Abstract:
:Disulfide exchange screening is a method for evaluating the binding of small molecule fragments to proteins that have at least one accessible cysteine. While operationally simple, it does require a large library of small fragment molecules bearing disulfide-containing side chains. These specialized fragments are not available commercially and this has limited the adoption of the method. We report here a convenient one-pot procedure that enables facile preparation of disulfide screening fragments while also producing less of an environmental impact. The new synthetic method involves the initial formation of symmetric disulfides, followed by a disulfide exchange reaction in which the symmetrical dimer is converted into the final screening fragment by introduction of a solubilizing 'cap'. The method is amenable to parallel synthetic methods and can be carried out in air without the need for the specialized equipment typically required for performing organic synthesis.
journal_name
ACS Comb Scijournal_title
ACS combinatorial scienceauthors
Burlingame MA,Tom CT,Renslo ARdoi
10.1021/co200038gsubject
Has Abstractpub_date
2011-05-09 00:00:00pages
205-8issue
3eissn
2156-8952issn
2156-8944journal_volume
13pub_type
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