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Last update 23 Jan 2025

BCAT2

Last update 23 Jan 2025

Basic Info

Synonyms

BCAM, BCAT(m), BCAT2

+ [8]

Introduction

Catalyzes the first reaction in the catabolism of the essential branched chain amino acids leucine, isoleucine, and valine (PubMed:8702755, PubMed:25653144, PubMed:17050531). May also function as a transporter of branched chain alpha-keto acids (By similarity).

Drugs associated with BCAT2

BCAT2 Inhibitors(Agios)

Target

BCAT2

Mechanism

BCAT2 inhibitors

Active Org.

Agios Pharmaceuticals, Inc.

Originator Org.

Agios Pharmaceuticals, Inc.

Active Indication

Methylmalonic Acidemia [+1]

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

GENA-111

Target

BCAT2

Mechanism

BCAT2 inhibitors

Active Org.

Genome & Co.

Originator Org.

Debiopharm International SA [+1]

Active Indication

Neoplasms

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

BAY-069

Target

BCAT1 x BCAT2

Mechanism

BCAT1 inhibitors [+1]

Active Org.

Bayer AG

Originator Org.

Bayer AG

Active Indication

Neoplasms

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with BCAT2

100 Translational Medicine associated with BCAT2

0 Patents (Medical) associated with BCAT2

342

Literatures (Medical) associated with BCAT2

08 Jan 2025·Current Medicinal Chemistry

A Review on Branched-Chain Amino Acid Aminotransferase (BCAT) Inhibitors: Current Status, Challenges and Perspectives

Article

Author: Luo, Wen ; Li, Yan ; Khan, Maaz ; Pan, Jiamin ; Xie, Hua ; Zhao, Guilong ; Zhang, Xiansheng ; Pan, Hong ; Li, Yong ; Zhu, Xinyuan

Abstract:Branched-chain amino acids (BCAAs) are essential amino acids for humans and play an indispensable role in many physiological and pathological processes. Branched-chain amino acid aminotransferase (BCAT) is a key enzyme that catalyzes the metabolism of BCAAs. BCAT is upregulated in many cancers and implicated in the development and progress of some other diseases, such as metabolic and neurological diseases; and therefore, targeting BCAT might be a potential therapeutic approach for these diseases. There are two isoforms of BCAT, i.e., cytoplasmic BCAT1 (or BCATc) and mitochondrial BCAT2 (or BCATm). The discovery of BCAT inhibitors was initiated by Warner-Lambert, a subsidiary of Pfizer, in 2000, followed by many other pharmaceutical companies, such as GlaxoSmithKline (GSK), Ergon, Icagen, Agios, and Bayer. Strategies of high-throughput screening (HTS), DNA-Encoded library technology (ELT), and fragment-based screening (FBS) have been employed for hit identification, followed by structural optimization. Despite low selectivity, both BCAT1 and BCAT2 selective inhibitors were individually developed, each with a few chemical structural classes. The most advanced BCAT1 inhibitor is BAY-069, discovered by Bayer, which has a potent enzymatic inhibitory activity against BCAT1 and a decent in vitro and in vivo pharmacokinetic profile but displayed weaker cellular inhibitory activity and almost no anti-proliferative activity. There are no BCAT inhibitors currently under investigation in clinical trials. Further studies are still needed to discover BCAT inhibitors with a more druggable profile for proof of concept. This review focuses on the latest progress of studies on the understanding of the physiology and pathology of BCAT and the discovery and development of BCAT inhibitors. The structure-activity relationship (SAR) and the druggability, and the challenges of BCAT inhibitors are discussed, with the aim of inspiring the discovery and development of BCAT inhibitors in the future.

01 Dec 2024·Comparative Biochemistry and Physiology Part D: Genomics and Proteomics

Transcriptomic and histologic analyses preliminarily reveal the immune-metabolic response mechanism to saline-alkaline in large yellow croaker (Larimichthys crocea)

Article

Author: Zhou, Fengfang ; Sha, Zhenxia ; Huang, Weiqing ; Ruan, Shaojiang ; Cai, Binxin ; Chang, Mengyang ; Liu, Zheng

There are large areas of saline-alkaline waters worldwide, the utilization of which would greatly enhance the development of aquaculture productivity. To elucidate the regulatory mechanisms underlying the adaptation of large yellow croaker (Larimichthys crocea) to saline-alkaline water, this study analyzed the growth performance, tissue histology, and gills transcriptome profiles of L. crocea in both seawater (CK) and saline-alkaline water (EX) groups. Growth indices statistics revealed that L. crocea can adapt to saline-alkaline water, with growth performance comparable to that of the CK group. Histological examination revealed partial cellular detachment and structural relaxation in the gills tissue of the EX group, while liver and kidney tissues appeared normal. Transcriptome analysis revealed 3821 differentially expressed genes (DEGs), with 1541 DEGs up-regulated and 2280 DEGs down-regulated. GO enrichment analysis indicated that up-regulated DEGs were enriched in terms related to metabolite production during biological activities, while down-regulated DEGs were associated with terms related to maintaining cellular activities. KEGG enrichment analysis revealed that up-regulated DEGs were enriched in pathways related to the synthesis and metabolism of amino acids and lipids, such as the PPAR signaling pathway and glutathione metabolism. The down-regulated DEGs were predominantly enriched in immune-related signaling pathways, including the Toll-like receptor signaling pathway and NOD-like receptor signaling pathway. Further analysis revealed that genes such as lipoprotein lipase A (lpla), branched-chain amino acid aminotransferase 2 (bcat2), interleukin 8 (il8), interleukin 10 (il10), and interferon regulatory factor 7 (irf7) were involved in the adaptation of L. crocea to saline-alkaline water culture conditions. This study provides a basis for understanding the adaptability of large yellow croaker to saline-alkaline water and lays the foundation for the rational utilization of fishery water resources.

01 Dec 2024·Food Chemistry

Low storage temperature affects quality and volatile compounds in fresh tomatoes

Article

Author: Liu, Shiyu ; Watkins, Christopher B ; Zheng, Yanyan ; Han, Lichun ; Tao, Jiejie ; He, Xuelian ; Liu, Ye ; Zhao, Xiaoyan ; Zuo, Jinhua ; Li, Jian ; Bai, Chunmei

To investigate the impact of low temperature on the quality and flavor of ripe red tomatoes, we analyzed transcriptomes and volatile metabolomes of ripe red fruits stored at 0 °C and 20 °C for 8 days. The results showed that 0 °C maintained the sugar content by increasing the expression of sucrose synthetase (SUS) and sucrose transporter (SUT). Low expression of aroma synthesis-related genes, such as alcohol dehydrogenase 1 (ADH1), amino acid decarboxylase 1 A (AADC1A), and branched-chain amino acid aminotransferase 2 (BCAT2), were associated with reduced levels of pentanal, hexanal, 3-methylbutanal, 2-methylbutanal, and 2-phenylethanol. Additionally, the expression of pectinesterase (PE), beta-galactosidase (β-GAL), and beta-glucosidase (β-Glu), as well as phytoene synthase1 (PSY1) involved in carotenoid synthesis, was inhibited, thereby maintaining fruits texture and color. Furthermore, storage at 0 °C induced the expression of numerous genes regulating antioxidant and heat shock proteins, which further preserved the postharvest quality of tomatoes.

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BCAT2

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