推荐产品
ligand
pomalidomide
质量水平
形式
powder
储存温度
2-8°C
SMILES字符串
O=C1C2=C(C(NCCCCCOP(OCCC#N)N(C(C)C)C(C)C)=CC=C2)C(N1C3C(NC(CC3)=O)=O)=O
应用
Protein degrader building block Pomalidomide-C5-phosphoramidite enables the synthesis of molecules for targeted protein degradation and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a Cereblon (CRBN) recruiting ligand, a rigid linker, and a pendant phosphoramidite for reactivity with target DNA-binding proteins such as transcription factors. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and degrader, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks, parallel synthesis can be used to more quickly generate degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks
其他说明
Targeted Protein Degradation by Small Molecules
Destruction of DNA-Binding Proteins by Programmable Oligonucleotide PROTAC (O′PROTAC): Effective Targeting of LEF1 and ERG
Small-Molecule PROTACS: New Approaches to Protein Degradation
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
Impact of linker length on the activity of PROTACs
Destruction of DNA-Binding Proteins by Programmable Oligonucleotide PROTAC (O′PROTAC): Effective Targeting of LEF1 and ERG
Small-Molecule PROTACS: New Approaches to Protein Degradation
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
Impact of linker length on the activity of PROTACs
法律信息
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
警示用语：
Danger
危险声明
危险分类
Repr. 1B
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Destruction of DNA-Binding Proteins by Programmable Oligonucleotide PROTAC (O'PROTAC): Effective Targeting of LEF1 and ERG
Jingwei Shao, et al.
Advanced science (Weinheim, Baden-Wurttemberg, Germany) (2021)
Jingwei Shao et al.
Advanced science (Weinheim, Baden-Wurttemberg, Germany), 8(20), e2102555-e2102555 (2021-08-17)
DNA-binding proteins, including transcription factors (TFs), play essential roles in various cellular processes and pathogenesis of diseases, deeming to be potential therapeutic targets. However, these proteins are generally considered undruggable as they lack an enzymatic catalytic site or a ligand-binding
Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of
Kedra Cyrus et al.
Molecular bioSystems, 7(2), 359-364 (2010-10-06)
Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations
Momar Toure et al.
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is
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