Epigenetic protein families: a new frontier for drug discovery
Epigenetic regulation of gene expression is a dynamic and reversible process that
establishes normal cellular phenotypes but also contributes to human diseases. At the …
establishes normal cellular phenotypes but also contributes to human diseases. At the …
The Curtius rearrangement: mechanistic insight and recent applications in natural product syntheses
The Curtius rearrangement is a versatile reaction in which a carboxylic acid can be
converted to an isocyanate through an acyl azide intermediate under mild conditions. The …
converted to an isocyanate through an acyl azide intermediate under mild conditions. The …
Iridium‐Catalyzed Enantioselective C(sp3)−H Borylation of Aminocyclopropanes
Y Shi, Y Yang, S Xu - Angewandte Chemie, 2022 - Wiley Online Library
Transition‐metal‐catalyzed regio‐and stereo‐controllable C− H functionalization remains a
formidable challenge in asymmetric catalysis. Herein, we disclose the first example of …
formidable challenge in asymmetric catalysis. Herein, we disclose the first example of …
Methods for the synthesis of donor-acceptor cyclopropanes
The interest in cyclopropane derivatives is caused by the facts that, first, the three-carbon
ring is present in quite a few natural and biologically active compounds and, second …
ring is present in quite a few natural and biologically active compounds and, second …
Lysine demethylases inhibitors
T Suzuki, N Miyata - Journal of medicinal chemistry, 2011 - ACS Publications
Recent studies have revealed that chromatin remodeling, caused by DNA methylation and
histone modifications such as acetylation, methylation, and phosphorylation, plays a pivotal …
histone modifications such as acetylation, methylation, and phosphorylation, plays a pivotal …
Novel KDM1A inhibitors induce differentiation and apoptosis of glioma stem cells via unfolded protein response pathway
Glioma stem cells (GSCs) have a central role in glioblastoma (GBM) development and
chemo/radiation resistance, and their elimination is critical for the development of efficient …
chemo/radiation resistance, and their elimination is critical for the development of efficient …
TCPs: privileged scaffolds for identifying potent LSD1 inhibitors for cancer therapy
Since the first lysine-specific demethylase (KDM), lysine-specific demethylase 1 (LSD1), was
characterized in 2004, several families of KDMs have been identified. LSD1 can specifically …
characterized in 2004, several families of KDMs have been identified. LSD1 can specifically …
Stereodivergent Synthesis of Arylcyclopropylamines by Sequential C H Borylation and Suzuki–Miyaura Coupling
S Miyamura, M Araki, T Suzuki… - Angewandte …, 2015 - Wiley Online Library
A step‐economical and stereodivergent synthesis of privileged 2‐arylcyclopropylamines
(ACPAs) through a C (sp3) H borylation and Suzuki–Miyaura coupling sequence has been …
(ACPAs) through a C (sp3) H borylation and Suzuki–Miyaura coupling sequence has been …
Histone lysine demethylase inhibitors
The dynamic regulation of covalent modifications to histones is essential for maintaining
genomic integrity and cell identity and is often compromised in cancer. Aberrant expression …
genomic integrity and cell identity and is often compromised in cancer. Aberrant expression …
Lysine-specific demethylase 1-selective inactivators: protein-targeted drug delivery mechanism.
Drug drop off: Given that lysine‐specific demethylase 1 (LSD1) could be potently and
selectively inactivated by delivering phenylcyclopropylamine (PCPA), a weak and …
selectively inactivated by delivering phenylcyclopropylamine (PCPA), a weak and …