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 …

Opportunities for tapping into three-dimensional chemical space through a quaternary carbon

TT Talele - Journal of Medicinal Chemistry, 2020 - ACS Publications
A quaternary carbon bears four other carbon substituents or combination of four non-
hydrogen substituents at four vertices of a tetrahedron. The spirocyclic quaternary carbon …

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

B Noce, E Di Bello, R Fioravanti, A Mai - Frontiers in pharmacology, 2023 - frontiersin.org
Histone lysine-specific demethylase 1 (LSD1/KDM1A) was first identified in 2004 as an
epigenetic enzyme able to demethylate specific lysine residues of histone H3, namely …

Enhancer activation by pharmacologic displacement of LSD1 from GFI1 induces differentiation in acute myeloid leukemia

A Maiques-Diaz, GJ Spencer, JT Lynch, F Ciceri… - Cell reports, 2018 - cell.com
Pharmacologic inhibition of LSD1 promotes blast cell differentiation in acute myeloid
leukemia (AML) with MLL translocations. The assumption has been that differentiation is …

Reversible lysine specific demethylase 1 (LSD1) inhibitors: a promising wrench to impair LSD1

XJ Dai, Y Liu, LP Xue, XP Xiong, Y Zhou… - Journal of medicinal …, 2021 - ACS Publications
As a flavin adenine dinucleotide (FAD)-dependent monoamine oxidase, lysine specific
demethylase 1 (LSD1/KDM1A) functions as a transcription coactivator or corepressor to …

Targeting LSD1 for acute myeloid leukemia (AML) treatment

S Zhang, M Liu, Y Yao, B Yu, H Liu - Pharmacological research, 2021 - Elsevier
Targeted therapy for acute myeloid leukemia (AML) is an effective strategy, but currently
there are very limited therapeutic targets for AML treatment. Histone lysine specific …

High-throughput screening for the discovery of enzyme inhibitors

MD Lloyd - Journal of Medicinal Chemistry, 2020 - ACS Publications
Enzymes are common targets in high-throughput screening and related campaigns. An
analysis of papers published between 1990 and 2018 showed that kinases were the most …

Therapeutic potential of targeting LSD1/KDM1A in cancers

X Zhang, X Wang, T Wu, W Yin, J Yan, Y Sun… - Pharmacological …, 2022 - Elsevier
LSD1 was the first histone demethylase identified by Professor Shi Yang and his team
members in 2004. LSD1 employs FAD as its cofactor, which catalyzes the demethylation of …

[HTML][HTML] Development of the triazole-fused pyrimidine derivatives as highly potent and reversible inhibitors of histone lysine specific demethylase 1 (LSD1/KDM1A)

Z Li, L Ding, Z Li, Z Wang, F Suo, D Shen… - … Pharmaceutica Sinica B, 2019 - Elsevier
Histone lysine specific demethylase 1 (LSD1) has been recognized as an important
modulator in post-translational process in epigenetics. Dysregulation of LSD1 has been …

Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors

X Zhang, H Huang, Z Zhang, J Yan, T Wu, W Yin… - European Journal of …, 2021 - Elsevier
Abstract Lysine-specific demethylase 1 (LSD1) is a FAD-dependent enzyme, which has
been proposed as a promising target for therapeutic cancer. Herein, a series of benzofuran …