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Last update 08 May 2025

BRPF2

Last update 08 May 2025

Basic Info

Synonyms

BR140-like, BR140-like protein, BRD1

+ [6]

Introduction

Scaffold subunit of various histone acetyltransferase (HAT) complexes, such as the MOZ/MORF and HBO1 complexes, that acts as a regulator of hematopoiesis (PubMed:16387653, PubMed:21753189, PubMed:21880731). Plays a key role in HBO1 complex by directing KAT7/HBO1 specificity towards histone H3 'Lys-14' acetylation (H3K14ac), thereby promoting erythroid differentiation (PubMed:21753189).

Drugs associated with BRPF2

CG-202

Target

BRPF2

Mechanism

BRPF2 inhibitors

Active Org.

Convergene LLC

Originator Org.

Convergene LLC

Active Indication

Hematologic Neoplasms

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

BAY-299

Target

BRPF2 x TAF1

Mechanism

BRPF2 inhibitors [+1]

Active Org.

Third Military Medical University

Originator Org.

Bayer AG

Active Indication

Acute Myeloid Leukemia

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

DW-1017

Target

BRPF2

Mechanism

BRPF2 inhibitors

Active Org.-

Originator Org.

DONG WHA PHARM Co., Ltd.

Active Indication-

Inactive Indication

Acute Myeloid Leukemia

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with BRPF2

100 Translational Medicine associated with BRPF2

0 Patents (Medical) associated with BRPF2

152

Literatures (Medical) associated with BRPF2

01 May 2025·Behavioural Brain Research

Targeted suppression of BRD7 with BI-9564 prevents seizure behaviors in pentylenetetrazol and pilocarpine-induced mouse model of epilepsy

Article

Author: Li, Yujia ; Zhou, Cuilan ; Li, Suyun ; Huo, Xiaofei ; Xu, Yang ; Cao, Wenyu ; Huang, Ziqiang ; Chen, Jie

Epilepsy is a serious neurological disorder, but its underlying cellular and molecular mechanisms remains incomplete. As a member of the bromodomain-containing protein (BCP) family, BRD7 has been implicated in a variety of cellular processes, including chromatin remodeling, transcriptional regulation, and cell cycle progression. However, the role of BRD7 in epilepsy in vivo is still poorly understood. In the present study, we found that pentylenetetrazole (PTZ)-induced epilepsy increased hippocampal BRD7, which was mainly localized in neurons. In addition, the enhanced expression of hippocampal BRD7 was normalized by using the anti-epilepsy drug valproic acid (VPA). Furthermore, we identified that the BRD7 inhibitor BI-9564 could dose dependently alleviated the seizure behavior in PTZ treated mice, which was also validated in pilocarpine mouse model. Mechanistically, the anti-seizure effect of BI- 9564 might be due to its negative-regulation of hippocampal TRPV4 that downregulated neuronal over-excitability. Importantly, BRD7 blockade retained its antiepileptic activity over chronic dosing that was not related to psychomotor or cognitive effects. To our knowledge, these results are the first evidence to demonstrate that BRD7 inhibitor can down-regulate neuronal over-excitation caused by epilepsy possible by regulating TRPV4. Targeting BRD7 through the development of selective inhibitors may lead to disease-modifying therapies that reduce seizure behavior.

13 Mar 2025·Journal of Medicinal Chemistry

Multi-Water Bridges Enable Design of BET BD1-Selective Inhibitors for Pancreatic Cancer Therapy

Article

Author: Jiang, Zhengyu ; Kang, Wenjing ; Wu, Tingting ; You, Qidong ; Cao, Danyan ; Du, Zhiyan ; Xiong, Bing ; Meng, Fanying ; Chen, Xuetao ; Chen, Yali ; Wang, Xinyue ; Guo, Xiaoke ; Yan, Leixin

Rational design of bromodomain (BD)-selective inhibitors could mitigate on-target toxicities associated with pan-BET inhibition but is challenging despite the availability of high-resolution structures. By simultaneously forming water bridges with BD1-specific residues in both the BC ring and the ZA channel, we identified a potent and orally bioavailable BET BD1-selective inhibitor DDO-8958, which exhibited a K_D of 5.6 nM for BRD4 BD1 and a 214-fold selectivity for BRD4 BD1 over BD2. The cocrystal structure demonstrated a unique multi-water bridge mechanism involving BD1-specific residues K91- and D145-driven BD1 selectivity. DDO-8958 extensively influenced the oncogene expression and metabolic pathway, including oxidative phosphorylation in MIA PaCa-2. In vivo, DDO-8958 inhibited tumor growth and markedly augmented the therapeutic efficacy of the glycolysis inhibitor 2-DG. These findings illuminate that multi-water bridges enable design of BD1-selective inhibitors and a therapeutic strategy involving combined targeting of BD1-induced epigenetic reprogramming and glycolysis pathways for the management of pancreatic cancer.

01 Dec 2024·Cancer Medicine

5‐Hydroxymethylcytosine Profiles of cfDNA in Urine as Diagnostic, Differential Diagnosis and Prognostic Markers for Multiple Myeloma

Article

Author: Dong, Yujun ; Tang, Bo ; Chu, Jinlin ; Li, Xuehui ; Xie, Weiwei ; Lin, Jian ; Zhang, Lei ; Huang, Wenrong ; Li, Linlin ; Chen, Hangyu

ABSTRACTBackgroundAn effective urine‐based method for the diagnosis, differential diagnosis and prognosis of multiple myeloma (MM) has not yet been developed. Urine cell‐free DNA (cfDNA) carrying cancer‐specific genetic and epigenetic aberrations may enable a noninvasive “liquid biopsy” for diagnosis and monitoring of cancer.MethodsWe first identified MM‐specific hydroxymethylcytosine signatures by comparing 64 MM patients, 23 amyloidosis (AM) patients and 59 healthy cohort. Then, we applied a machine learning algorithm to develop diagnostic and differential diagnosis model. Finally, the prognosis of MM patients was predicted based on their survival time at the last follow‐up.ResultsWe identified 11 5hmC markers using logistic regression algorithm could effectively diagnosis MM (AUC = 0.902), and achieved 85.00% specificity and 85.71% sensitivity. These 11 markers could also effectively differential diagnosis MM (AUC = 0.805) with 88.89% specificity and 73.08% sensitivity. In addition, the prognostic prediction model also effectively predicted the prognosis of patients with MM (p < 0.01), of which 4 differential markers (RAPGEF2, BRD1, TET2, TRAF3IP2) could independently predict the prognosis of MM.ConclusionsTogether, our findings showed the value of urine cfDNA hydroxymethylcytosine markers in the diagnosis, differential diagnosis and prognosis of MM. Meantime, our study provides a promising and completely non‐invasive method for the diagnosis, differential diagnosis and prognosis prediction of MM.

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BRPF2

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