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 …

Spirocyclic scaffolds in medicinal chemistry

K Hiesinger, D Dar'in, E Proschak… - Journal of Medicinal …, 2020 - ACS Publications
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 …

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 …

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 …

Revisited metabolic control and reprogramming cancers by means of the warburg effect in tumor cells

A Fukushi, HD Kim, YC Chang, CH Kim - International journal of …, 2022 - mdpi.com
Aerobic glycolysis is an emerging hallmark of many human cancers, as cancer cells are
defined as a “metabolically abnormal system”. Carbohydrates are metabolically …

Global profiling of lysine reactivity and ligandability in the human proteome

SM Hacker, KM Backus, MR Lazear, S Forli… - Nature …, 2017 - nature.com
Nucleophilic amino acids make important contributions to protein function, including
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 …

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 …

Chemical proteomics approaches for identifying the cellular targets of natural products

MH Wright, SA Sieber - Natural product reports, 2016 - pubs.rsc.org
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 …

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 …