The emerging role of mass spectrometry-based proteomics in drug discovery

F Meissner, J Geddes-McAlister, M Mann… - Nature Reviews Drug …, 2022 - nature.com
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 …

Drug repurposing: progress, challenges and recommendations

S Pushpakom, F Iorio, PA Eyers, KJ Escott… - Nature reviews Drug …, 2019 - nature.com
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 …

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 …

The target landscape of clinical kinase drugs

S Klaeger, S Heinzlmeir, M Wilhelm, H Polzer, B Vick… - Science, 2017 - science.org
INTRODUCTION Molecularly targeted drugs such as imatinib and crizotinib have
revolutionized the treatment of certain blood and lung cancers because of their remarkable …

Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors

M Reinecke, P Brear, L Vornholz, BT Berger… - Nature Chemical …, 2024 - nature.com
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 …

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 …

Proteome integral solubility alteration: a high-throughput proteomics assay for target deconvolution

M Gaetani, P Sabatier, AA Saei… - Journal of proteome …, 2019 - ACS Publications
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 …

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 …

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 …

[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 …