Bromodomains: a new target class for drug development

AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …

[HTML][HTML] Histone acetyltransferases CBP/p300 in tumorigenesis and CBP/p300 inhibitors as promising novel anticancer agents

Q Chen, B Yang, X Liu, XD Zhang, L Zhang, T Liu - Theranostics, 2022 - ncbi.nlm.nih.gov
The histone acetyltransferases CBP and p300, often referred to as CBP/p300 due to their
sequence homology and functional overlap and co-operation, are emerging as critical …

Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

S Biswas, CM Rao - European journal of pharmacology, 2018 - Elsevier
Addition of chemical tags on the DNA and modification of histone proteins impart a distinct
feature on chromatin architecture. With the advancement in scientific research, the key …

The 2016 WHO classification of tumours of the urinary system and male genital organs—part B: prostate and bladder tumours

PA Humphrey, H Moch, AL Cubilla, TM Ulbright… - European urology, 2016 - Elsevier
It has been 12 yr since the publication of the last World Health Organization (WHO)
classification of tumours of the prostate and bladder. During this time, significant new …

[HTML][HTML] Protein lysine acetylation by p300/CBP

BM Dancy, PA Cole - Chemical reviews, 2015 - ACS Publications
Since their discovery in the 1980s and 1990s, the human protein lysine acetyltransferase
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …

Bromodomain inhibitors and cancer therapy: From structures to applications

M Pérez-Salvia, M Esteller - Epigenetics, 2017 - Taylor & Francis
Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes
that are “writers,”“erasers,” or “readers” of histone modification marks are common …

Acetylation targeting chimera enables acetylation of the tumor suppressor p53

M Kabir, N Sun, X Hu, TC Martin, J Yi… - Journal of the …, 2023 - ACS Publications
With advances in chemically induced proximity technologies, heterobifunctional modalities
such as proteolysis targeting chimeras (PROTACs) have been successfully advanced to …

The role of fatty acid β-oxidation in lymphangiogenesis

BW Wong, X Wang, A Zecchin, B Thienpont… - Nature, 2017 - nature.com
Lymphatic vessels are lined by lymphatic endothelial cells (LECs), and are critical for health.
However, the role of metabolism in lymphatic development has not yet been elucidated …

[HTML][HTML] Cation–π interactions in protein–ligand binding: theory and data-mining reveal different roles for lysine and arginine

K Kumar, SM Woo, T Siu, WA Cortopassi, F Duarte… - Chemical …, 2018 - pubs.rsc.org
We have studied the cation–π interactions of neutral aromatic ligands with the cationic
amino acid residues arginine, histidine and lysine using ab initio calculations, symmetry …

[HTML][HTML] BET bromodomain inhibition suppresses the function of hematopoietic transcription factors in acute myeloid leukemia

JS Roe, F Mercan, K Rivera, DJ Pappin, CR Vakoc - Molecular cell, 2015 - cell.com
The bromodomain and extraterminal (BET) protein BRD4 is a validated drug target in
leukemia, yet its regulatory function in this disease is not well understood. Here, we show …