5fe1 Citations

Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.

Abstract

The P300/CBP-associated factor plays a central role in retroviral infection and cancer development, and the C-terminal bromodomain provides an opportunity for selective targeting. Here, we report several new classes of acetyl-lysine mimetic ligands ranging from mM to low micromolar affinity that were identified using fragment screening approaches. The binding modes of the most attractive fragments were determined using high resolution crystal structures providing chemical starting points and structural models for the development of potent and selective PCAF inhibitors.

Reviews - 5fe1 mentioned but not cited (1)

  1. Progress and prospects of reversible solid oxide fuel cell materials. Shen M, Ai F, Ma H, Xu H, Zhang Y. iScience 24 103464 (2021)

Articles - 5fe1 mentioned but not cited (2)



Reviews citing this publication (3)

  1. Bromodomain inhibitors and cancer therapy: From structures to applications. Pérez-Salvia M, Esteller M. Epigenetics 12 323-339 (2017)
  2. Chemical probes and inhibitors of bromodomains outside the BET family. Moustakim M, Clark PGK, Hay DA, Dixon DJ, Brennan PE. Medchemcomm 7 2246-2264 (2016)
  3. Target-based drug discovery: Applications of fluorescence techniques in high throughput and fragment-based screening. Kumar V, Chunchagatta Lakshman PK, Prasad TK, Manjunath K, Bairy S, Vasu AS, Ganavi B, Jasti S, Kamariah N. Heliyon 10 e23864 (2024)

Articles citing this publication (7)