Through an effort to develop novel ligands that have subtype selectivity for the estrogen
receptors alpha (ERα) and beta (ERβ), we have found that 2,3-bis(4-hydroxyphenyl)propionitrile …

The R,R enantiomer of 5,11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol (THC) exerts
opposite effects on the transcriptional activity of the two estrogen receptor (ER) subtypes, …

We report on the identification of novel, nonsteroidal ligands that show pronounced subtype-selective
differences in ligand binding and transcriptional potency or efficacy for the two …

Proteases of the malaria parasite Plasmodium falciparum have long been investigated as
drug targets. The P. falciparum genome encodes 10 aspartic proteases called plasmepsins, …

A new class of potent kinase inhibitors selective for mitogen-activated protein kinase-activated
protein kinase 2 (MAPKAP-K2 or MK-2) for the treatment of rheumatoid arthritis has been …

Activation of the p38 kinase pathway in immune cells leads to the transcriptional and
translational regulation of proinflammatory cytokines. Mitogen-activated protein kinase-activated …

A structure–activity relationship study was conducted on a series of tetrahydro-β-carboline-1-carboxylic
acid analogs in order to identify the key functionality responsible for activity …

Nucleos(t)ide analog therapy blocks DNA synthesis by the hepatitis B virus (HBV) reverse
transcriptase and can control the infection, but treatment is life-long and has high costs and …

Hepatitis B virus (HBV) remains a major human pathogen despite the development of both
antiviral drugs and a vaccine, in part because the current therapies do not suppress HBV …

We have discovered a novel class of nonsteroidal pyrazoline antagonists of the
mineralocorticoid receptor (MR) that show excellent potency and selectivity against other nuclear …