Patentscope RSS feed

USE OF TWO DIMENSIONAL 15N/1N NMR CORRELATION SPECTROSCOPY IN A PROCESS FOR DESIGNING HIGH-AFFINITY LIGANDS TO TARGET BIOMOLECULES (Tue, 01 Jun 2004)
A process of designing a drug that serves as a ligand to a given target molecule comprising the steps of: (a) identifying a first ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; (b) identifying a second ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; (c) forming a ternary complex by binding the first and second ligands to the target molecule; (d) determining the three dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and (e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained. 1149 י" ב בסיון התשס" ד - June 1, 2004
>> Read More

USE OF TWO DIMENSIONAL 15N/1H NMR CORRELATION SPECTROSCOPY IN A PROCESS FOR DESIGNING HIGH - AFFINITY LIGANDS TO TARGET BIOMOLECULES (Tue, 01 Jun 2004)
A process for designing a high affinity ligand to a given target molecule, comprising: (a) preparing an isotopically-labeled target molecule wherein said molecule is enriched with an NMR detectable isotope; (b) generating a two dimensional 15N/1H NMR correlation spectrum of the isotopically-labeled target molecule; (c) screening the isotopically-labeled target molecule by exposing the target molecule to a plurality of compounds to identify by two dimensional 15N/1H NMR correlation spectroscopy at least a first and second ligand which bind to distinct sites on the target molecule; (d) forming at least a ternary complex by exposing at least the first and second ligand to the isotopically-labeled target molecule; (e) determining the spatial orientation of the at least first and second ligand on the isotopically-labeled target molecule; (f) using the spatial orientation determined in step (e) to design the high affinity ligand based upon the combination of the at least first and second ligands. 1148 י" ב בסיון התשס" ד - June 1, 2004
>> Read More

USE OF TWO DIMENSIONAL 15N/1N NMR CORRELATION SPECTROSCOPY IN A PROCESS FOR DESIGNING HIGH-AFFINITY LIGANDS TO TARGET BIOMOLECULES (Tue, 01 Jun 2004)
A method for discovering high- affinity ligands to target molecules using structure-activity relationships obtained from nuclear magnetic resonance, comprising: (i) screening low molecular weight (l450mw) compounds which bind to a subsite 1 of a given target molecule using two dimensional 15N/1H NMR correlation spectroscopy to measure binding affinity; (ii) screening analogs prepared from binding results obtained in step (i) to optimize binding of a first fragment to the target molecule; (iii) screening for compounds and corresponding analogs which bind to a nearby binding site, subsite 2, of the target molecule using two dimensional 15N/1H NMR correlation spectroscopy to measure binding affinity to optimize binding of a second fragment to the target molecule; and (iv) combining the first and second fragments to design a high-affinity ligand.
>> Read More

USE OF TWO-DIMENSIONAL 15N/1H NMR CORRELATION SPECTROSCOPY IN A PROCESS FOR DESIGNING HIGH-AFFINITY LIGANDS TO TARGET MOLECULES (Tue, 01 Jun 2004)
A process for designing a high- affinity ligand to a given target molecule comprising: (a) identifying a first ligand to the target molecule using two dimensional 15N/1H NMR correlation spectroscopy; (b) identifying a second ligand to the target molecule using two dimensional 15N/1H NMR correlation spectroscopy wherein the second ligand may be the same or different than the first ligand and wherein the second ligand binds to a different site on the target molecule than the first ligand; (c) forming a ternary complex by binding the first and second ligands to the target molecule; (d) determining the three dimensional structure of the complex and thus the spatial orientation of the first ligand and the second ligand on the target molecule; and (e) designing the high-affinity ligand wherein the spatial orientation of step (d) is maintained. 1147 י" ב בסיון התשס" ד - June 1, 2004
>> Read More

USE OF NUCLEAR MAGNETIC RESONANCE TO IDENTIFY LIGANDS TO TARGET BIOMOLECULES (Wed, 30 Sep 1998)
The present invention provides a process for identifying compounds which bind to a specific target molecule. The process includes the steps of: a) generating a first two-dimensional ?15¿N/?1¿H NMR correlation spectrum of a ?15¿N-labeled target molecule; b) exposing the labeled target molecule to one or a mixture of chemical compounds; c) generating a second two-dimensional ?15¿N/?1¿H NMR correlation spectrum of the labeled target molecule that has been exposed to one or a mixture of compounds in step (b); and d) comparing said first and second two-dimensional ?15¿N/?1¿H NMR correlation spectra to determine differences between said first and said second spectra, the differences indentifying the presence of one or more compounds that are ligands which have bound to the target molecule.
>> Read More

