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Methods for Identifying Compounds that Modulate Enzymatic Activities by Employing Covalently Bonded Target-Extender Complexes with Ligand Candidates

  • US 20080220536A1
  • Filed: 04/16/2007
  • Published: 09/11/2008
  • Est. Priority Date: 06/26/1998
  • Status: Abandoned Application
First Claim
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1. A method comprising:

  • a) providing a target having a reactive thiol located outside of a site of interest;

    b) contacting the target with an extender thereby forming a target-extender complex wherein the extender comprises a first functionality that forms a first covalent bond with the thiol and a second functionality that is capable of forming a second covalent bond;

    c) contacting the target-extender complex with a candidate ligand that comprises a group that is capable of forming a second covalent bond with the second functionality;

    d) forming a second covalent bond between the target-extender complex and the candidate ligand thereby forming a target-extender-ligand conjugate; and

    , e) identifying the candidate ligand present in the target-extender-ligand conjugate;

    wherein at least the second covalent bond formed is a disulfide bond.

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