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 …
Spirocyclic scaffolds in medicinal chemistry
Spirocyclic scaffolds are incorporated in various approved drugs and drug candidates. The
increasing interest in less planar bioactive compounds has given rise to the development of …
increasing interest in less planar bioactive compounds has given rise to the development of …
The Warburg effect 97 years after its discovery
RM Pascale, DF Calvisi, MM Simile, CF Feo, F Feo - Cancers, 2020 - mdpi.com
Simple Summary The deregulation of the oxidative metabolism in cancer cells,
characterized by an increased ratio between glycolysis and oxygen consumption (Warburgv …
characterized by an increased ratio between glycolysis and oxygen consumption (Warburgv …
Emerging and re-emerging warheads for targeted covalent inhibitors: applications in medicinal chemistry and chemical biology
M Gehringer, SA Laufer - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …
Revisited metabolic control and reprogramming cancers by means of the warburg effect in tumor cells
Aerobic glycolysis is an emerging hallmark of many human cancers, as cancer cells are
defined as a “metabolically abnormal system”. Carbohydrates are metabolically …
defined as a “metabolically abnormal system”. Carbohydrates are metabolically …
Global profiling of lysine reactivity and ligandability in the human proteome
Nucleophilic amino acids make important contributions to protein function, including
performing key roles in catalysis and serving as sites for post-translational modification …
performing key roles in catalysis and serving as sites for post-translational modification …
Click chemistry for drug development and diverse chemical–biology applications
P Thirumurugan, D Matosiuk, K Jozwiak - Chemical reviews, 2013 - ACS Publications
Chemistry, traditionally being the science of synthesis and structural manipulations of
molecules, has gradually undertaken the more challenging task of biology-oriented …
molecules, has gradually undertaken the more challenging task of biology-oriented …
Target identification and mechanism of action in chemical biology and drug discovery
M Schenone, V Dančík, BK Wagner… - Nature chemical …, 2013 - nature.com
Target-identification and mechanism-of-action studies have important roles in small-
molecule probe and drug discovery. Biological and technological advances have resulted in …
molecule probe and drug discovery. Biological and technological advances have resulted in …
Chemical proteomics approaches for identifying the cellular targets of natural products
Covering: 2010 up to 2016 Deconvoluting the mode of action of natural products and drugs
remains one of the biggest challenges in chemistry and biology today. Chemical proteomics …
remains one of the biggest challenges in chemistry and biology today. Chemical proteomics …
Targeting cancer metabolism: a therapeutic window opens
MG Vander Heiden - Nature reviews Drug discovery, 2011 - nature.com
Genetic events in cancer activate signalling pathways that alter cell metabolism. Clinical
evidence has linked cell metabolism with cancer outcomes. Together, these observations …
evidence has linked cell metabolism with cancer outcomes. Together, these observations …