Use of nuclear magnetic resonance to identify ligands to target biomolecules (Tue, 08 Sep 1998)
The present invention provides a process for identifying compounds which bind to a specific target molecule. The process includes the steps of a) generating a first two-dimensional .sup.15 N/.sup.1 H NMR correlation spectrum of a .sup.15 N-labeled target molecule; b) exposing the labeled target molecule to one or a mixture of chemical compounds; c) generating a second two-dimensional .sup.15 N/.sup.1 H NMR correlation spectrum of the labeled target molecule that has been exposed to one or a mixture of compounds in step (b); and d) comparing said first and second two-dimensional .sup.15 N/.sup.1 H NMR correlation spectra to determine differences between said first and said second spectra, the differences identifying the presence of one or more compounds that are ligands which have bound to the target molecule.
>> Read More

USE OF NUCLEAR MAGNETIC RESONANCE TO IDENTIFY LIGANDS TO TARGET BIOMOLECULES (Thu, 22 May 1997)
The present invention provides a process for identifying compounds which bind to a specific target molecule. The process includes the steps of: a) generating a first two-dimensional 15N/1H NMR correlation spectrum of a 15N-labeled target molecule; b) exposing the labeled target molecule to one or a mixture of chemical compounds; c) generating a second two-dimensional 15N/1H NMR correlation spectrum of the labeled target molecule that has been exposed to one or a mixture of compounds in step (b); and d) comparing said first and second two-dimensional 15N/1H NMR correlation spectra to determine differences between said first and said second spectra, the differences indentifying the presence of one or more compounds that are ligands which have bound to the target molecule.
>> Read More

PROCESS OF DESIGNING A DRUG (Thu, 22 May 1997)
The present invention provides a process of designing compounds which bind to a specific target molecule. The process includes the steps of a) identifying a first ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; b) identifying a second ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; c) forming a ternary complex by binding the first and second ligands to the target molecule; d) determining the three-dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained.
>> Read More

USE OF NUCLEAR MAGNETIC RESONANCE TO DESIGN LIGANDS TO TARGET BIOMOLECULES (Thu, 22 May 1997)
The present invention provides a process of designing compounds which bind to a specific target molecule. The process includes the steps of a) identifying a first ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; b) identifying a second ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; c) forming a ternary complex by binding the first and second ligands to the target molecule; d) determining the three-dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained.
>> Read More

USE OF NUCLEAR MAGNETIC RESONANCE TO DESIGN LIGANDS TO TARGET BIOMOLECULES (Wed, 14 Oct 1998)
The present invention provides a process of designing compounds which bind to a specific target molecule. The process includes the steps of a) identifying a first ligand to the target molecule using two-dimensional ?15¿N/?1¿H NMR correlation spectroscopy; b) identifying a second ligand to the target molecule using two-dimensional ?15¿N/?1¿H NMR correlation spectroscopy; c) forming a ternary complex by binding the first and second ligands to the target molecule; d) determining the three-dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained.
>> Read More

Method of designing and forming ligands which bind to target biomolecules (Wed, 23 Feb 2000)
A method for designing and forming a ligand which binds to a specific target molecule comprises the steps of: (a) identifying a first ligand moiety that binds to the target molecule using two-dimensional <15>N/<1>H NMR correlation spectroscopy; (b) identifying subsequent ligand moieties that bind to the target molecule using two-dimensional <15>N/<1>H NMR correlation spectroscopy; (c) forming a complex of the first and subsequent ligand moieties to the target molecule; (d) determining the three-dimensional structure of the complex and, thus, the spatial orientation of the first and subsequent ligand moieties on the target molecule; and (e) linking the first and subsequent ligand moieties to form a new ligand to maintain the spatial orientation of the ligand moieties.
>> Read More

Use of nuclear magnetic resonance to design ligands to target biomolecules (Tue, 06 Apr 1999)
The present invention provides a process of designing compounds which bind to a specific target molecule. The process includes the steps of a) identifying a first ligand to the target molecule using two-dimensional .sup.15 N/.sup.1 H NMR correlation spectroscopy; b) identifying a second ligand to the target molecule using two-dimensional .sup.15 N/.sup.1 H NMR correlation spectroscopy; c) forming a ternary complex by binding the first and second ligands to the target molecule; d) determining the three dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained.
>> Read More

