An inhibitor based on crosslinked peptides from the interfacial region of HIV-1 protease, previously shown to act by dimerization inhibition, was modified by N-methylation to ascertain the importance of the amide hydrogens on inhibition. The effects of N-methylation on HIV-1 protease inhibition, as well as the effects on degradation by proteases are described. (C) 2004 Elsevier Ltd. All rights reserved.
机构:
Kyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashima Ku, Kyoto 6078412, JapanKyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashima Ku, Kyoto 6078412, Japan
Song, MC
Rajesh, S
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Kyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashima Ku, Kyoto 6078412, JapanKyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashima Ku, Kyoto 6078412, Japan
Rajesh, S
Hayashi, Y
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Kyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashima Ku, Kyoto 6078412, JapanKyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashima Ku, Kyoto 6078412, Japan
Hayashi, Y
Kiso, Y
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Kyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashima Ku, Kyoto 6078412, JapanKyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashima Ku, Kyoto 6078412, Japan
机构:
Univ N Carolina Hosp, Div Pharmacotherapy & Infect Dis, Chapel Hill, NC 27514 USAUniv N Carolina Hosp, Div Pharmacotherapy & Infect Dis, Chapel Hill, NC 27514 USA
Dietrich, MA
Butts, JD
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Univ N Carolina Hosp, Div Pharmacotherapy & Infect Dis, Chapel Hill, NC 27514 USAUniv N Carolina Hosp, Div Pharmacotherapy & Infect Dis, Chapel Hill, NC 27514 USA
Butts, JD
Raasch, RH
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Univ N Carolina Hosp, Div Pharmacotherapy & Infect Dis, Chapel Hill, NC 27514 USAUniv N Carolina Hosp, Div Pharmacotherapy & Infect Dis, Chapel Hill, NC 27514 USA