الڪائلٿيوفينيم سالٽ استعمال ڪندي سيسٽين تي مشتمل پيپٽائڊس يا پروٽين جي درست تبديلي

الڪائلٿيوفينيم سالٽ استعمال ڪندي سيسٽين تي مشتمل پيپٽائڊس يا پروٽين جي درست تبديلي

حياتياتي ڪيميا, نرم جسماني حالتن جي تحت بايوموليڪولس جي چونڊيل ترميم لاءِ هڪ ورسٽائل طريقو, has attracted the attention of the scientific community in recent years due to its wide range of applications and far-reaching impact. بهرحال, reactive groups (مثال, alkynyl, azide, tetrazine, وغيره) in conventional click chemistry are extremely rare in natural biomolecules, making the introduction of these groups a challenging task. Cysteine (سائيس) is widely present in peptides and proteins, and it is estimated that about 2% of cysteine (سائيس) is present in natural products.This amino acid, which is relatively abundant in proteins and is rich in thiol groups, provides an SH site for the modification of peptides and proteins, based on which an orthogonal chemical modification strategy based on alkyl thiophenium salts has been developed by the research organization.

Technical Highlights

  • Highly selective: Alkyl thiophenium salts are able to directly and selectively orthogonally modify cysteine residues via S_N2 reaction, a process that takes place under mild conditions with high chemoselectivity and compatibility.
  • Multifunctional modification: The technology is capable of introducing a wide range of functional structures, including PEG chains, fluorescent molecules, drugs, carboboranes, carbohydrates, and peptides, greatly enriching the functionality of biomolecules.
  • Multifunctional biocoupling: The study further reveals that the technology enables multifunctional biocoupling by introducing clickable “handles” such as alkynes and azides. This means that a variety of complex biocouplings can be flexibly assembled in a “two-step, one-pot” reaction, further broadening the scope of biomodification applications.
  • Successful application to proteins: The application of this technology to complex proteins has also been validated. Scientists successfully labeled bovine serum albumin (BSA) using alkylthioindigo salts, demonstrating the universality and effectiveness of the method in complex biomolecules.

The orthogonal biocoupling technique based on alkylthiophenium salts is an efficient and precise modification method, which provides a powerful tool for efficient and specific modification of peptides and proteins, and has a broad application prospect.

منتظم اوتار

Xiaoxia چن

نئين دوا آر&ڊي ٽيڪنيشن بنيادي ماهر: ٽارگيٽ دريافت, جوڙجڪ-سرگرمي تعلق (SAR) تجزيو, peptide-drug conjugates (PDCs), ۽ مخالف عمر ۽ ميٽابولڪ پيپٽائڊس جي ترقي.

پروفائل: Xiaoxia Cheن ڪيترن ئي ميٽابولڪ ۽ ٽيومر جي حدف ٿيل پيپٽائڊ دوائن لاءِ ابتدائي دريافت ۽ اڳڪٿي تحقيق جي اڳواڻي ڪئي آهي. هوءَ نه رڳو پيپٽائڊ لائبريرين جي اعليٰ درجي جي اسڪريننگ ۾ ماهر آهي پر ڊي نوو پيپٽائڊ سيڪوئنس ڊيزائن لاءِ AI جي مدد سان ڪمپيوٽيشنل بائيولاجي استعمال ڪرڻ ۾ پڻ ماهر آهي.. في الحال, هوءَ هڪ ٽيم جي اڳواڻي ڪري رهي آهي جيڪا ايندڙ نسل جي گھڻائي واري تحقيق ۽ ترقي لاءِ وقف ڪري رهي آهي. (جهڙوڪ ٻه- يا ٽي ڀيرا ھدف ٿلهي گھٽائيندڙ پيپٽائڊس) ۽ انتهائي سرگرم ٽشو-مرمت peptides.

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