Small molecule kinase inhibitors for the treatment of brain cancer

TP Heffron - Journal of medicinal chemistry, 2016 - ACS Publications
In addition to each of the factors that govern the identification of a successful oncology drug
candidate, drug discovery aimed at treating neurological cancer must also consider the …

Alvocidib (flavopiridol) for the treatment of chronic lymphocytic leukemia

PH Wiernik - Expert opinion on investigational drugs, 2016 - Taylor & Francis
Introduction: Alvocidib, which has orphan drug designation in chronic lymphocytic leukemia
(CLL) from the FDA and the EMA, is a plant-derived semisynthetic flavone that acts as a …

Overcoming resistance to the THZ series of covalent transcriptional CDK inhibitors

Y Gao, T Zhang, H Terai, SB Ficarro, N Kwiatkowski… - Cell chemical …, 2018 - cell.com
Irreversible inhibition of transcriptional cyclin-dependent kinases (CDKs) provides a
therapeutic strategy for cancers that rely on aberrant transcription; however, lack of …

Ribociclib shows potential for pharmacokinetic drug-drug interactions being a substrate of ABCB1 and potent inhibitor of ABCB1, ABCG2 and CYP450 isoforms in vitro

A Sorf, J Hofman, R Kučera, F Staud… - Biochemical …, 2018 - Elsevier
Ribociclib is a novel cyclin-dependent kinase (CDK) 4 and 6 selective inhibitor that recently
gained breakthrough therapy status and global approval for advanced breast cancer …

Effective drug delivery in diffuse intrinsic pontine glioma: a theoretical model to identify potential candidates

FE El-Khouly, DG Van Vuurden, T Stroink… - Frontiers in …, 2017 - frontiersin.org
Despite decades of clinical trials for diffuse intrinsic pontine glioma (DIPG), patient survival
does not exceed 10% at two years post-diagnosis. Lack of benefit from systemic …

European mtDNA variants are associated with differential responses to cisplatin, an anticancer drug: implications for drug resistance and side effects

TH Patel, L Norman, S Chang, S Abedi, C Liu… - Frontiers in …, 2019 - frontiersin.org
Background: Cisplatin, a powerful antitumor agent, causes formation of DNA adducts, and
activation of apoptotic pathways. Presently, cisplatin resistance develops in up to 70% of …

Brivanib Exhibits Potential for Pharmacokinetic Drug–Drug Interactions and the Modulation of Multidrug Resistance through the Inhibition of Human ABCG2 Drug …

J Hofman, A Sorf, D Vagiannis, S Sucha… - Molecular …, 2019 - ACS Publications
Brivanib, a promising tyrosine kinase inhibitor, is currently undergoing advanced stages of
clinical evaluation for solid tumor therapy. In this work, we investigated possible interactions …

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

V Namasivayam, K Silbermann, J Pahnke… - Computational and …, 2021 - Elsevier
Computer-aided pattern analysis (C@ PA) was recently presented as a powerful tool to
predict multitarget ABC transporter inhibitors. The backbone of this computational …

Epithelial–mesenchymal transition and gastric cancer stem cell

P Xia, XY Xu - Tumor Biology, 2017 - journals.sagepub.com
Gastric cancer remains a big health problem in China. Gastric cancer cells contain a small
subpopulation of cells that exhibit capabilities of differentiation and tumorigenicity. A putative …

Inhibition of cyclin-dependent kinases by AT7519 is effective to overcome chemoresistance in colon and cervical cancer

C Xi, L Wang, J Yu, H Ye, L Cao, Z Gong - Biochemical and biophysical …, 2019 - Elsevier
Abstract Cyclin-dependent kinases (CDK), a family of heterodimeric kinases that play central
roles in regulation of cell cycle progression and transcription, have garnered attention in …