The influence of the gut microbiota on the bioavailability of oral drugs

Autor: Ying Han, Xintong Zhang, Wei Huang, Zhonggao Gao, Mingji Jin

Publikováno v: Acta Pharmaceutica Sinica B, Vol 11, Iss 7, Pp 1789-1812 (2021)
Acta Pharmaceutica Sinica. B

Due to its safety, convenience, low cost and good compliance, oral administration attracts lots of attention. However, the efficacy of many oral drugs is limited to their unsatisfactory bioavailability in the gastrointestinal tract. One of the critic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d001e27a816f9de7d75ff16dd2143ec
http://www.sciencedirect.com/science/article/pii/S2211383520307279

Preclinical efficacy against acute myeloid leukaemia of SH1573, a novel mutant IDH2 inhibitor approved for clinical trials in China

Autor: Shengtao Yuan, Han Luwei, Dezhen Peng, Zhiqiang Wang, Hongzhi Du, Li Sun, Zhang Xian, Zhao Liwen, Danyu Du, Ligong Lu, Meixiao Zhan, Zhibo Zhang, Yong Li

Publikováno v: Acta Pharmaceutica Sinica B, Vol 11, Iss 6, Pp 1526-1540 (2021)
Acta Pharmaceutica Sinica. B

Acute myeloid leukaemia (AML) is the most common form of acute leukaemia in adults, with increasing incidence with age and a generally poor prognosis. Almost 20% of AML patients express mutant isocitrate dehydrogenase 2 (mIDH2), which leads to the ac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1989ebe7a9db18d2c8b52de1673685c1
http://www.sciencedirect.com/science/article/pii/S2211383521000769

Scaffold fragmentation and substructure hopping reveal potential, robustness, and limits of computer-aided pattern analysis (C@PA)

Autor: Vigneshwaran Namasivayam, Jens Pahnke, Katja Silbermann, Michael Wiese, Sven Marcel Stefan

Publikováno v: Computational and Structural Biotechnology Journal
Computational and Structural Biotechnology Journal, Vol 19, Iss, Pp 3269-3283 (2021)

Graphical abstract
Highlights • Exploratory changes in substructure patterns are well tolerated by C@PA. • Extended positive substructures support prediction capability. • Increased biological hit rate of 40% for multitarget pan-ABC transp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d40715d0bceb0276ecc21ab6730bd845
https://doi.org/10.1016/j.csbj.2021.05.018

Porphyrin-Induced Protein Oxidation and Aggregation as a Mechanism of Porphyria-Associated Cell Injury

Autor: Juliana Bragazzi Cunha, Jordan A. Shavit, Herbert L. Bonkovsky, Dhiman Maitra, Jared S. Elenbaas, M. Bishr Omary

Publikováno v: Cellular and Molecular Gastroenterology and Hepatology, Vol 8, Iss 4, Pp 535-548 (2019)
Cellular and Molecular Gastroenterology and Hepatology

Genetic porphyrias comprise eight diseases caused by defects in the heme biosynthetic pathway that lead to accumulation of heme precursors. Consequences of porphyria include photosensitivity, liver damage and increased risk of hepatocellular carcinom

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b0af3ebb574e4ee6cf3f3b54e0ba117c
https://doi.org/10.1016/j.jcmgh.2019.06.006

Improved Brain Penetration and Antitumor Efficacy of Temozolomide by Inhibition of ABCB1 and ABCG2

Autor: de Gooijer, Mark C, de Vries, Nienke A, Buckle, Tessa, Buil, Levi C M, Beijnen, Jos H, Boogerd, Willem, van Tellingen, Olaf, Afd Pharmacoepi & Clinical Pharmacology, Pharmacoepidemiology and Clinical Pharmacology

Publikováno v: Neoplasia: An International Journal for Oncology Research, Vol 20, Iss 7, Pp 710-720 (2018)
Neoplasia, 20(7), 710. Elsevier
Neoplasia (New York, N.Y.)

The anticancer drug temozolomide is the only drug with proven activity against high-grade gliomas and has therefore become a part of the standard treatment of these tumors. P-glycoprotein (P-gp; ABCB1) and breast cancer resistance protein (BCRP; ABCG

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::172288b7db60137160830a6682e4d13e
https://doi.org/10.1016/j.neo.2018.05.001