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Overview

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Neoplasms

Gene therapy

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

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Targets

Most frequently developed targets

Disease Domain	Count

Neoplasms	1

Top 5 Drug Type	Count

Gene therapy	1

Top 5 Target	Count

RUNX3(Runt-related transcription factor 3)	1

BACKGROUNDMany histone deacetylase (HDAC) inhibitors are well recognized as potential anti-cancer drugs. Inhibition of HDACs induces temporal transcription or epigenetic control, thus regulating many different biological responses. Here, we investigated the osteogenic effect of the HDAC inhibitor suberoylanilide hydroxamic acid (SAHA; vorinostat).METHODSThe effects of SAHA on osteoblast differentiation were examined in the 6XOSE-Luc reporter assay for determination of runt-related transcription factor 2 (Runx2) activity and alkaline phosphatase (ALP) activity and in an immunoprecipitation assay to determine the Runx2 acetylation state. The osteogenic activity of SAHA in vivo was studied in and receptor activator of nuclear factor-kappa B ligand (RANKL)-induced osteoporotic mouse model.RESULTSSAHA increased the transcriptional activity of Runx2 in a dose-dependent manner in the 6XOSE-Luc reporter assay. SAHA by itself was unable to induce ALP activity; however, SAHA enhanced ALP activity induced by bone morphogenetic protein-2 (BMP-2). The degree of acetylation of Runx2 was increased with SAHA treatment, which suggests that the increase in Runx2 transcriptional activity might be dependent on stabilization by acetylation. Also, SAHA successfully reversed soluble RANKL-induced osteoporotic bone loss.CONCLUSIONSOur study shows an intriguing osteogenic potential of SAHA in a BMP-2-dependent manner and suggests that SAHA could be used at lower doses along with BMP-2 to treat osteoporosis.

American Journal of Translational Research

Histone deacetylase inhibitors: molecular mechanisms of action and clinical trials as anti-cancer drugs

Author: Bae, Suk-Chul ; Kim, Hyun-Jung

A review.Histone deacetylase (HDAC) inhibitors are a relatively new class of anti-cancer agents that play important roles in epigenetic or non-epigenetic regulation, inducing death, apoptosis, and cell cycle arrest in cancer cells.Recently, their use has been clin. validated in cancer patients resulting in the approval of two HDAC inhibitors, vorinostat and depsipetide, by the FDA.Also, clin. trials of several HDAC inhibitors for use as anti-cancer drugs (alone or in combination with other anti-cancer therapeutics) are ongoing.However, the mol. mechanisms underlying the response to HDAC inhibitors in cancer patients are not fully understood.In this review, we summarize our understanding of the mol. and biol. events that underpin the anti-cancer effects of HDAC inhibitors and the outcomes of recent clin. trials involving these drugs.

100 Deals associated with Biorunx Co., Ltd.

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100 Translational Medicine associated with Biorunx Co., Ltd.

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Pipeline

Pipeline Snapshot as of 23 Feb 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Phase 2 Clinical

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

Amina-X ( RUNX3 )	Neoplasms More	Phase 2
BRX-1002 ( RUNX3 )	Neoplasms More	Pending
BRX-100982 ( RUNX3 )	Neoplasms More	Pending
BRX-10030 ( RUNX3 )	Neoplasms More	Pending