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Position 120-123, a potential active site of trichosanthin.

机译:位置120-123,天花粉蛋白的潜在活性位点。

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Trichosanthin (TCS) is a type-I ribosome-inactivating protein (RIP) with wide spectrum of biological and pharmacological activities. In the present study, a potential site on the TCS molecule (position 120-123) is identified which may be important for the biological activities of TCS. By using site-directed mutagenesis, position 120-123 of TCS was either deleted or changed from Lys-Ile-Arg-Glu (hydrophilic) to Ser-Ala-Gly-Gly (hydrophobic). Deletion of these residues rendered a TCS molecule completely deprived of ribosome inactivating activity, while hydrophobic replacement caused 4000-fold decrease in ribosome inactivating activity. The abortifacient activity of these two mutants was retained with decreased potency. This implies that position 120-123 of the native TCS molecule plays a critical role in maintaining its biological activity.
机译:天花粉蛋白(TCS)是一种I型核糖体失活蛋白(RIP),具有广泛的生物学和药理活性。在本研究中,确定了TCS分子上的潜在位点(位置120-123),这对于TCS的生物学活性可能很重要。通过使用定点诱变,TCS的位置120-123被删除或从Lys-Ile-Arg-Glu(亲水)变为Ser-Ala-Gly-Gly(疏水)。这些残基的缺失使得TCS分子完全丧失了核糖体的失活活性,而疏水性置换导致核糖体的失活活性降低了4000倍。这两个突变体的堕胎活性得以保留,但效力降低。这暗示着天然TCS分子的120-123位在维持其生物活性中起关键作用。

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