Structure, function and inhibition of critical protein–protein interactions involving mixed lineage leukemia 1 and its fusion oncoproteins

X Li, Y Song - Journal of hematology & oncology, 2021 - Springer
Abstract Mixed lineage leukemia 1 (MLL1, also known as MLL or KMT2A) is an important
transcription factor and histone-H3 lysine-4 (H3K4) methyltransferase. It is a master …

The design and development of covalent protein-protein interaction inhibitors for cancer treatment

SS Cheng, GJ Yang, W Wang, CH Leung… - Journal of hematology & …, 2020 - Springer
Protein-protein interactions (PPIs) are central to a variety of biological processes, and their
dysfunction is implicated in the pathogenesis of a range of human diseases, including …

Divergent reactivity of sulfinates with pyridinium salts based on one-versus two-electron pathways

M Kim, E You, S Park, S Hong - Chemical Science, 2021 - pubs.rsc.org
One of the main goals of modern synthesis is to develop distinct reaction pathways from
identical starting materials for the efficient synthesis of diverse compounds. Herein, we …

Chemical biology and pharmacology of histone lysine methylation inhibitors

SH Barghout, RAC Machado… - Biochimica et Biophysica …, 2022 - Elsevier
Histone lysine methylation is a post-translational modification that plays a key role in the
epigenetic regulation of a broad spectrum of biological processes. Moreover, the …

Sulfonylation of Pyridyl Phosphonium Salts with Sulfinate Salts in Aqueous Media for the Synthesis of 4-Pyridyl Sulfones via C–P Bond Cleavage

BJ Huo, WW Wang, YJ Huang, XQ Chu, H Xu… - Organic …, 2024 - ACS Publications
A Na2S2O8-initiated sulfonylation of pyridyl phosphonium salts with sulfinate salts in
aqueous media has been developed for facile access to 4-pyridyl sulfones. The reactions …

Recent progress of small molecule menin–MLL interaction inhibitors as therapeutic agents for acute leukemia

H Lei, SQ Zhang, S Fan, HR Bai, HY Zhao… - Journal of medicinal …, 2021 - ACS Publications
Mixed lineage leukemia (MLL) gene rearrangements are associated with acute leukemia.
The protein menin is regarded as a critical oncogenic cofactor of the resulting MLL fusion …

Menin-MLL protein-protein interaction inhibitors: a patent review (2014–2021)

H Bai, SQ Zhang, H Lei, F Wang, M Ma… - Expert Opinion on …, 2022 - Taylor & Francis
Introduction Chromosomal translocations involving the mixed-lineage leukemia (MLL,
KMT2A, MLL1) genes result in the production of MLL fusion proteins, which cause abnormal …

Histone H3K4 methyltransferases as targets for drug-resistant cancers

L Yang, M Jin, KW Jeong - Biology, 2021 - mdpi.com
Simple Summary Epigenetic modifications can regulate gene expression by altering
chromatin structure. Since the beginning of comprehensive research into changes in gene …

[HTML][HTML] Targeting epigenetic machinery: emerging novel allosteric inhibitors

F Ye, J Huang, H Wang, C Luo, K Zhao - Pharmacology & Therapeutics, 2019 - Elsevier
Epigenetics has emerged as an extremely exciting fast-growing area of biomedical research
in post genome era. Epigenetic dysfunction is tightly related with various diseases such as …

Discovery of M-1121 as an orally active covalent inhibitor of menin-MLL interaction capable of achieving complete and long-lasting tumor regression

M Zhang, A Aguilar, S Xu, L Huang… - Journal of medicinal …, 2021 - ACS Publications
Targeting the menin-MLL protein–protein interaction is being pursued as a new therapeutic
strategy for the treatment of acute leukemia carrying MLL-rearrangements (MLLr leukemia) …