[HTML][HTML] Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective
T Webb, C Craigon, A Ciulli - Bioorganic & Medicinal Chemistry Letters, 2022 - Elsevier
Epigenetic modulators perform critical functions in gene expression for rapid adaption to
external stimuli and are prevalent in all higher-order organisms. The establishment of a link …
external stimuli and are prevalent in all higher-order organisms. The establishment of a link …
The bump-and-hole tactic: expanding the scope of chemical genetics
K Islam - Cell chemical biology, 2018 - cell.com
Successful mapping of the human genome has sparked a widespread interest in
deciphering functional information encoded in gene sequences. However, because of the …
deciphering functional information encoded in gene sequences. However, because of the …
2-Oxoglutarate derivatives can selectively enhance or inhibit the activity of human oxygenases
Y Nakashima, L Brewitz, A Tumber, E Salah… - Nature …, 2021 - nature.com
Oxoglutarate (2OG) oxygenases are validated agrochemical and human drug targets. The
potential for modulating their activity with 2OG derivatives has not been explored, possibly …
potential for modulating their activity with 2OG derivatives has not been explored, possibly …
Activity Guided Azide-methyllysine Photo-trapping for Substrate Profiling of Lysine Demethylases
J Kuwik, K Hinkelman, M Waldman… - Journal of the …, 2023 - ACS Publications
Reversible post-translational modifications (PTMs) are key to establishing protein–protein
and protein–nucleic acid interactions that govern a majority of the signaling pathways in …
and protein–nucleic acid interactions that govern a majority of the signaling pathways in …
Chemogenetics of cell surface receptors: beyond genetic and pharmacological approaches
Y Miura, A Senoo, T Doura, S Kiyonaka - RSC Chemical Biology, 2022 - pubs.rsc.org
Cell surface receptors transmit extracellular information into cells. Spatiotemporal regulation
of receptor signaling is crucial for cellular functions, and dysregulation of signaling causes …
of receptor signaling is crucial for cellular functions, and dysregulation of signaling causes …
Substitution of 2-oxoglutarate alters reaction outcomes of the Pseudomonas savastanoi ethylene-forming enzyme
In seeding plants, biosynthesis of the phytohormone ethylene, which regulates processes
including fruit ripening and senescence, is catalyzed by 1-aminocyclopropane-1-carboxylic …
including fruit ripening and senescence, is catalyzed by 1-aminocyclopropane-1-carboxylic …
Chemogenetics a robust approach to pharmacology and gene therapy
O Keifer, K Kambara, A Lau, S Makinson… - Biochemical …, 2020 - Elsevier
Modern developments in organic chemistry, molecular biology, virology, and genetics have
opened new, exciting possibilities to better understand physiology and to create innovative …
opened new, exciting possibilities to better understand physiology and to create innovative …
Natural and synthetic 2-oxoglutarate derivatives are substrates for oncogenic variants of human isocitrate dehydrogenase 1 and 2
Variants of isocitrate dehydrogenase (IDH) 1 and 2 (IDH1/2) alter metabolism in cancer cells
by catalyzing the NADPH-dependent reduction of 2-oxoglutarate (2OG) to (2R) …
by catalyzing the NADPH-dependent reduction of 2-oxoglutarate (2OG) to (2R) …
Kinetic and inhibition studies on human Jumonji-C (JmjC) domain-containing protein 5
Jumonji-C (JmjC) domain-containing protein 5 (JMJD5) is a human 2-oxoglutarate (2OG)
and Fe (II)-dependent oxygenase which catalyses the post-translational C3 hydroxylation of …
and Fe (II)-dependent oxygenase which catalyses the post-translational C3 hydroxylation of …
A rapid mass spectrometric method for the measurement of catalytic activity of ten-eleven translocation enzymes
B Sudhamalla, D Dey, M Breski, K Islam - Analytical biochemistry, 2017 - Elsevier
Enzymatic methylation at carbon five on cytosine (5mC) in DNA is a hallmark of mammalian
epigenetic programming and is critical to gene regulation during early embryonic …
epigenetic programming and is critical to gene regulation during early embryonic …