Advances in targeting 'undruggable'transcription factors with small molecules
MJ Henley, AN Koehler - Nature Reviews Drug Discovery, 2021 - nature.com
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 transcription factors in cancer—from undruggable to reality
JH Bushweller - Nature Reviews Cancer, 2019 - nature.com
Mutated or dysregulated transcription factors represent a unique class of drug targets that
mediate aberrant gene expression, including blockade of differentiation and cell death gene …
mediate aberrant gene expression, including blockade of differentiation and cell death gene …
Multiple endocrine neoplasia type 1: latest insights
ML Brandi, SK Agarwal, ND Perrier, KE Lines… - Endocrine …, 2021 - academic.oup.com
Multiple endocrine neoplasia type 1 (MEN1), a rare tumor syndrome that is inherited in an
autosomal dominant pattern, is continuing to raise great interest for endocrinology …
autosomal dominant pattern, is continuing to raise great interest for endocrinology …
Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease
Protein lysine methylation is a crucial post-translational modification that regulates the
functions of both histone and non-histone proteins. Deregulation of the enzymes or 'writers' …
functions of both histone and non-histone proteins. Deregulation of the enzymes or 'writers' …
Menin inhibitor MI-3454 induces remission in MLL1-rearranged and NPM1-mutated models of leukemia
S Klossowski, H Miao, K Kempinska… - The Journal of …, 2020 - Am Soc Clin Investig
The protein-protein interaction between menin and mixed lineage leukemia 1 (MLL1) plays
a critical role in acute leukemias with translocations of the MLL1 gene or with mutations in …
a critical role in acute leukemias with translocations of the MLL1 gene or with mutations in …
Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c)
Abstract Treatment with Menin inhibitor (MI) disrupts the interaction between Menin and
MLL1 or MLL1-fusion protein (FP), inhibits HOXA9/MEIS1, induces differentiation and loss of …
MLL1 or MLL1-fusion protein (FP), inhibits HOXA9/MEIS1, induces differentiation and loss of …
Synergistic targeting of FLT3 mutations in AML via combined menin-MLL and FLT3 inhibition
MM Dzama, M Steiner, J Rausch… - Blood, The Journal …, 2020 - ashpublications.org
The interaction of menin (MEN1) and MLL (MLL1, KMT2A) is a dependency and provides a
potential opportunity for treatment of NPM1-mutant (NPM1 mut) and MLL-rearranged (MLL-r) …
potential opportunity for treatment of NPM1-mutant (NPM1 mut) and MLL-rearranged (MLL-r) …
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 …
Genome-scale CRISPR-Cas9 screen of Wnt/β-catenin signaling identifies therapeutic targets for colorectal cancer
Aberrant activation of Wnt/β-catenin pathway is a key driver of colorectal cancer (CRC)
growth and of great therapeutic importance. In this study, we performed comprehensive …
growth and of great therapeutic importance. In this study, we performed comprehensive …
Rewiring the Epigenetic Networks in MLL-Rearranged Leukemias: Epigenetic Dysregulation and Pharmacological Interventions
Leukemias driven by chromosomal translocation of the mixed-lineage leukemia gene (MLL
or KMT2A) are highly prevalent in pediatric oncology. The poor survival rate and lack of an …
or KMT2A) are highly prevalent in pediatric oncology. The poor survival rate and lack of an …