Application of ring-closing metathesis macrocyclization to the development of Tsg101-binding antagonists
摘要:
HIV-1 viral budding involves binding of the viral Gag(p6) protein to the ubiquitin E2 variant domain of the human tumor susceptibility gene 101 protein (Tsg101). Recognition of p6 by Tsg101 is mediated in part by a proline-rich motif that contains the sequence 'Pro-Thr-Ala-Pro' ('PTAP'). Using the p6-derived 9-mer sequence 'PEPTAPPEE', we had previously improved peptide binding affinity by employing N-alkylglycine ('peptoid') residues. The current study applies ring-closing metathesis macrocyclization strategies to Tsg101-binding peptide-peptoid hybrids as an approach to stabilize binding conformations and to observe the effects of such macrocyclization on Tsg101-binding affinity and bioavailability. Published by Elsevier Ltd.
Application of ring-closing metathesis macrocyclization to the development of Tsg101-binding antagonists
摘要:
HIV-1 viral budding involves binding of the viral Gag(p6) protein to the ubiquitin E2 variant domain of the human tumor susceptibility gene 101 protein (Tsg101). Recognition of p6 by Tsg101 is mediated in part by a proline-rich motif that contains the sequence 'Pro-Thr-Ala-Pro' ('PTAP'). Using the p6-derived 9-mer sequence 'PEPTAPPEE', we had previously improved peptide binding affinity by employing N-alkylglycine ('peptoid') residues. The current study applies ring-closing metathesis macrocyclization strategies to Tsg101-binding peptide-peptoid hybrids as an approach to stabilize binding conformations and to observe the effects of such macrocyclization on Tsg101-binding affinity and bioavailability. Published by Elsevier Ltd.
Novel Silane Compounds and Use of Same for Functionalizing Solid Supports and Immobilizing Biological Molecules on These Supports
申请人:Martin Franck
公开号:US20090029875A1
公开(公告)日:2009-01-29
The invention relates to novel silane compounds corresponding to the formula (I) below:
A-E-X (I)
in which:
X represents a silyl group capable of creating a covalent bond after reaction with the hydroxyl or hydride functional groups of a support;
E represents an organic spacer group;
A represents a group chosen from the groups of formulae below:
in which:
Z
1
to Z
5
independently represent a hydrogen atom or a halogen atom;
Z
6
and Z
7
represent a group for protecting the phosphonic acid functional group, a hydrogen atom or a monovalent cation;
Z
8
to Z
12
independently represent a group for protecting the carboxylic acid functional group, a hydrogen atom or a monovalent cation; and
Z
13
represents an imidazole, N-hydroxysuccinimide, nitrophenyl, pentafluorophenyl or acid anhydride group.
Use of these silane compounds for functionalizing solid supports and for immobilizing biological molecules on these supports.
US9657042B2
申请人:——
公开号:US9657042B2
公开(公告)日:2017-05-23
Application of ring-closing metathesis macrocyclization to the development of Tsg101-binding antagonists
作者:Fa Liu、Andrew G. Stephen、Abdul A. Waheed、Eric O. Freed、Robert J. Fisher、Terrence R. Burke
DOI:10.1016/j.bmcl.2009.10.105
日期:2010.1
HIV-1 viral budding involves binding of the viral Gag(p6) protein to the ubiquitin E2 variant domain of the human tumor susceptibility gene 101 protein (Tsg101). Recognition of p6 by Tsg101 is mediated in part by a proline-rich motif that contains the sequence 'Pro-Thr-Ala-Pro' ('PTAP'). Using the p6-derived 9-mer sequence 'PEPTAPPEE', we had previously improved peptide binding affinity by employing N-alkylglycine ('peptoid') residues. The current study applies ring-closing metathesis macrocyclization strategies to Tsg101-binding peptide-peptoid hybrids as an approach to stabilize binding conformations and to observe the effects of such macrocyclization on Tsg101-binding affinity and bioavailability. Published by Elsevier Ltd.