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

From monoclonal antibodies to small molecules: the development of inhibitors targeting the PD-1/PD-L1 pathway.

Cancer immunotherapy has made an extraordinary journey from bench to bedside. Blocking the interactions between programmed cell death protein 1 (PD-1) and its ligand, PD-L1, has emerged as a promising immunotherapy for treating cancer. Here, we review the development of drugs targeting the PD-1/PD-L1 pathway. We discuss the monoclonal antibodies (mAbs) approved or in clinical trials, peptides a...

Structures, Substrates, and Regulators of Mammalian Sirtuins – Opportunities and Challenges for Drug Development

Sirtuins are NAD(+)-dependent protein deacetylases regulating metabolism, stress responses, and aging processes. Mammalia have seven Sirtuin isoforms, Sirt1-7, which differ in their substrate specificities and subcellular localizations. The physiological functions of Sirtuins make them interesting therapeutic targets, which has stimulated extensive efforts on development of small molecule Sirtu...

Recent advances in developing small molecules targeting RNA.

RNAs are underexploited targets for small molecule drugs or chemical probes of function. This may be due, in part, to a fundamental lack of understanding of the types of small molecules that bind RNA specifically and the types of RNA motifs that specifically bind small molecules. In this review, we describe recent advances in the development and design of small molecules that bind to RNA and mo...

Sirtuin 1 Facilitates Generation of Induced Pluripotent Stem Cells from Mouse Embryonic Fibroblasts through the miR-34a and p53 Pathways

Forced-expression of transcription factors can reprogram somatic cells into induced pluripotent stem cells (iPSC). Recent studies show that the reprogramming efficiency can be improved by inclusion of small molecules that regulate chromatin modifying enzymes. We report here that sirtuin 1 (SIRT1), a member of the sirtuin family of NAD(+)-dependent protein deacetylases, is involved in iPSC forma...

Closure of Small Patent Ductus Arteriosus by Occluding Detachable Coil