We disclose the development of a novel series of 2-phenyl-2H-indazole-7-carboxamides as
poly(ADP-ribose)polymerase (PARP) 1 and 2 inhibitors. This series was optimized to …

There is growing evidence that activation of metabotropic glutamate receptor 4 (mGlu 4 )
leads to anxiolytic- and antipsychotic-like efficacy in rodent models, yet its relevance to …

Background Viscosupplementation of synovial fluid with intra-articular (IA) injections of
hyaluronic acid (HA) is widely used for symptomatic treatment of osteoarthritis (OA). Herein we …

HIV integrase is one of the three enzymes encoded by HIV genome and is essential for viral
replication, but integrase inhibitors as marketed drugs have just very recently started to …

The optimization of a potent, class I selective ketone HDAC inhibitor is shown. It possesses
optimized pharmacokinetic properties in preclinical species, has a clean off-target profile, …

In this work, the authors present a novel, robotic, automated protocol for assessing a
metabolic stability protocol assembled on a Hamilton platform and a new strategy for pooling …

The Hedgehog (Hh-) signaling pathway is a key developmental pathway which gets
reactivated in many human tumors, and smoothened (Smo) antagonists are emerging as novel …

LNA-i-miR-221 is a novel phosphorothioate backbone 13-mer locked nucleic acid
oligonucleotide-targeting microRNA-221 designed for the treatment of human malignancies. To …

Smoothened (Smo) antagonists are emerging as new therapies for the treatment of
neoplasias with aberrantly reactivated hedgehog (Hh) signaling pathway. A novel series of 4-[3-(…

UDP-glucuronosyltransferases (UGTs) and cytochrome P450s (CYPs) are the major
enzymes involved in hepatic metabolism of drugs. Hepatic drug metabolism is commonly …