The emerging role of mass spectrometry-based proteomics in drug discovery
Proteins are the main targets of most drugs; however, system-wide methods to monitor
protein activity and function are still underused in drug discovery. Novel biochemical …
protein activity and function are still underused in drug discovery. Novel biochemical …
Drug repurposing: progress, challenges and recommendations
Given the high attrition rates, substantial costs and slow pace of new drug discovery and
development, repurposing of'old'drugs to treat both common and rare diseases is …
development, repurposing of'old'drugs to treat both common and rare diseases is …
Kinase inhibitors: the road ahead
FM Ferguson, NS Gray - Nature reviews Drug discovery, 2018 - nature.com
Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …
Rethink of EGFR in cancer with its kinase independent function on board
R Thomas, Z Weihua - Frontiers in oncology, 2019 - frontiersin.org
The epidermal growth factor receptor (EGFR) is one of most potent oncogenes that are
commonly altered in cancers. As a receptor tyrosine kinase, EGFR's kinase activity has been …
commonly altered in cancers. As a receptor tyrosine kinase, EGFR's kinase activity has been …
Molecular targets and anticancer activity of quinoline–chalcone hybrids: Literature review
MFA Mohamed, GEDA Abuo-Rahma - RSC advances, 2020 - pubs.rsc.org
α, β-Unsaturated chalcone moieties and quinoline scaffolds play an important role in
medicinal chemistry, especially in the identification and development of potential anticancer …
medicinal chemistry, especially in the identification and development of potential anticancer …
Combined CRISPRi/a-based chemical genetic screens reveal that rigosertib is a microtubule-destabilizing agent
Chemical libraries paired with phenotypic screens can now readily identify compounds with
therapeutic potential. A central limitation to exploiting these compounds, however, has been …
therapeutic potential. A central limitation to exploiting these compounds, however, has been …
DEEPScreen: high performance drug–target interaction prediction with convolutional neural networks using 2-D structural compound representations
The identification of physical interactions between drug candidate compounds and target
biomolecules is an important process in drug discovery. Since conventional screening …
biomolecules is an important process in drug discovery. Since conventional screening …
Aurora-PLK1 cascades as key signaling modules in the regulation of mitosis
V Joukov, A De Nicolo - Science signaling, 2018 - science.org
Mitosis is controlled by reversible protein phosphorylation involving specific kinases and
phosphatases. A handful of major mitotic protein kinases, such as the cyclin B–CDK1 …
phosphatases. A handful of major mitotic protein kinases, such as the cyclin B–CDK1 …
Current approaches in CRISPR-Cas9 mediated gene editing for biomedical and therapeutic applications
A single gene mutation can cause a number of human diseases that affect the quality of life.
Until the development of clustered regularly interspaced short palindromic repeats …
Until the development of clustered regularly interspaced short palindromic repeats …
CRISPR/Cas9–An evolving biological tool kit for cancer biology and oncology
The development of genetic engineering in the 1970s marked a new frontier in genome-
editing technology. Gene-editing technologies have provided a plethora of benefits to the life …
editing technology. Gene-editing technologies have provided a plethora of benefits to the life …