5 documents found, page 1 of 1
Therapeutic targeting of PD-1/PD-L1 blockade by novel small-molecule inhibitors...
Acúrcio, Rita C; Pozzi, Sabina; Carreira, Barbara; Pojo, Marta; Gómez-Cebrián, Nuria; Casimiro, Sandra; Fernandes, Adelaide; Barateiro, AndreiaBackground: Inhibiting programmed cell death protein 1 (PD-1) or PD-ligand 1 (PD-L1) has shown exciting clinical outcomes in diverse human cancers. So far, only monoclonal antibodies are approved as PD-1/PD-L1 inhibitors. While significant clinical outcomes are observed on patients who respond to these therapeutics, a large proportion of the patients do not benefit from the currently available immune checkpoint...
Modulation of Human Phenylalanine Hydroxylase by 3-Hydroxyquinolin-2(1H)-One De...
Lopes, Raquel R.; Tomé, Catarina S.; Russo, Roberto; Paterna, Roberta; Leandro, João; Candeias, Nuno R.; Gonçalves, Lídia; Teixeira, MiguelPhenylketonuria (PKU) is a genetic disease caused by deficient activity of human phenylalanine hydroxylase (hPAH) that, when untreated, can lead to severe psychomotor impairment. Protein misfolding is recognized as the main underlying pathogenic mechanism of PKU. Therefore, the use of stabilizers of protein structure and/or activity is an attractive therapeutic strategy for this condition. Here, we report that ...
Spray dried Petiveria alliacea extracts: standardization and evaluation of the ...
Souza, C. R.; Guedes, R. C.; Fusco-Almeida, A. M. [UNESP]; Oliveira, W. P.Made available in DSpace on 2020-12-10T16:31:20Z (GMT). No. of bitstreams: 0 Previous issue date: 2013-09-01; Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, BR-14040903 Ribeirao Preto, SP, Brazil; UNESP, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil; UNESP, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP, Brazil
Chemical patterns of proteasome inhibitors: lessons learned from two decades of...
Guedes, R. A.; Aniceto, N.; Andrade, M. A. P.; Salvador, J. A. R.; Guedes, R. C.Drug discovery now faces a new challenge, where the availability of experimental data is no longer the limiting step, and instead, making sense of the data has gained a new level of importance, propelled by the extensive incorporation of cheminformatics and bioinformatics methodologies into the drug discovery and development pipeline. These enable, for example, the inference of structure-activity relationships ...
3-Hydroxypyrrolidine and (3,4)-dihydroxypyrrolidine derivatives: inhibition of ...
Carreiro, E. P.; Louro, P.; Adriano, G; Guedes, R. A.; Vannuchic, N.; Costa, A. R.; Antunes, C. M.; Guedes, R. C.; Burke, A.J.Thirteen pyrrolidine-based iminosugar derivatives have been synthesized and evaluated for inhibition of α-glucosidase from rat intestine. The compounds studied were the non-hydroxy, mono-hydroxy and dihydroxypyrrolidines. All the compounds were N-benzylated apart from one. Four of the compounds had a carbonyl group in the 2,5-position of the pyrrolidine ring. The most promising iminosugar was the trans-3,4-dihy...