Targeting ribosome biogenesis in cancer: lessons learned and way forward
A Zisi, J Bartek, MS Lindström - Cancers, 2022 - mdpi.com
Simple Summary Cells need to produce ribosomes to sustain continuous proliferation and
expand in numbers, a feature that is even more prominent in uncontrollably proliferating …
expand in numbers, a feature that is even more prominent in uncontrollably proliferating …
CETSA and thermal proteome profiling strategies for target identification and drug discovery of natural products
Y Tu, L Tan, H Tao, Y Li, H Liu - Phytomedicine, 2023 - Elsevier
Background Monitoring target engagement at various stages of drug development is
essential for natural product (NP)-based drug discovery and development. The cellular …
essential for natural product (NP)-based drug discovery and development. The cellular …
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 …
Identifying purine nucleoside phosphorylase as the target of quinine using cellular thermal shift assay
Mechanisms of action (MoAs) have been elusive for most antimalarial drugs in clinical use.
Decreasing responsiveness to antimalarial treatments stresses the need for a better …
Decreasing responsiveness to antimalarial treatments stresses the need for a better …
Current advances in CETSA
TA Tolvanen - Frontiers in molecular biosciences, 2022 - frontiersin.org
Knowing that the drug candidate binds to its intended target is a vital part of drug discovery.
Thus, several labeled and label-free methods have been developed to study target …
Thus, several labeled and label-free methods have been developed to study target …
Large-scale characterization of drug mechanism of action using proteome-wide thermal shift assays
In response to an ever-increasing demand of new small molecules therapeutics, numerous
chemical and genetic tools have been developed to interrogate compound mechanism of …
chemical and genetic tools have been developed to interrogate compound mechanism of …
Decitabine-and 5-azacytidine resistance emerges from adaptive responses of the pyrimidine metabolism network
Mechanisms-of-resistance to decitabine and 5-azacytidine, mainstay treatments for myeloid
malignancies, require investigation and countermeasures. Both are nucleoside analog pro …
malignancies, require investigation and countermeasures. Both are nucleoside analog pro …
Preclinical efficacy of azacitidine and venetoclax for infant KMT2A-rearranged acute lymphoblastic leukemia reveals a new therapeutic strategy
Infants with KMT2A-rearranged B-cell acute lymphoblastic leukemia (ALL) have a dismal
prognosis. Survival outcomes have remained static in recent decades despite treatment …
prognosis. Survival outcomes have remained static in recent decades despite treatment …
Oral tetrahydrouridine and decitabine for non-cytotoxic epigenetic gene regulation in sickle cell disease: a randomized phase 1 study
R Molokie, D Lavelle, M Gowhari, M Pacini… - PLoS …, 2017 - journals.plos.org
Background Sickle cell disease (SCD), a congenital hemolytic anemia that exacts terrible
global morbidity and mortality, is driven by polymerization of mutated sickle hemoglobin …
global morbidity and mortality, is driven by polymerization of mutated sickle hemoglobin …
Nucleobase and nucleoside analogues: resistance and re-sensitisation at the level of pharmacokinetics, pharmacodynamics and metabolism
Antimetabolites, in particular nucleobase and nucleoside analogues, are cytotoxic drugs
that, starting from the small field of paediatric oncology, in combination with other …
that, starting from the small field of paediatric oncology, in combination with other …