Targeting AURKA in Cancer: molecular mechanisms and opportunities for Cancer therapy
R Du, C Huang, K Liu, X Li, Z Dong - Molecular cancer, 2021 - Springer
Aurora kinase A (AURKA) belongs to the family of serine/threonine kinases, whose
activation is necessary for cell division processes via regulation of mitosis. AURKA shows …
activation is necessary for cell division processes via regulation of mitosis. AURKA shows …
Computational methods in drug discovery
Computer-aided drug discovery/design methods have played a major role in the
development of therapeutically important small molecules for over three decades. These …
development of therapeutically important small molecules for over three decades. These …
Irreversible protein kinase inhibitors: balancing the benefits and risks
T Barf, A Kaptein - Journal of medicinal chemistry, 2012 - ACS Publications
In the relatively young but expanding field of irreversible kinase inhibitor drug discovery,
there are two main developments that are of central importance. First, the patients have …
there are two main developments that are of central importance. First, the patients have …
Pyrimidine-based EGFR TK inhibitors in targeted cancer therapy
Despite significant improvements of new treatment options, cancer continues to represent as
one of the most common and fatal disease. The EGFR signaling pathway is considered as a …
one of the most common and fatal disease. The EGFR signaling pathway is considered as a …
Overview of recent strategic advances in medicinal chemistry
G Wu, T Zhao, D Kang, J Zhang, Y Song… - Journal of medicinal …, 2019 - ACS Publications
Introducing novel strategies, concepts, and technologies that speed up drug discovery and
the drug development cycle is of great importance both in the highly competitive …
the drug development cycle is of great importance both in the highly competitive …
A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies
AC Borisa, HG Bhatt - European journal of medicinal chemistry, 2017 - Elsevier
Aurora kinase belongs to serine/threonine kinase family which controls cell division.
Therapeutic inhibition of Aurora kinase showed great promise as probable anticancer …
Therapeutic inhibition of Aurora kinase showed great promise as probable anticancer …
Pyrimidine and fused pyrimidine derivatives as promising protein kinase inhibitors for cancer treatment
KRA Abdellatif, RB Bakr - Medicinal Chemistry Research, 2021 - Springer
Pyrimidine ring and its fused derivatives including pyrazolo [3, 4-d] pyrimidine, pyrido [2, 3-d]
pyrimidine, quinazoline, and furo [2, 3-d] pyrimidine compounds had received much interest …
pyrimidine, quinazoline, and furo [2, 3-d] pyrimidine compounds had received much interest …
Structure-based virtual screening approach for discovery of covalently bound ligands
D Toledo Warshaviak, G Golan… - Journal of chemical …, 2014 - ACS Publications
We present a fast and effective covalent docking approach suitable for large-scale virtual
screening (VS). We applied this method to four targets (HCV NS3 protease, Cathepsin K …
screening (VS). We applied this method to four targets (HCV NS3 protease, Cathepsin K …
Protein kinase inhibitor design by targeting the Asp-Phe-Gly (DFG) motif: the role of the DFG motif in the design of epidermal growth factor receptor inhibitors
YH Peng, HY Shiao, CH Tu, PM Liu… - Journal of medicinal …, 2013 - ACS Publications
The Asp-Phe-Gly (DFG) motif plays an important role in the regulation of kinase activity.
Structure-based drug design was performed to design compounds able to interact with the …
Structure-based drug design was performed to design compounds able to interact with the …
Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine790→ …
The EGFRT790M mutant contributes approximately 50% to clinically acquired resistance
against gefitinib or erlotinib. However, almost all the single agent clinical trials of the second …
against gefitinib or erlotinib. However, almost all the single agent clinical trials of the second …