Synthesis, SAR, and application of JQ1 analogs as PROTACs for …
2024年10月1日 · In this review, we have covered the discovery and synthesis of the JQ1 molecule. The SAR of the JQ1 analogs will help researchers develop potent JQ1 compounds …
<br>JQ1 类似物的合成、SAR 及其作为 PROTAC 在癌症治疗中的 …
2024年8月16日 · JQ1 类似物的 SAR 将帮助研究人员开发有效的 JQ1 化合物，并改善对恶性细胞的抑制特性。 此外，我们还探讨了 JQ1 类似物在 PROTAC 技术中的潜在应用。 溴结构域蛋 …
Direct-to-Biology Accelerates PROTAC Synthesis and the …
The D2B synthesis library was designed using dBET1 (1, Scheme 1) as a model system to investigate linker SAR for degraders. Using JQ1 (2) as the POI ligand linked to CRBN E3 …
Synthesis, SAR, and application of JQ1 analogs as ... - ResearchGate
2024年8月16日 · In this review, we have covered the discovery and synthesis of the JQ1 molecule. The SAR of the JQ1 analogs will help researchers develop potent JQ1 compounds …
Drug Discovery Targeting Bromodomain-Containing Protein 4
2017年2月14日 · BRD4 inhibitor (+)-JQ1 (7, Figure 5) is highly efficacious against NMC tumor growth in xenografted mice. BRD4 can also physically interact with androgen receptor (AR), …
Synthesis, SAR, and application of JQ1 analogs as PROTACs for …
2024年8月16日 · JQ1: a novel potential therapeutic target. Accumulating evidence supports the notion of BRD4 suppression as a target of therapeutic intervention in clinical oncology and …
JQ1 synergizes with the Bcl-2 inhibitor ABT-263 against MYCN …
We found that MYCN -amplified SCLC cells were highly sensitive to a Bromodomain and Extra-Terminal domain (BET) inhibitor JQ1, which was able to inhibit N-Myc protein expression. The …
JQ1 synergizes with the Bcl-2 inhibitor ABT-263 against
2017年9月21日 · We found that MYCN-amplified SCLC cells were highly sensitive to a Bromodomain and Extra-Terminal domain (BET) inhibitor JQ1, which was able to inhibit N-Myc …
Immune-enhanced and tumor-targeted PDT cascade therapy for …
2024年4月1日 · PDT and JQ1 provided a cascading facilitation effect and added strengths and compensates for weaknesses. JQ1, a small molecule inhibitor of BRD4, is superior in …
研发前沿|分子胶的理性设计(1)——基于“降解尾巴”的分子胶设计策 …
利用分子胶SAR范围窄的特点，设计基于CRBN（或其他E3连接酶）的数量巨大的化合物库，再通过表型筛选+蛋白质组学的方法去发现基于新靶点的分子胶降解剂。 达歌生物的技术平台便是 …