Chemical Synthesis of an Enzyme Containing an Artificial Catalytic Apparatus
Keyword(s):
Hiv 1
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With the goal of investigating electronic aspects of the catalysis of peptide bond hydrolysis, an analogue of HIV-1 protease was designed in which a non-peptide hydroxy-isoquinolinone artificial catalytic apparatus replaced the conserved Asp25–Thr26–Gly27 sequence in each 99-residue polypeptide chain of the homodimeric enzyme molecule. The enzyme analogue was prepared by total chemical synthesis and had detectable catalytic activity on known HIV-1 protease peptide substrates. Compared with uncatalyzed hydrolysis, the analogue enzyme increased the rate of peptide bond hydrolysis by ∼108-fold. Extensions of this unique approach to the study of enzyme catalysis in HIV-1 protease are discussed.
2007 ◽
Vol 46
(10)
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pp. 1667-1670
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Keyword(s):
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2020 ◽
Vol 26
(8)
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pp. 802-814
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1998 ◽
Vol 63
(4)
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pp. 541-548
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2007 ◽
Vol 13
(1-2)
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pp. 221-227
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1993 ◽
Vol 90
(24)
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pp. 11638-11642
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1998 ◽
Vol 423
(1-2)
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pp. 137-152
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