Review




Structured Review

Santa Cruz Biotechnology brd2
D072 exerts anti-inflammatory effects by specifically degrading BRD3 (A) The expressions of <t>BRD2,</t> BRD3, and BRD4 in control group, EAU group, and D072 treatment group of the retina. (B) The in vitro expression of BRD2, BRD3, and BRD4 under the intervention of the ubiquitin pathway. (C) Molecular docking of BRD3 and BRD4. (D) After knockdown of BRD3 in BV2 cells, the protein expression levels of INOS, COX2, and Galectin-3 receptor in response to LPS stimulation were measured. (A) Upper: representative western blot images of retinal BRD2, BRD3, and BRD4 in Control group, EAU+Vehicle group, and EAU+D072 group, respectively. Lower: quantification of the relative fold changes of the left ( n = 3/group; mean ± SD; ∗p < 0.05, ∗∗p < 0.01, ∗∗∗p < 0.001; one-way ANOVA). (B) Left: representative western blot images of BRD2, BRD3, and BRD4 in each group in BV2. Right: quantification of the relative changes of the left ( n = 3/group; mean ± SD; ∗∗∗p < 0.001; one-way ANOVA). (C) The binding modes of BRD3 and BRD4 with D072. (D) Western blotting analysis of the protein levels of iNOS, COX-2, Galectin-3, and BRD3 in different groups. Left: representative western blot images of iNOS, COX-2, Galectin-3, and BRD3 in different groups. Right: quantification of the relative fold changes of the left ( n = 3/group; mean ± SD; ∗p < 0.05, ∗∗p < 0.01, ∗∗∗p < 0.001; one-way ANOVA).
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Images

1) Product Images from "BRD3 PROTAC degrader targets H3K18ac to alleviate retinal microglia-driven uveitis"

Article Title: BRD3 PROTAC degrader targets H3K18ac to alleviate retinal microglia-driven uveitis

Journal: iScience

doi: 10.1016/j.isci.2025.114526

D072 exerts anti-inflammatory effects by specifically degrading BRD3 (A) The expressions of BRD2, BRD3, and BRD4 in control group, EAU group, and D072 treatment group of the retina. (B) The in vitro expression of BRD2, BRD3, and BRD4 under the intervention of the ubiquitin pathway. (C) Molecular docking of BRD3 and BRD4. (D) After knockdown of BRD3 in BV2 cells, the protein expression levels of INOS, COX2, and Galectin-3 receptor in response to LPS stimulation were measured. (A) Upper: representative western blot images of retinal BRD2, BRD3, and BRD4 in Control group, EAU+Vehicle group, and EAU+D072 group, respectively. Lower: quantification of the relative fold changes of the left ( n = 3/group; mean ± SD; ∗p < 0.05, ∗∗p < 0.01, ∗∗∗p < 0.001; one-way ANOVA). (B) Left: representative western blot images of BRD2, BRD3, and BRD4 in each group in BV2. Right: quantification of the relative changes of the left ( n = 3/group; mean ± SD; ∗∗∗p < 0.001; one-way ANOVA). (C) The binding modes of BRD3 and BRD4 with D072. (D) Western blotting analysis of the protein levels of iNOS, COX-2, Galectin-3, and BRD3 in different groups. Left: representative western blot images of iNOS, COX-2, Galectin-3, and BRD3 in different groups. Right: quantification of the relative fold changes of the left ( n = 3/group; mean ± SD; ∗p < 0.05, ∗∗p < 0.01, ∗∗∗p < 0.001; one-way ANOVA).
Figure Legend Snippet: D072 exerts anti-inflammatory effects by specifically degrading BRD3 (A) The expressions of BRD2, BRD3, and BRD4 in control group, EAU group, and D072 treatment group of the retina. (B) The in vitro expression of BRD2, BRD3, and BRD4 under the intervention of the ubiquitin pathway. (C) Molecular docking of BRD3 and BRD4. (D) After knockdown of BRD3 in BV2 cells, the protein expression levels of INOS, COX2, and Galectin-3 receptor in response to LPS stimulation were measured. (A) Upper: representative western blot images of retinal BRD2, BRD3, and BRD4 in Control group, EAU+Vehicle group, and EAU+D072 group, respectively. Lower: quantification of the relative fold changes of the left ( n = 3/group; mean ± SD; ∗p < 0.05, ∗∗p < 0.01, ∗∗∗p < 0.001; one-way ANOVA). (B) Left: representative western blot images of BRD2, BRD3, and BRD4 in each group in BV2. Right: quantification of the relative changes of the left ( n = 3/group; mean ± SD; ∗∗∗p < 0.001; one-way ANOVA). (C) The binding modes of BRD3 and BRD4 with D072. (D) Western blotting analysis of the protein levels of iNOS, COX-2, Galectin-3, and BRD3 in different groups. Left: representative western blot images of iNOS, COX-2, Galectin-3, and BRD3 in different groups. Right: quantification of the relative fold changes of the left ( n = 3/group; mean ± SD; ∗p < 0.05, ∗∗p < 0.01, ∗∗∗p < 0.001; one-way ANOVA).

