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MITACS Inc
proteolysis protein chimeras (protacs) targeting nsd2 degradation  Proteolysis Protein Chimeras (Protacs) Targeting Nsd2 Degradation, supplied by MITACS Inc, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more https://www.bioz.com/result/proteolysis protein chimeras (protacs) targeting nsd2 degradation/product/MITACS Inc Average 90 stars, based on 1 article reviews
proteolysis protein chimeras (protacs) targeting nsd2 degradation - by Bioz Stars,
2026-02
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Shanghai GenePharma
sirnas targeting nsrp1 or nsd2  Sirnas Targeting Nsrp1 Or Nsd2, supplied by Shanghai GenePharma, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more https://www.bioz.com/result/sirnas targeting nsrp1 or nsd2/product/Shanghai GenePharma Average 90 stars, based on 1 article reviews
sirnas targeting nsrp1 or nsd2 - by Bioz Stars,
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Image Search Results
Journal: Journal of medicinal chemistry
Article Title: Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)
doi: 10.1021/acs.jmedchem.3c00948
Figure Lengend Snippet: Chemical structures of representative NSD2 inhibitors and degraders 10–16.
Article Snippet: Both NSD2 and its target gene HDAC2 were revealed to activate the NF-κB signaling pathway inducing the occurrence and progression of inflammation by promoting the release of proinflammatory cytokines.204 Meanwhile, NSD2 can modulate the envelope protein (protein E) of SARS-CoV2 via interactions with BRD4, suggesting that NSD2 may play an important role in the progression of SARS-CoV2.204 Proteolysis protein chimeras (PROTACs) targeting
Techniques:
Journal: Journal of medicinal chemistry
Article Title: Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)
doi: 10.1021/acs.jmedchem.3c00948
Figure Lengend Snippet: The biological functions of NSD2 and underlying mechanisms.
Article Snippet: Both NSD2 and its target gene HDAC2 were revealed to activate the NF-κB signaling pathway inducing the occurrence and progression of inflammation by promoting the release of proinflammatory cytokines.204 Meanwhile, NSD2 can modulate the envelope protein (protein E) of SARS-CoV2 via interactions with BRD4, suggesting that NSD2 may play an important role in the progression of SARS-CoV2.204 Proteolysis protein chimeras (PROTACs) targeting
Techniques:
Journal: Journal of medicinal chemistry
Article Title: Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)
doi: 10.1021/acs.jmedchem.3c00948
Figure Lengend Snippet: Overview of various cancers associated with NSD lysine methyltransferases (KMTases) dysregulation.
Article Snippet: Both NSD2 and its target gene HDAC2 were revealed to activate the NF-κB signaling pathway inducing the occurrence and progression of inflammation by promoting the release of proinflammatory cytokines.204 Meanwhile, NSD2 can modulate the envelope protein (protein E) of SARS-CoV2 via interactions with BRD4, suggesting that NSD2 may play an important role in the progression of SARS-CoV2.204 Proteolysis protein chimeras (PROTACs) targeting
Techniques: Migration, Mutagenesis, Activity Assay, Transformation Assay, Expressing, DNA Synthesis
Journal: Journal of medicinal chemistry
Article Title: Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)
doi: 10.1021/acs.jmedchem.3c00948
Figure Lengend Snippet: Crystal structure of compound 50 (MR837) in complex with NSD2-PWWP1 domain (PDB ID: 6UE6). Hydrogen bonds formed between 50 and the key residues in the NSD2-PWWP1 domain are highlighted by red dashed lines. Compound 50 is shown as yellow sticks. Key residues ALA-270, TYR-233, TRP-236, PHE-266, and VAL-230 in the NSD2-PWWP1 domain are shown as green sticks.
Article Snippet: Both NSD2 and its target gene HDAC2 were revealed to activate the NF-κB signaling pathway inducing the occurrence and progression of inflammation by promoting the release of proinflammatory cytokines.204 Meanwhile, NSD2 can modulate the envelope protein (protein E) of SARS-CoV2 via interactions with BRD4, suggesting that NSD2 may play an important role in the progression of SARS-CoV2.204 Proteolysis protein chimeras (PROTACs) targeting
Techniques:
Journal: Journal of medicinal chemistry
Article Title: Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)
doi: 10.1021/acs.jmedchem.3c00948
Figure Lengend Snippet: (a) SAM crystal structure in complex with NSD2-SET domain (PDB ID: 5LSU). SAM is shown as cyan sticks; (b) Crystal structure of DNA in complex with NSD2-PWWP1 domain (PDB ID: 5VC8). The key residues LYS-304, LYS-309, and LYS-312 in NSD2-PWWP1 domain that form direct electrostatic interactions with the DNA phosphate backbone are shown as cyan sticks; and (c) The structures of three NSD2 isoforms (NSD2-long, NSD2-short, and RE-IIBP) that are composed of multiple domains, including PWWP domain, PHD domain, SET domain (AWS/pre-SET, SET, and post-SET), etc.
