2364-59-2Relevant articles and documents
Benzoxepine-5-ketone compound as well as preparation method and application thereof
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Paragraph 0124-0128, (2021/03/30)
The invention relates to a benzoxazepine-5-ketone compound as well as a preparation method and application thereof. The benzoxazepine-5-ketone compound has a structure as shown in a formula (I) defined in the description. The benzoxazepine-5-ketone compound can block the excessive generation of pro-inflammatory factors in the brain, and provides a feasible alternative treatment strategy for treating AIS.
Chemoselective and Site-Selective Lysine-Directed Lysine Modification Enables Single-Site Labeling of Native Proteins
Adusumalli, Srinivasa Rao,Kalra, Neetu,Purushottam, Landa,Rai, Vishal,Rawale, Dattatraya Gautam,Reddy, Neelesh C.,Shukla, Sanjeev,Thakur, Kalyani
supporting information, p. 10332 - 10336 (2020/04/27)
The necessity for precision labeling of proteins emerged during the efforts to understand and regulate their structure and function. It demands selective attachment of tags such as affinity probes, fluorophores, and potent cytotoxins. Here, we report a method that enables single-site labeling of a high-frequency Lys residue in the native proteins. At first, the enabling reagent forms stabilized imines with multiple solvent-accessible Lys residues chemoselectively. These linchpins create the opportunity to regulate the position of a second Lys-selective electrophile connected by a spacer. Consequently, it enables the irreversible single-site labeling of a Lys residue independent of its place in the reactivity order. The user-friendly protocol involves a series of steps to deconvolute and address chemoselectivity, site-selectivity, and modularity. Also, it delivers ordered immobilization and analytically pure probe-tagged proteins. Besides, the methodology provides access to antibody-drug conjugate (ADC), which exhibits highly selective anti-proliferative activity towards HER-2 expressing SKBR-3 breast cancer cells.
Aldehydes can switch the chemoselectivity of electrophiles in protein labeling
Adusumalli, Srinivasa Rao,Rawale, Dattatraya Gautam,Rai, Vishal
supporting information, p. 9377 - 9381 (2019/01/03)
We show that the chemoselectivity of an electrophile in protein labeling can be promiscuous. An aldehyde enables switching of chemoselectivity of an epoxide and a sulfonate ester along with an enhanced rate of reaction. The chemical technology renders single-site installation of diverse probes on a protein and delivers analytically pure tagged proteins.