Target intelligence / Profile preview

SERTA domain-containing protein 2 (SERTAD2)

Target
SERTAD2
Molecular classification
Transcriptional co-regulator, Transcription factor (coactivator/corepressor), Other (TRIP-Br/SERTAD family)
01

Overview

SERTA domain-containing protein 2 (SERTAD2) is a transcriptional co-regulator that acts at E2F-responsive promoters, integrating signals from PHD- and bromodomain-containing transcription factors. It can function either as a coactivator or corepressor of critical transcription complexes, modulating gene expression associated with cell cycle progression and fat metabolism. SERTAD2 plays a pivotal role in energy homeostasis, with knockout studies in mice showing resistance to obesity and insulin resistance, suggesting enhanced lipid turnover and energy expenditure. Its expression is tightly regulated through the cell cycle, peaking at the G1/S boundary, and is subject to CRM1-mediated nuclear export and proteasomal degradation. SERTAD2 is frequently overexpressed in multiple human tumors, including lung cancer (where it is upregulated downstream of REV1/Rad18 in the DNA damage response), emphasizing its relevance in oncogenesis as well as metabolic disorders. Currently, there are no approved drugs directly targeting SERTAD2, but its biological significance in cancer and metabolism positions it as a candidate therapeutic target for future research[1][2][3][4].

Other names
TRIP-Br2TRIPBR2Sei-2KIAA0127SERTA domain containing 2SERTA domain-containing protein 2Transcriptional regulator interacting with the PHD-bromodomain 2SEI-2SRTD2_HUMAN
02

Mechanism of action

Not directly applicable; may become relevant if drugs are developed that inhibit its co-regulatory function for E2F-responsive transcription or modulate its effect on fat metabolism and cell proliferation

03

Biological functions

Cell cycle progressionTranscriptional regulation (E2F-responsive promoters)Regulation of fat storageNegative regulation of cell growthRegulation of adipocyte lipolysis, thermogenesis, and oxidative metabolism
04

Disease associations

Cancer (tumorigenesis; overexpressed in multiple human tumors, including lung cancer)Metabolic disorders (obesity, insulin resistance)Other (potential roles in energy homeostasis and DNA damage tolerance)
05

Safety considerations

None specifically documented, as this is not an established therapeutic target with clinical drugs; however, theoretical concerns involve disruption of cell-cycle regulation, risk of metabolic dysregulation, and off-target effects if targeted
06

Interacting drugs

None identified in available sources; no approved therapeutic agents or drugs directly target SERTAD2 as of current literature
07

Biomarkers

SERTAD2 expression in visceral fat (potential biomarker for obesity/metabolic risk)SERTAD2 overexpression in tumors (potential biomarker for certain cancers, especially lung cancer)

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