Article Snippet: Both NSD2 and its target gene HDAC2 were revealed to activate the NF-κB signaling pathway inducing the occurrence and progression of inflammation by promoting the release of proinflammatory cytokines.204 Meanwhile, NSD2 can modulate the envelope protein (protein E) of SARS-CoV2 via interactions with BRD4, suggesting that NSD2 may play an important role in the progression of SARS-CoV2.204 Proteolysis protein chimeras (PROTACs) targeting
Techniques:
Journal: Journal of medicinal chemistry
Article Title: Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)
doi: 10.1021/acs.jmedchem.3c00948
Figure Lengend Snippet: (a) Crystal structure of compound 51 (MRT866) in complex with NSD2-PWWP1 domain (PDB ID: 7MDN). Red dash lines highlight the hydrogen bonds between compound 51 and the key residues in NSD2-PWWP1 domain. Compound 51 is shown as yellow sticks. Key residues ALA-270, GLN-321, TYR-233, TRP-236, and PHE-266 in the NSD2-PWWP1 domain are shown as green sticks. (b) Crystal structure of compound 14 (UNC6934) in complex with NSD2-PWWP1 domain (PDB ID: 6XCG). Red dash lines highlight the hydrogen bonds formed between compound 14 and the key residues in NSD2-PWWP1 domain. Compound 14 is shown as yellow sticks. Key residues ALA-270, GLN-321, TYR-233, ARG-273, TRP-236, and PHE-266 in the NSD2-PWWP1 domain are shown as green sticks.
Article Snippet: Both NSD2 and its target gene HDAC2 were revealed to activate the NF-κB signaling pathway inducing the occurrence and progression of inflammation by promoting the release of proinflammatory cytokines.204 Meanwhile, NSD2 can modulate the envelope protein (protein E) of SARS-CoV2 via interactions with BRD4, suggesting that NSD2 may play an important role in the progression of SARS-CoV2.204 Proteolysis protein chimeras (PROTACs) targeting
Techniques:
Journal: Journal of medicinal chemistry
Article Title: Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)
doi: 10.1021/acs.jmedchem.3c00948
Figure Lengend Snippet: Crystal structure of compound 54 in complex with NSD2-PWWP1 domain (PDB ID: 7VLN). Hydrogen bonds formed between compound 54 and the key residues in the NSD2-PWWP1 domain are highlighted by red dashed lines. Compound 54 is shown as yellow sticks. Key residues ALA-270, ASP-269, TYR-233, GLU-291, and GLU-272 in the NSD2-PWWP1 domain are shown as green sticks.
Article Snippet: Both NSD2 and its target gene HDAC2 were revealed to activate the NF-κB signaling pathway inducing the occurrence and progression of inflammation by promoting the release of proinflammatory cytokines.204 Meanwhile, NSD2 can modulate the envelope protein (protein E) of SARS-CoV2 via interactions with BRD4, suggesting that NSD2 may play an important role in the progression of SARS-CoV2.204 Proteolysis protein chimeras (PROTACs) targeting
Techniques:
Journal: Journal of medicinal chemistry
Article Title: Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)
doi: 10.1021/acs.jmedchem.3c00948
Figure Lengend Snippet: Crystal structure of compound 14 (UNC6934) in complex with NSD2-PWWP1 domain (PDB ID: 6XCG). Compound 14 is shown as green sticks, and the red dashed circle highlights the pyrimidine ring that points into the solvent-exposed region.
