Small-Molecules Targeting Sirtuin 1: A Patent Review (2012-2015)

Small-Molecules Targeting Sirtuin 1: A Patent Review (2012-2015)

Sirtuins are a family of enzymes, which govern genome regulation, stress response, metabolic homeostasis and lifespan. Among all the discovered human isoforms (SIRT1-7), SIRT1 emerged as a promising molecular target for the treatment of several diseases. The SIRT1 activators have shown beneficial effects in diabetes, obesity, disorders related to aging, cardiovascular and neurodegenerative dise...

Inhibitors of programmed cell death 1 (PD-1): a patent review (2010-2015).

Targeting RNA with small molecules.

5.1. Binding Sites of the Aminoglycosides 1185 5.2. Importance of Electrostatic Interactions 1185 5.3. Nonionic Interactions 1185 5.4. Pseudo-Base Pair Interactions 1186 5.5. Water-Mediated Contacts 1186 5.6. Shape Complementarity and Conformational Adaptation 1186 6. Assays for Evaluating RNA Binding 1186 6.1. Methods Utilizing Fluorescently Labeled RNA 1186 6.2. NMR-Based Methods 1187 6.3. El...

Small molecules targeting viral RNA.

Highly conserved noncoding RNA (ncRNA) elements in viral genomes and transcripts offer new opportunities to expand the repertoire of drug targets for the development of antiinfective therapy. Ligands binding to ncRNA architectures are able to affect interactions, structural stability or conformational changes and thereby block processes essential for viral replication. Proof of concept for targ...

Indoleamine 2,3-dioxygenase inhibitors: a patent review (2008 - 2012).

INTRODUCTION The inhibition of indoleamine 2,3-dioxygenase (IDO) has emerged as a key area in cancer immunotherapy in the past decade. Despite the large variety of potential inhibitors screened so far, the number of active scaffolds remains limited. AREAS COVERED All relevant patent literature published between 2008 and 2012 is reviewed. Representative examples are given for each patent and/o...