Novel Pyrazolo[3,4-b]pyrazines as SHP2 Inhibitors for Treating Cancer

SHP2 phosphatase as a novel therapeutic target for melanoma treatment

Melanoma ranks among the most aggressive and deadly human cancers. Although a number of targeted therapies are available, they are effective only in a subset of patients and the emergence of drug resistance often reduces durable responses. Thus there is an urgent need to identify new therapeutic targets and develop more potent pharmacological agents for melanoma treatment. Herein we report that...

Tetrahydroisoquinolines as novel histone deacetylase inhibitors for treatment of cancer.

Histone acetylation is a critical process in the regulation of chromatin structure and gene expression. Histone deacetylases (HDACs) remove the acetyl group, leading to chromatin condensation and transcriptional repression. HDAC inhibitors are considered a new class of anticancer agents and have been shown to alter gene transcription and exert antitumor effects. This paper describes our work on...

Rho Kinase Inhibitors as a Novel Treatment for Glaucoma and Ocular Hypertension

In an elegant example of bench-to-bedside research, a hypothesis that cells in the outflow pathway actively regulate conventional outflow resistance was proposed in the 1990s and systematically pursued, exposing novel cellular and molecular mechanisms of intraocular pressure (IOP) regulation. The critical discovery that pharmacologic manipulation of the cytoskeleton of outflow pathway cells dec...

Chemoimmunotherapy as a Novel Cancer Therapy

Over the past decade, it was widely accepted that some chemotherapeutic drugs can be combined with immunotherapeutic drugs in treatment of cancer. Chemotherapeutic drugs can induce apoptosis in the tumor cell and at the same time stimulate the immune response. Several reports support the use   immunomodulators in treatment of cancers through regulating the immune response and boosting the micro...

novel coumarin analogues: as new acetylcholinesterase inhibitors