Techniques Used: Control, In Vitro, Expressing, Ubiquitin Proteomics, Knockdown, Western Blot, Binding Assay

Related Articles

other:

Article Title: BRD3 PROTAC degrader targets H3K18ac to alleviate retinal microglia-driven uveitis
Article Snippet: BRD2 , Santa Cruz , sc-514103; RRID:AB_3720459.

Western Blot:

Article Title: Resistance of estrogen receptor function to BET bromodomain inhibition is mediated by transcriptional coactivator cooperativity.
Article Snippet: The bromodomain and extraterminal domain (BET) family of proteins are critical chromatin readers that bind to acetylated histones through their bromodomains to activate transcription.. Here, we reveal that bromodomain inhibition fails to repress oncogenic targets of estrogen receptor because of an intrinsic transcriptional mechanism.. While bromodomains are necessary for the transcription of many genes, bromodomain-containing protein 4 (BRD4) binds to estrogen receptor binding sites and activates transcription of critical oncogenes such as MYC, independently of its bromodomains.

Chromatin Immunoprecipitation:

Article Title: Resistance of estrogen receptor function to BET bromodomain inhibition is mediated by transcriptional coactivator cooperativity.
Article Snippet: The bromodomain and extraterminal domain (BET) family of proteins are critical chromatin readers that bind to acetylated histones through their bromodomains to activate transcription.. Here, we reveal that bromodomain inhibition fails to repress oncogenic targets of estrogen receptor because of an intrinsic transcriptional mechanism.. While bromodomains are necessary for the transcription of many genes, bromodomain-containing protein 4 (BRD4) binds to estrogen receptor binding sites and activates transcription of critical oncogenes such as MYC, independently of its bromodomains.

Blocking Assay:

Article Title: Inhibition of Brd4 alleviates osteoarthritis pain via suppression of neuroinflammation and activation of Nrf2-mediated antioxidant signalling.
Article Snippet: Funding information National Natural Science Foundation of China, Grant/Award Numbers: 82001198, 82071556, 82101310, 82271291; National Key Research and Development Program of China, Grant/Award Number: 2020YFC2005303 Abstract Background and Purpose: Osteoarthritis (OA) pain remains a major clinical problem.. It is urgent to identify novel therapeutic approaches for OA pain states.. Bromodomain and extra-terminal (BET) protein inhibitors have robust anti-inflammatory effects in several pain models.

Incubation:

Article Title: Inhibition of Brd4 alleviates osteoarthritis pain via suppression of neuroinflammation and activation of Nrf2-mediated antioxidant signalling.
Article Snippet: Funding information National Natural Science Foundation of China, Grant/Award Numbers: 82001198, 82071556, 82101310, 82271291; National Key Research and Development Program of China, Grant/Award Number: 2020YFC2005303 Abstract Background and Purpose: Osteoarthritis (OA) pain remains a major clinical problem.. It is urgent to identify novel therapeutic approaches for OA pain states.. Bromodomain and extra-terminal (BET) protein inhibitors have robust anti-inflammatory effects in several pain models.

Article Title: Differential responses of pulmonary vascular cells from PAH patients and controls to TNFα and the effect of the BET inhibitor JQ1.
Article Snippet: .. After washing in PBS, sections were incubated for 1 h with mouse anti-human BRD2 (sc-393720; Santa Cruz Biotechnology) at a 1∶2900 dilution (0.069 μg/ml) or with rabbit anti-human BRD4 (ab128874; Abcam) at a 1∶300 dilution (1.577 μg/ml). .. For negative control slides, normal mouse or normal rabbit non-specific immunoglobulins (Santa Cruz Biotechnology) were used at the same protein concentration as the primary antibodies.



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Image Search Results


Serum levels of reproductive hormones in mice. ( A ) Serum AMH concentration; ( B ) serum E2 concentration; ( C ) serum FSH concentration, n = 10. * p < 0.05, ** p < 0.01, *** p < 0.001; ns, no significant difference.

Journal: International Journal of Molecular Sciences

Article Title: Establishment of an Autoimmune Premature Ovarian Insufficiency Mouse Model with Proteomic Analyses: An Exploratory Study

doi: 10.3390/ijms27104270

Figure Lengend Snippet: Serum levels of reproductive hormones in mice. ( A ) Serum AMH concentration; ( B ) serum E2 concentration; ( C ) serum FSH concentration, n = 10. * p < 0.05, ** p < 0.01, *** p < 0.001; ns, no significant difference.

Article Snippet: The ELISA kits used were as follows: FSH (RK04237, ABclonal, Shanghai, China), AMH (RK09261, ABclonal, China), and E2 (RK00651, ABclonal, China).

Techniques: Concentration Assay