N-(3-(p-azido-m-[125I]iodophenyl)propionyl)-succinimide--a heterobifunctional reagent for the synthesis of radioactive photoaffinity ligands: synthesis of a carrier-free 125I-labeled cardiac glycoside photoaffinity label.
N-(3-(p-azido-m-[125I]iodophenyl)propionyl)-succinimide--a heterobifunctional reagent for the synthesis of radioactive photoaffinity ligands: synthesis of a carrier-free 125I-labeled cardiac glycoside photoaffinity label.
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N-(3-(对叠氮基-间-[125I]碘苯基)丙酰基)-琥珀酰亚胺--一种用于合成放射性光亲和配体的异双功能试剂：合成无载体的125I标记的强心苷光亲和标记。
DOI：
10.1016/0003-2697(88)90007-3
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发表时间：
1988
影响因子：
2.9
通讯作者：
Ruoho,AE
中科院分区：
文献类型：
--
作者：
Lowndes,JM;Hokin-Neaverson,M;Ruoho,AE
合成了一种新的异双功能试剂 N-(3-(对叠氮基-间碘苯基)丙酰基)-琥珀酰亚胺 (AIPPS)，并进行了化学表征。该试剂的放射化学形式[125I]AIPPS应该作为光活性试剂广泛使用，用于衍生化多种生物活性化合物（包括许多激素）上的游离氨基。含氨基配体可以用[ 125 I]AIPPS衍生化，其方法与用于125 I-标记的Bolton-Hunter试剂(N-(3-(对羟基苯基)丙酰基)-琥珀酰亚胺)的方法类似。然而，[125I]AIPPS 的额外优点是配体衍生物在一步中具有光活性和放射性。作为如何使用该试剂的一个例子，我们制备了无载体的[125I]AIPPS，并将其与含氨基的强心苷、4-氨基-4,6-二脱氧葡萄糖基洋地黄毒苷（GluD）反应。放射性碘标记的强心苷[125I]AIPP-GluD通过薄层色谱法纯化，无载体，比放射性为2175 Ci/mmol。纯化的犬肾酶和人红细胞酶的特异性光亲和标记表明，[125I]AIPP-GluD 是 Na,K-ATP 酶的有效光亲和标记。
A new heterobifunctional reagent, N-(3-(p-azido-m-iodophenyl)propionyl)-succinimide (AIPPS), was synthesized and chemically characterized. The radiochemical form of the reagent, [125I]AIPPS, should be of general use as a photoactive reagent for the derivatization of free amino groups on a large variety of biologically active compounds, including many hormones. Amino-containing ligands can be derivatized with [125I]AIPPS in a method which is similar to that used for the125I-labeled Bolton-Hunter reagent (N-(3-(p-hydroxyphenyl)propionyl)-succinimide). The added advantage with [125I]AIPPS, however, is that the ligand derivative is made both photoactive and radioactive in a single step. As an example of how this reagent can be used, we have prepared carrier-free [125I]AIPPS and reacted it with the amino-containing cardiac glycoside, 4-amino-4,6-dideoxyglucosyl digitoxigenin (GluD). The radioiodinated cardiac glycoside, [125I]AIPP-GluD, was purified by thin-layer chromatography and was carrier-free with a specific radioactivity of 2175 Ci/mmol. [125I]AIPP-GluD was an effective photoaffinity label for Na,K-ATPase as shown by specific photoaffinity labeling of purified canine kidney enzyme and human erythrocyte enzyme.