Article Snippet: Both NSD2 and its target gene HDAC2 were revealed to activate the NF-κB signaling pathway inducing the occurrence and progression of inflammation by promoting the release of proinflammatory cytokines.204 Meanwhile, NSD2 can modulate the envelope protein (protein E) of SARS-CoV2 via interactions with BRD4, suggesting that NSD2 may play an important role in the progression of SARS-CoV2.204 Proteolysis protein chimeras (PROTACs) targeting
Techniques: Solvent
Journal: The Journal of Biological Chemistry
Article Title: Downregulation of the splicing regulator NSRP1 confers resistance to CDK4/6 inhibitors via activation of interferon signaling in breast cancer
doi: 10.1016/j.jbc.2024.108070
Figure Lengend Snippet: NSRP1 regulated the AS of many oncogenes . A , Volcano plots of significant altered AS events in MCF7 cells with transfection of siNSRP1s or siControl. B , Pie plot of the proportion of 5 AS types of significant altered AS events (siNSRP1s vs. siControl). C , distribution of AS events in locations of transcripts. D , KEGG enrichment of genes with altered AS events. The genes regulating the IFN pathway were labeled with bold style. E–G , Sashimi plots of altered AS events in NSD2, IL4R, and HRAS. RT-PCR was also performed to detect the inclusion of exons in NSD2, IL4R, and HRAS. Comparison by one-way ANOVA followed by the Tukey test ( E–G : n = 3 replicates/group). Error bars represent SD.
Article Snippet: Control siRNA and siRNAs targeting NSRP1 or
Techniques: Transfection, Labeling, Reverse Transcription Polymerase Chain Reaction, Comparison
Journal: The Journal of Biological Chemistry
Article Title: Downregulation of the splicing regulator NSRP1 confers resistance to CDK4/6 inhibitors via activation of interferon signaling in breast cancer
doi: 10.1016/j.jbc.2024.108070
Figure Lengend Snippet: The inclusion of NSD2 exon 2 was elevated in breast cancer . A , RT-PCR detection of the inclusion of NSD2 exon 2 in MCF7 and MCF7-PalR cells. B , the PSI values of NSD2 exon 2 between breast tumors and normal tissues were compared. C , the association between the PSI values of NSD2 exon 2 and the overall survival of patients with breast cancer was analyzed with the Kaplan-Meier method. D , RT-PCR detection of the inclusion of NSD2 exon 2 in 15 pairs of breast tumors and matched normal tissues from patients diagnosed with ER+/Her2-breast cancer. Comparison by Student’s t test ( A : n = 3 replicates/group, unpaired; B : n = 3 for Normal, n = 143 for Tumor, unpaired; D, n = 14 samples/group, paired) or Kaplan-Meier analysis ( C ). Error bars represent SD.
Article Snippet: Control siRNA and siRNAs targeting NSRP1 or
Techniques: Reverse Transcription Polymerase Chain Reaction, Comparison
Journal: The Journal of Biological Chemistry
Article Title: Downregulation of the splicing regulator NSRP1 confers resistance to CDK4/6 inhibitors via activation of interferon signaling in breast cancer
doi: 10.1016/j.jbc.2024.108070
Figure Lengend Snippet: NSRP1 negatively regulated NSD2 protein expression . A , analysis of the structures of NSD2 transcripts with or without exon 2. B , ribo-Seq data showed that peaks were observed in the exon 2 region in the NSD2 transcript. C , the polysome profiling curves of siControl, siNSRP1-1, and siNSRP1-2 MCF7 cells were indicated. D , RT-qPCR was performed to detect the ratio of NSD2 mRNA in polysomal (Poly) and subpolysomal (Subpoly) fractions from polysome profiling of siControl, siNSRP1-1, and siNSRP1-2 MCF7 cells. E and F , Western blotting detection of protein levels of NSD2 in MCF7 ( E ) and MCF7-PalR ( F ) cells with transfection of siNSRP1s or siControl. G , Western blotting detection of protein levels of NSD2 in MCF7-PalR cells with transfection of pcDNA3 or pcDNA3-NSRP1. H and I , Western blotting detection of protein levels of NSD2 and IFN-stimulated genes in MCF7 or MCF7-PalR cells with transfection of siNSD2s or siControl. J , Western blotting detection of protein levels of NSD2 and IFN-stimulated genes in MCF7 cells with overexpression of NSD2. K , Western blotting detection of protein levels of NSRP1, NSD2, and IFN-stimulated genes in MCF7-PalR cells with overexpression of NSRP1 or NSD2 or NSRP1 + NSD2. Comparison by one-way ANOVA followed by the Tukey test ( D–F , H , I , K , and L : n = 3 replicates/group) or Student’s t test ( G and J : n = 3 replicates/group, unpaired). Error bars represent SD.
Article Snippet: Control siRNA and siRNAs targeting NSRP1 or
Techniques: Expressing, Quantitative RT-PCR, Western Blot, Transfection, Over Expression, Comparison