CREB1 x CRTC2

Last update 08 May 2025

Basic Info

Related Targets

CREB1CRTC2

Drugs associated with CREB1 x CRTC2

A57

Target

CREB1 x CRTC2

Mechanism

CREB1 inhibitors [+1]

Active Org.

Fudan University

Originator Org.

Fudan University

Active Indication

Type 2 diabetes mellitus in obese

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with CREB1 x CRTC2

100 Translational Medicine associated with CREB1 x CRTC2

0 Patents (Medical) associated with CREB1 x CRTC2

167

Literatures (Medical) associated with CREB1 x CRTC2

11 Mar 2025·International journal of fertility & sterility

Dynamic Regulation of CYP19A1 Promoter Region under Control of CREB Family Members in Endometrial Tissues of Women with Endometriosis: A Case-Control Study.

Article

Author: Shahhoseini, Maryam ; Ramezanali, Fariba ; Kalantari, Shadi ; Amirchaghmaghi, Elham ; Saadat Varnosfaderani, Ameneh

BACKGROUNDEndometriosis is an estrogen-dependent disease. Cytochrome P450 aromatase which encoded by CYP19A1 is a key enzyme in the pathway of estrogen biosynthesis. cAMP response element (CRE) binding protein (CREB) and cAMP response element modulator (CREM), two members of the CREB family have important roles in the regulation of steroidogenic gene expression. CREB and CREM form homo and heterodimers for binding to the CRE sequence in the promoter of the CYP19A1 gene and regulate its expression. CREB regulated transcription coactivator 2 (CRTC2) is a CREB coactivator and regulates aromatase gene expression via binding to the CREB. Inducible cAMP early repressor (ICER) is one of CREM inhibitory isoforms that represses cAMP-induced transcription. Therefore, in this study, we decided to examine the expression levels of CREB, CREM, and CRTC2 genes and also the binding of ICER to the promoter II of the aromatase gene in endometriosis.MATERIALS AND METHODSIn this case-control study, ectopic and eutopic endometrial tissues of women with endometriosis and endometrial control samples were collected. Real-time polymerase chain reaction (PCR) technique was used for quantitative gene expression of CREB, CREM, and CRTC2. For protein-DNA interaction analysis, soluble chromatin was extracted, and chromatin immunoprecipitation (ChIP) coupled with real-time PCR was performed to quantify the binding of ICER to CYP19A1 promoter II.RESULTSGene expression levels of CREB, CREM, and CRTC2 were significantly increased in ectopic lesions compared with control endometrial samples. In addition, the binding of ICER to CYP19A1 promoter II was significantly decreased in ectopic and eutopic samples compared to the controls.CONCLUSIONThe overexpression of CREB, CREM, and CRTC2 in the endometriotic tissue samples and decreased binding of ICER to the CYP19A1 prompter II in ectopic and eutopic samples may contribute to the pathogenesis of endometriosis via their regulatory role in the expression of estrogen biosynthesis enzymes.

06 Mar 2025·Open Life Sciences

SIK1 inhibits IL-1β-stimulated cartilage apoptosis and inflammation in vitro through the CRTC2/CREB1 signaling

Article

Author: Chen, Mangmang ; Ye, Luyou ; Lin, Shenglei

AbstractOsteoarthritis (OA) is a chronic degenerative joint disease that affects 70–90% of individuals over the age of 75 and over 100 million people globally. Current treatments primarily offer symptomatic relief and do not effectively halt disease progression, highlighting the need for improved therapeutic strategies. Salt-inducible kinase 1 (SIK1) plays a role in regulating key physiological processes, including gluconeogenesis, glycolysis, and bone metabolism. Despite these insights, the specific role and underlying mechanisms of SIK1 in OA pathogenesis remain inadequately understood. This study aims to elucidate the function of SIK1 in OA cells. We observed that SIK1 was downregulated in a cell model of OA. The overexpression of SIK1 was found to inhibit IL-1β-induced chondrocyte apoptosis and inflammation. Additionally, SIK1 overexpression enhanced the activation of the CRTC2/CREB1 axis, suggesting a protective role for SIK1 in cartilage cells. In summary, SIK1 exerts a protective effect against IL-1β-induced cartilage apoptosis and inflammation in vitro through the CRTC2/CREB1 signaling axis.

01 Feb 2025·Virologica Sinica

CRTC3 restricts SARS-CoV-2 replication and is antagonized by CREB

Article

Author: Luo, Rong-Hua ; Long, Xin-Yan ; Cheng, Wei ; Fu, Xiang-Hui ; Zeng, Xiao-Tao ; Ren, Hai-Yan ; Tang, Ying ; Zheng, Yong-Tang ; Zhang, Wan-Jiang ; Ren, Si-Xue ; Yang, Li

Virus-encoding RNA-dependent RNA polymerase (RdRp) is essential for genome replication and gene transcription of human coronaviruses (HCoVs), including severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). We previously identified the interaction between the catalytic subunit NSP12 of SARS-CoV-2 RdRp and the host protein CREB-regulated transcription coactivator 3 (CRTC3), a member of the CRTC family that regulates cyclic AMP response element-binding protein (CREB)-mediated transcriptional activation. Currently, the implication of CRTC3 in the pathogenesis of HCoVs is poorly understood. Herein, we demonstrated that CRTC3 attenuates RdRp activity and SARS-CoV-2 genome replication, therefore reducing the production of progeny viruses. The interaction of CRTC3 with NSP12 contributes to its inhibitory effect on RdRp activity. Furthermore, we expanded the suppressive effects of two other CRTC family members (CRTC1 and CRTC2) on the RdRp activities of lethal HCoVs, including SARS-CoV-2 and Middle East respiratory syndrome coronavirus (MERS-CoV), along with the CREB antagonization. Overall, our research suggests that CRTCs restrict the replication of HCoVs and are antagonized by CREB, which not only provides new insights into the replication regulation of HCoVs, but also offers important information for the development of anti-HCoV interventions.

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