selective G-Quadruplex Ligands: From Previously Reported Berberine Derivatives to New Palmatine Analogues

Autor: Marco Franceschin, Lorenzo Cianni, Massimo Pitorri, Emanuela Micheli, Stefano Cacchione, Claudio Frezza, Mauro Serafini, Ming-Hao Hu, Huafi Su, Zhishu Huang, Lianquan Gu, Armandodoriano Bianco

Publikováno v: Molecules, Vol 23, Iss 6, p 1423 (2018)

In this paper, the selective interactions of synthetic derivatives of two natural compounds, berberine and palmatine, with DNA G-quadruplex structures were reported. In particular, the previous works on this subject concerning berberine were further

Externí odkaz: https://doaj.org/article/750815bcf13a4b359fa7e87123b56c1f

N-Sulfonyl dipeptide nitriles as inhibitors of human cathepsin S. In silico design, synthesis and biochemical characterization

Autor: Jürgen Bajorath, Carlos A. Montanari, Jiafei Yin, Michael Gütschow, Carina Lemke, Christian Feldmann, Daniela De Vita, Fernanda dos Reis Rocho, Lorenzo Cianni, Erik Gilberg, Ulrike Bartz

Publikováno v: Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP

A library of cathepsin S inhibitors of the dipeptide nitrile chemotype, bearing a bioisosteric sulfonamide moiety, was synthesized. Kinetic investigations were performed at four human cysteine proteases, i.e. cathepsins S, B, K and L. Compound 12 wit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aee2526b3b5bca0ed211a7033399460d
http://hdl.handle.net/11573/1477075

Assessment of the cruzain cysteine protease reversible and Irreversible covalent inhibition mechanism

Autor: José Rogério A. Silva, Daniela De Vita, Jerônimo Lameira, Fabiana Rosini, Andrei Leitão, Pedro Henrique Jatai Batista, Lorenzo Cianni, Carlos A. Montanari, Deborah Araujo

Publikováno v: Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP

Reversible and irreversible covalent ligands are advanced cysteine protease inhibitors in the drug development pipeline. K777 is an irreversible inhibitor of cruzain, a necessary enzyme for the survival of the Trypanosoma cruzi (T. cruzi) parasite, t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2a29c283c53fae550c9f270c7bdab1f
http://hdl.handle.net/11573/1404853

A comparative study of warheads for design of cysteine protease inhibitors

Autor: Caio Haddad Franco, Josmar R. Rocha, Carolina B. Moraes, Antonio C. B. Burtoloso, Daniel G. Silva, Daniela De Vita, Carlos A. Montanari, Peter W. Kenny, Andrei Leitão, Jean F. R. Ribeiro, Lorenzo Cianni, Lucio H. Freitas-Junior

Publikováno v: Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP

The effects on potency of cruzain inhibition of replacing a nitrile group with alternative warheads were explored. The oxime was almost an order of magnitude more potent than the corresponding nitrile and has the potential to provide access to the pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a458345f2b22da4227d15e544da7adc
https://doi.org/10.1016/j.bmcl.2017.10.002

Mapping the S1 and S1’ subsites of cysteine proteases with new dipeptidyl nitrile inhibitors as trypanocidal agents

Autor: Sérgio de Albuquerque, Christian Feldmann, Carla D. Lopes, Erik Gilberg, Jean F. R. Ribeiro, Fabiana Rosini, Andrei Leitão, Stefan Laufer, Carina Lemke, Lorenzo Cianni, Michael Gütschow, Jürgen Bajorath, Daiane Y. Tezuka, Carlos A. Montanari, Fernanda dos Reis Rocho

Publikováno v: PLoS Neglected Tropical Diseases
PLoS Neglected Tropical Diseases, Vol 14, Iss 3, p e0007755 (2020)
Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP

The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. A series of 26 new compounds were designed, synthesized, and tested against the recombinant cruzain (Cz) to map it

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbfec629b9cbe1226217c69826b410da
https://doi.org/10.1101/760736