Hixson S H, Hixson S S
Biochemistry. 1975 Sep 23;14(19):4251-4. doi: 10.1021/bi00690a016.
The synthesis of the photochemically labile bifunctional reagent p-azidophenacyl bromide (1) is described. This compound may be covalently attached to a known site of an enzyme or other macromolecule by nucleophilic displacement at the alpha-bromo ketone moiety. Subsequent irradiation of the bound reagent gives a nitrene which may insert into a second portion of the enzyme forming a cross-link. Regeant 1 proved to be an excellent inhibitor of rabbit muscle glyceraldehyde-3-phosphate dehydrogenase.
描述了光化学不稳定的双功能试剂对叠氮苯甲酰溴（1）的合成。该化合物可通过α-溴代酮部分的亲核取代共价连接到酶或其他大分子的已知位点。随后对结合的试剂进行辐照会产生氮烯，其可插入酶的另一部分形成交联。试剂1被证明是兔肌肉甘油醛-3-磷酸脱氢酶的优良抑制剂。
