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
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 …
The target landscape of clinical kinase drugs
INTRODUCTION Molecularly targeted drugs such as imatinib and crizotinib have
revolutionized the treatment of certain blood and lung cancers because of their remarkable …
revolutionized the treatment of certain blood and lung cancers because of their remarkable …
Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors
Medicinal chemistry has discovered thousands of potent protein and lipid kinase inhibitors.
These may be developed into therapeutic drugs or chemical probes to study kinase biology …
These may be developed into therapeutic drugs or chemical probes to study kinase biology …
Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target
S Lechner, MIP Malgapo, C Grätz… - Nature chemical …, 2022 - nature.com
Drugs that target histone deacetylase (HDAC) entered the pharmacopoeia in the 2000s.
However, some enigmatic phenotypes suggest off-target engagement. Here, we developed …
However, some enigmatic phenotypes suggest off-target engagement. Here, we developed …
Proteome integral solubility alteration: a high-throughput proteomics assay for target deconvolution
Various agents, including drugs as well as nonmolecular stimuli, induce alterations in the
physicochemical properties of proteins in cell lysates, living cells, and organisms. These …
physicochemical properties of proteins in cell lysates, living cells, and organisms. These …
Choose and use your chemical probe wisely to explore cancer biology
J Blagg, P Workman - Cancer cell, 2017 - cell.com
Small-molecule chemical probes or tools have become progressively more important in
recent years as valuable reagents to investigate fundamental biological mechanisms and …
recent years as valuable reagents to investigate fundamental biological mechanisms and …
New perspectives, opportunities, and challenges in exploring the human protein kinome
LJ Wilson, A Linley, DE Hammond, FE Hood… - Cancer research, 2018 - AACR
The human protein kinome comprises 535 proteins that, with the exception of approximately
50 pseudokinases, control intracellular signaling networks by catalyzing the phosphorylation …
50 pseudokinases, control intracellular signaling networks by catalyzing the phosphorylation …
[HTML][HTML] Flavonoid 4, 4′-dimethoxychalcone induced ferroptosis in cancer cells by synergistically activating Keap1/Nrf2/HMOX1 pathway and inhibiting FECH
C Yang, T Wang, Y Zhao, X Meng, W Ding… - Free Radical Biology …, 2022 - Elsevier
Flavonoids are widely distributed in plants as secondary metabolites and have various
biological benefits such as anti-tumor, anti-oxidant, anti-inflammatory and anti-aging. We …
biological benefits such as anti-tumor, anti-oxidant, anti-inflammatory and anti-aging. We …