Patent classifications
C07K7/64
Cyclic polypeptides for PCSK9 inhibition
- Alonso Ricardo ,
- Thomas Joseph Tucker ,
- Nicolas Cedric Boyer ,
- Joseph R. Stringer ,
- Derek M. LaPlaca ,
- Angela Dawn Kerekes ,
- Chengwei Wu ,
- Sookhee Nicole Ha ,
- Hyewon Youm ,
- Mark W. Embrey ,
- Elisabetta Bianchi ,
- Danila Branca ,
- Raffaele Ingenito ,
- Willy Costantini ,
- Alessia Santoprete ,
- Roberto Costante ,
- Immacolata Conte ,
- Stefania Colarusso ,
- Eric J. Gilbert ,
- Aurash Shahripour ,
- Yusheng Xiong
Provided herein are cyclic polypeptide compounds that can, e.g., bind specifically to human proprotein convertase subtilisin/kexin type 9 (PCSK9) and optionally also inhibit interaction between human PCSK9 and human low density lipoprotein receptor (LDLR), and pharmaceutical compositions comprising one or more of these compounds. Also provided are methods of reducing LDL cholesterol level in a subject in need thereof that include administering to the subject one or more of the cyclic polypeptide compounds or a pharmaceutical composition provided herein.
Cyclic polypeptides for PCSK9 inhibition
- Alonso Ricardo ,
- Thomas Joseph Tucker ,
- Nicolas Cedric Boyer ,
- Joseph R. Stringer ,
- Derek M. LaPlaca ,
- Angela Dawn Kerekes ,
- Chengwei Wu ,
- Sookhee Nicole Ha ,
- Hyewon Youm ,
- Mark W. Embrey ,
- Elisabetta Bianchi ,
- Danila Branca ,
- Raffaele Ingenito ,
- Willy Costantini ,
- Alessia Santoprete ,
- Roberto Costante ,
- Immacolata Conte ,
- Stefania Colarusso ,
- Eric J. Gilbert ,
- Aurash Shahripour ,
- Yusheng Xiong
Provided herein are cyclic polypeptide compounds that can, e.g., bind specifically to human proprotein convertase subtilisin/kexin type 9 (PCSK9) and optionally also inhibit interaction between human PCSK9 and human low density lipoprotein receptor (LDLR), and pharmaceutical compositions comprising one or more of these compounds. Also provided are methods of reducing LDL cholesterol level in a subject in need thereof that include administering to the subject one or more of the cyclic polypeptide compounds or a pharmaceutical composition provided herein.
MULTI-ANTIGENIC PEPTIDE MIMICS OF GONOCOCCAL LIPO-OLIGOSACCHARIDE (LOS) EPITOPES
In some aspects, the disclosure relates to compositions of peptide mimics useful in the treatment of Neisseria gonorrhoeae (N. gonorrhoeae). In some embodiments, the peptide mimics are multi-antigenic molecules of a conserved gonococcal lipoohgosaccharaide (LOS) epitope. In some aspects, the disclosure relates to methods of making peptide mimics for the treatment of N. gonorrhoeae. In some aspects, the disclosure relates to methods of using peptide mimics for the treatment of N. gonorrhoeae.
MULTI-ANTIGENIC PEPTIDE MIMICS OF GONOCOCCAL LIPO-OLIGOSACCHARIDE (LOS) EPITOPES
In some aspects, the disclosure relates to compositions of peptide mimics useful in the treatment of Neisseria gonorrhoeae (N. gonorrhoeae). In some embodiments, the peptide mimics are multi-antigenic molecules of a conserved gonococcal lipoohgosaccharaide (LOS) epitope. In some aspects, the disclosure relates to methods of making peptide mimics for the treatment of N. gonorrhoeae. In some aspects, the disclosure relates to methods of using peptide mimics for the treatment of N. gonorrhoeae.
Macrocyclic polypeptides
Disclosed herein are macrocyclic polypeptides having no more than 3 ammo acid substitutions compared to the amino acid sequence of any one of SEQ ID NO: 1-2.37 or a mirror image thereof, wherein the polypeptide includes both L and D amino acids, libraries of such polypeptides, and uses thereof.
Macrocyclic polypeptides
Disclosed herein are macrocyclic polypeptides having no more than 3 ammo acid substitutions compared to the amino acid sequence of any one of SEQ ID NO: 1-2.37 or a mirror image thereof, wherein the polypeptide includes both L and D amino acids, libraries of such polypeptides, and uses thereof.
Synthesis of echinocandin antifungal agent
The present invention relates to echinocandin cyclopeptides and to methods for preparing echinocandin cyclopeptides.
Synthesis of echinocandin antifungal agent
The present invention relates to echinocandin cyclopeptides and to methods for preparing echinocandin cyclopeptides.
Targeting aminoacid lipids
The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Optionally one or more further bioactive agents may be encapsulated or embedded within or attached to or adsorbed onto the carrier system. The present invention is further directed to methods of their preparation and their uses in medical applications, such as targeted delivery of bioactive agents to specific tissues or cells and antigen display systems for the study, diagnosis, and treatment of traits, diseases and conditions that respond to said bioactive agents.
Targeting aminoacid lipids
The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Optionally one or more further bioactive agents may be encapsulated or embedded within or attached to or adsorbed onto the carrier system. The present invention is further directed to methods of their preparation and their uses in medical applications, such as targeted delivery of bioactive agents to specific tissues or cells and antigen display systems for the study, diagnosis, and treatment of traits, diseases and conditions that respond to said bioactive agents.