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Advances in targeting 'undruggable'transcription factors with small molecules
Transcription factors (TFs) represent key biological players in diseases including cancer,
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …
Targeting arginine methyltransferase PRMT5 for cancer therapy: updated progress and novel strategies
J Zheng, B Li, Y Wu, X Wu, Y Wang - Journal of Medicinal …, 2023 - ACS Publications
As a predominant type II protein arginine methyltransferase, PRMT5 plays critical roles in
various normal cellular processes by catalyzing the mono-and symmetrical dimethylation of …
various normal cellular processes by catalyzing the mono-and symmetrical dimethylation of …
[HTML][HTML] Small molecules targeting protein–protein interactions for cancer therapy
Protein–protein interactions (PPIs) are fundamental to many biological processes that play
an important role in the occurrence and development of a variety of diseases. Targeting the …
an important role in the occurrence and development of a variety of diseases. Targeting the …
Structure, function and inhibition of critical protein–protein interactions involving mixed lineage leukemia 1 and its fusion oncoproteins
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 …
transcription factor and histone-H3 lysine-4 (H3K4) methyltransferase. It is a master …
Approaching the catalytic mechanism of protein lysine methyltransferases by biochemical and simulation techniques
Protein lysine methyltransferases (PKMTs) transfer up to three methyl groups to the side
chains of lysine residues in proteins and fulfill important regulatory functions by controlling …
chains of lysine residues in proteins and fulfill important regulatory functions by controlling …
Small Molecule Menin Inhibitors: Novel Therapeutic Agents Targeting Acute Myeloid Leukemia with KMT2A Rearrangement or NPM1 Mutation
X Thomas - Oncology and Therapy, 2024 - Springer
Recent advances have included insights into the clinical value of genomic abnormalities in
acute myeloid leukemia (AML) and consequently the development of numerous targeted …
acute myeloid leukemia (AML) and consequently the development of numerous targeted …
Discovery of a new-generation S-Adenosylmethionine-noncompetitive covalent inhibitor targeting the lysine methyltransferase enhancer of zeste homologue 2
Y Zhang, H Yang, B Li, J Li, H Li, Q Shi… - Journal of Medicinal …, 2023 - ACS Publications
The first-generation enhancer of zeste homologue 2 (EZH2) inhibitors suffer from several
limitations, such as high dosage, cofactor S-adenosylmethionine (SAM) competition, and …
limitations, such as high dosage, cofactor S-adenosylmethionine (SAM) competition, and …
Menin–MLL1 interaction small molecule inhibitors: A potential therapeutic strategy for leukemia and cancers
Q Shi, M Xu, Z Kang, M Zhang, Y Luo - Molecules, 2023 - mdpi.com
Encoded by the MEN1 gene, menin protein is a fusion protein that is essential for the
oncogenic transformation of mixed-lineage leukemia (MLL) and leads to acute leukemia …
oncogenic transformation of mixed-lineage leukemia (MLL) and leads to acute leukemia …
Chemical biology and pharmacology of histone lysine methylation inhibitors
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 …
epigenetic regulation of a broad spectrum of biological processes. Moreover, the …
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 …
KMT2A, MLL1) genes result in the production of MLL fusion proteins, which cause abnormal …