[EN] Phosphatase Binding Compounds and Methods of Using Same<br/>[FR] COMPOSÉS DE LIAISON À LA PHOSPHATASE ET LEURS PROCÉDÉS D'UTILISATION
申请人:UNIV YALE
公开号:WO2020146470A1
公开(公告)日:2020-07-16
The present invention provides bifunctional compounds that efficiently dephosphorylate certain phospho-activated target proteins. Such target proteins can be any protein involved in the pathway of a disease or disorder, such as but not limited to cancer, neurodegeneration, metabolic disease, diabetes, insulin resistance, and so forth.
Compositions and methods for enhancing proteasome activity
申请人:President and Fellows of Harvard College
公开号:US10351568B2
公开(公告)日:2019-07-16
Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.
Provided herein are novel small-molecules that have use in the inhibition of Eis, which mediates kanamycin resistance in
Mycobacterium tuberculosis
. The presently-disclosed subject matter further includes a pharmaceutical composition including a small molecule inhibitor, as described herein, and a suitable pharmaceutical carrier. Methods of treating
tuberculosis
comprising administering to an individual an effective amount of the disclosed small molecule inhibitors to mediate kanamycin A resistance and treat
tuberculosis
are also provided.
Photometric Characterization of the Reductive Amination Scope of the Imine Reductases from<i>Streptomyces tsukubaensis</i>and<i>Streptomyces ipomoeae</i>
reductive amination catalyzed by two promising imine reductases is established in a rapid photometric NADPH assay. Substrates ranging from aldehydes to ketones and from primary to secondaryamines are accepted, thus giving access to various secondary and tertiaryamine products.