Patent classifications
C07D295/185
CYCLIC PEPTIDE COMPOUND HAVING KRAS INHIBITORY ACTION
The present inventors found cyclic peptide compounds that interact with Ras, and non-natural amino acids useful for the production of the cyclic peptide compounds. The inventors also found that the cyclic peptide compounds inhibit the binding between Ras and SOS. In addition, the inventors found specific non-natural amino acids contained in the cyclic peptide compounds and methods for production thereof.
METHOD FOR RACEMIC PREPARATION OF CHIRAL B-AMINO ACIDS AND DERIVATIVES THEREOF
The present disclosure relates to the field of medicine synthesis, and relates to a method for a racemic preparation of chiral h β-amino acids and derivatives thereof, and in particular to a method for racemizing sitagliptin intermediates.
##STR00001##
where R.sub.1 is hydrogen, alkyl or aryl; R.sub.2 is hydrogen, alkyl or aryl; R.sub.3 is hydrogen, alkyl, aryl or acyl; R.sub.4 is alkyl, aryl, OR′, SR′, NHR′ or NR′R″, wherein R′, R″ are hydrogen, alkyl or aryl.
PROTEIN-PROTEIN INTERACTION STABILIZERS
- Michelle R. Arkin ,
- Lucas Brunsveld ,
- Christian Ottmann ,
- Adam R. Renslo ,
- R. Jeffrey Neitz ,
- Mengqi Zhong ,
- Kenneth K. Hallenbeck ,
- Priyadarshini Jaishankar ,
- Shubhankar Dutta ,
- John K. Morrow ,
- Eline Sijbesma ,
- Bente Aminhan Somsen ,
- Galen Patrick Miley ,
- Emira Josien Visser ,
- Peter James Cossar ,
- Madita Wolter ,
- Thorsten Genski ,
- Laura Mariana Levy ,
- Torsten Hoffmann ,
- Dimitrios Tzalis ,
- Dario Valenti ,
- Markella Konstantinidou
Provided herein, inter alia, are stabilizers of protein-protein interactions and methods of identifying and using the same.
PROTEIN-PROTEIN INTERACTION STABILIZERS
- Michelle R. Arkin ,
- Lucas Brunsveld ,
- Christian Ottmann ,
- Adam R. Renslo ,
- R. Jeffrey Neitz ,
- Mengqi Zhong ,
- Kenneth K. Hallenbeck ,
- Priyadarshini Jaishankar ,
- Shubhankar Dutta ,
- John K. Morrow ,
- Eline Sijbesma ,
- Bente Aminhan Somsen ,
- Galen Patrick Miley ,
- Emira Josien Visser ,
- Peter James Cossar ,
- Madita Wolter ,
- Thorsten Genski ,
- Laura Mariana Levy ,
- Torsten Hoffmann ,
- Dimitrios Tzalis ,
- Dario Valenti ,
- Markella Konstantinidou
Provided herein, inter alia, are stabilizers of protein-protein interactions and methods of identifying and using the same.
COMPOSITIONS AND METHODS FOR TREATING CANCER
K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
COMPOSITIONS AND METHODS FOR TREATING CANCER
K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING NEURODEGENERATIVE DISORDERS
Compounds, pharmaceutical compositions, methods and kits are described for treating or preventing neurodegenerative diseases such as Alzheimer's disease.
COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING NEURODEGENERATIVE DISORDERS
Compounds, pharmaceutical compositions, methods and kits are described for treating or preventing neurodegenerative diseases such as Alzheimer's disease.
TREATMENT OF DISORDERS ASSOCIATED WITH OXIDATIVE STRESS AND COMPOUNDS FOR SAME
The present invention relates to the treatment of disorders associated with oxidative stress including neuropathic pain and small synthetically derived compounds for treating such disorders.
USE OF STEREOSELECTIVE TRANSAMINASE IN ASYMMETRIC SYNTHESIS OF CHIRAL AMINE
Use of a stereoselective transaminase in the asymmetric synthesis of a chiral amine. In particular, provided is use of a polypeptide in the production of a chiral amine or a downstream product using a chiral amine as a precursor. Further provided is a method for producing a chiral amine, comprising culturing a strain expressing the polypeptide so as to obtain a chiral amine. Further provided are novel prochiral compounds, a chiral amine production strain and a method for constructing the chiral amine production strain. The stereoselective transaminase has a broad substrate spectrum and thus has a broad application potential in the preparation of a chiral amine.