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1. 发明申请

WO03057258A3 QUANTITATIVE RANKING OF TRANSIENT LIGAND BINDING TO TARGET BIOMOLECULES 审中-公开
标题翻译：瞬态配体绑定到目标生物分子的定量分级
公开(公告)号：WO03057258A3
公开(公告)日：2003-10-16
申请号：PCT/CA0300014
申请日：2003-01-10
申请人： CA NAT RESEARCH COUNCIL , NI FENG , SU ZHENGDING , XU PING , TOLKATCHEV DMITRI , OSBORNE MICHAEL J , KOUTYCHENKO ANATOL
发明人： NI FENG , SU ZHENGDING , XU PING , TOLKATCHEV DMITRI , OSBORNE MICHAEL J , KOUTYCHENKO ANATOL
IPC分类号： C12Q1/68 , G01N24/08 , G01N33/00 , G01N33/542 , G01R33/46 , G01R33/465 , A61K49/06
CPC分类号： G01N33/542 , G01N24/08 , G01R33/4625 , G01R33/465
摘要： There is provided a method of quantitatively ranking transient ligand binding to target biomolecules by means of NMR relaxation dispersion profiles. The present invention also relates to a method to identify ligand site obeying two-state and more complex binding behavior in a transient complex of a ligand with a target molecule, still with the use of NMR. There is also provided an efficient method to quantitate fast dissociation rates of ligands containing at least one magnetic nuclei by performing NMR relaxation dispersion experiments at different protein concentrations, enabling the evaluation of populations and exchange rates, and extending the practical applicability of the NMR relaxation dispersion experiments.
摘要翻译：提供了一种通过NMR松弛分散谱定量分析瞬时配体与靶生物分子结合的方法。本发明还涉及在使用NMR的情况下，鉴定配体与靶分子的瞬时复合物中符合双态和更复杂结合行为的配体位点的方法。还提供了通过在不同蛋白质浓度下进行NMR松弛分散实验来定量含有至少一个磁核的配体的快速解离速率的有效方法，使得能够评价群体和交换速率，并且扩展了NMR松弛分散体的实际适用性实验。

2. 发明专利

CA2515798A1 PEPTIDE INHIBITORS OF THROMBIN AS POTENT ANTICOAGULANTS 未知
公开(公告)号：CA2515798A1
公开(公告)日：2004-09-10
申请号：CA2515798
申请日：2004-02-27
申请人： CA NAT RESEARCH COUNCIL
发明人： TOLKATCHEV DMITRI , KOUTYCHENKO ANATOL , NI FENG , NATAPOVA ANNA , SU ZHENGDING
IPC分类号： A61K38/00 , C07K14/815 , A61K38/58
摘要： The tetrapeptide Phe-Asn-Pro-Arg (SEQ ID NO: 3) is a structurally-optimized sequence for binding to the active site of thrombin. By conjugating this tetrapeptide or variants thereof to a C-terminal fragment of hirudin, we were able to generate a series of new multivalent inhibitors of thrombin containing only genetically encodable natural amino acids. We found that synergistic binding to both the active site and an exosite of thrombin can be enhanced through substitutions of amino acid residues at the P4, P3 and P3' sites of the active-site directed sequence, Xaa (P4)-Yaa (P3)-Pro (P2)-Arg (P1)-Pro(P1')-Gln(P2')-Zaa(P3'). Complementary to rational design, a phage library was constructed to explore further the residue requirements at the P4, P3 and P3' sites for multivalent and optimized bridge-binding. Panning of the phage library has led to thrombin-inhibitory peptides possessing strong anti-clotting activities in the low nanomolar range and yet interfering only partially with the catalytic active site of thrombin. In all, the availability of potent and genetically-encodable polypeptide inhibitors of thrombin opens the door for much wider applications of this clinically-successful class of anticoagulants, e.g. through more cost-effective recombinant peptide production, in areas such as gene therapy as well as to improve clinical efficacy/safety through the incorporation of homing peptides for targeted delivery.

3. 发明专利

CA2472193A1 QUANTITATIVE RANKING OF TRANSIENT LIGAND BINDING TO TARGET BIOMOLECULES 未知
公开(公告)号：CA2472193A1
公开(公告)日：2003-07-17
申请号：CA2472193
申请日：2003-01-10
申请人： CA NAT RESEARCH COUNCIL
发明人： TOLKATCHEV DMITRI , OSBORNE MICHAEL J , KOUTYCHENKO ANATOL , SU ZHENGDING , XU PING , NI FENG
IPC分类号： C12Q1/68 , G01N24/08 , G01N33/00 , G01N33/542 , G01R33/46 , G01R33/465 , A61K49/06
摘要： There is provided a method of quantitatively ranking transient ligand binding to target biomolecules by means of NMR relaxation dispersion profiles. The present invention also relates to a method to identify ligand site obeying two- state and more complex binding behavior in a transient complex of a ligand with a target molecule, still with the use of NMR. There is also provided an efficient method to quantitate fast dissociation rates of ligands containing at least one magnetic nuclei by performing NMR relaxation dispersion experiments at different protein concentrations, enabling the evaluation of populations and exchange rates, and extending the practical applicability of the NMR relaxation dispersion experiments.

4. 发明专利

AU2003201554A1 QUANTITATIVE RANKING OF TRANSIENT LIGAND BINDING TO TARGET BIOMOLECULES BY USE OF NUCLEAR MAGNETIC RESONANCE 未知
公开(公告)号：AU2003201554A1
公开(公告)日：2003-07-24
申请号：AU2003201554
申请日：2003-01-10
申请人： CA NAT RESEARCH COUNCIL
发明人： NI FENG , SU ZHENGDING , XU PING , TOLKATCHEV DMITRI , OSBORNE MICHAEL J , KOUTYCHENKO ANATOL
IPC分类号： C12Q1/68 , G01N24/08 , G01N33/00 , G01N33/542 , G01R33/46 , G01R33/465 , A61K49/00
摘要： There is provided a method of quantitatively ranking transient ligand binding to target biomolecules by means of NMR relaxation dispersion profiles. The present invention also relates to a method to identify ligand site obeying two-state and more complex binding behavior in a transient complex of a ligand with a target molecule, still with the use of NMR. There is also provided an efficient method to quantitate fast dissociation rates of ligands containing at least one magnetic nuclei by performing NMR relaxation dispersion experiments at different protein concentrations, enabling the evaluation of populations and exchange rates, and extending the practical applicability of the NMR relaxation dispersion experiments.

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