Use of nuclear magnetic resonance to design ligands to target biomolecules (Tue, 23 Nov 1999)
The present invention provides a process of designing compounds which bind to a specific target molecule. The process includes the steps of a) identifying a first ligand to the target molecule using two-dimensional .sup.15 N/.sup.1 H NMR correlation spectroscopy; b) identifying a second ligand to the target molecule using two-dimensional .sup.15 N/.sup.1 H NMR correlation spectroscopy; c) forming a ternary complex by binding the first and second ligands to the target molecule; d) determining the three dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained.
>> Read More

USE OF TWO-DIMENSIONAL 15N/1H NMR CORRELATION SPECTROSCOPY IN A PROCESS FOR DESIGNING HIGH-AFFINITY LIGANDS TO TARGET MOLECULES (Tue, 01 Jun 2004)
A process for designing a high affinity ligand to a given target molecule, comprising: (a) identifying at least two ligands to the target molecule which bind to distinct binding sites on the target molecule using two dimensional 15N/1H NMR correlation spectroscopy; (b) forming at least a ternary complex by exposing the at least two ligands to the target molecule; (c) determining the three dimensional structure of the complex and the spatial orientation of the at least two ligands on the target molecule; and (d) using the spatial orientation determined in step (c) to design the affinity ligand. 989 י" ב בסיון התשס" ד - June 1, 2004
>> Read More

METHOD FOR IDENTIFYING LIGANDS (Thu, 22 May 1997)
The present invention provides a process of designing compounds which bind to a specific target molecule. The process includes the steps of a) identifying a first ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; b) identifying a second ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; c) forming a ternary complex by binding the first and second ligands to the target molecule; d) determining the three-dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained.
>> Read More

USE OF NUCLEAR MAGNETIC RESONANCE TO IDENTIFY LIGANDS TO TARGET BIOMOLECULES (Thu, 22 May 1997)
The present invention provides a process for identifying compounds which bind to a specific target molecule. The process includes the steps of: a) generating a first two-dimensional 15N/1H NMR correlation spectrum of a 15N-labeled target molecule; b) exposing the labeled target molecule to one or a mixture of chemical compounds; c) generating a second two-dimensional 15N/1H NMR correlation spectrum of the labeled target molecule that has been exposed to one or a mixture of compounds in step (b); and d) comparing said first and second two-dimensional 15N/1H NMR correlation spectra to determine differences between said first and said second spectra, the differences indentifying the presence of one or more compounds that are ligands which have bound to the target molecule.
>> Read More

USE OF 13C-NMR TO DETECT BINDING (Thu, 19 Oct 2000)
Methods of detecting binding of a putative ligand to a 13C-enriched target molecule, methods of screening for compounds which bind to a 13C-enriched target molecule, methods for calculating the dissociation constant of a ligand compound which binds to a 13C-enriched target molecule, and methods employed in the determination of the specific amino acids in a 13C-enriched target molecule affected by the binding of a ligand, as well as compounds identified by these screening methods, are provided herewith.
>> Read More

USE OF 13C-NMR TO DETECT BINDING (Wed, 09 Jan 2002)
Methods of detecting binding of a putative ligand to a ?13¿C-enriched target molecule, methods of screening for compounds which bind to a ?13¿C-enriched target molecule, methods for calculating the dissociation constant of a ligand compound which binds to a ?13¿C-enriched target molecule, and methods employed in the determination of the specific amino acids in a ?13¿C-enriched target molecule affected by the binding of a ligand, as well as compounds identified by these screening methods, are provided herewith.
>> Read More

USE OF 13C-NMR TO DETECT BINDING (Sun, 17 Jun 2007)

>> Read More

USE OF NUCLEAR MAGNETIC RESONANCE TO DESIGN LIGANDS TO TARGET BIOMOLECULES (Thu, 22 May 1997)
The present invention provides a process of designing compounds which bind to a specific target molecule. The process includes the steps of a) identifying a first ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; b) identifying a second ligand to the target molecule using two-dimensional 15N/1H NMR correlation spectroscopy; c) forming a ternary complex by binding the first and second ligands to the target molecule; d) determining the three-dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained.
>> Read More