Current lipid-altering agents that lower low density lipoprotein cholesterol (LDL-C) primarily through increased hepatic LDL receptor activity include statins, bile acid sequestrants/resins and cholesterol absorption inhibitors such as ezetimibe, plant stanols/sterols, polyphenols, as well as nutraceuticals such as oat bran, psyllium and soy proteins; those currently in development include newe...

INTRODUCTION The introduction of tumor necrosis factor-alpha (TNF-alpha) inhibitors represented a significant advance in the management of rheumatoid arthritis (RA) and other chronic inflammatory diseases. Although three TNF-alpha inhibitors have been approved for the treatment of RA by the US Food and Drug Administration (FDA) and the European Medicinal Products Evaluation Agency (EMEA), not a...

Chronic inflammation is implicated in the pathophysiology of ovarian cancer. Tumor necrosis factor-alpha (TNF-alpha), a major inflammatory cytokine, is abundant in the ovarian cancer microenvironment. TNF-alpha modulates the expression of CD44 in normal T lymphocytes and CD44 is implicated in ovarian carcinogenesis and metastases. However, little is known about the role of TNF-alpha in CD44 exp...

Stromal cell-derived factor 1 alpha (SDF1 alpha) and its cognate chemokine receptor CXCR4 act as potent chemoattractants and regulate trafficking and homing of hematopoietic progenitor cells and lymphocytes. However, the molecular mechanisms regulating SDF1 alpha-driven cell migration are not well defined. In this study, we have explored the roles of the second messenger NO and the transcriptio...

Mutation of the conserved leucine residue, in the second transmembrane domain of the neuronal alpha7 acetylcholine receptor to a threonine (L247T) causes pleiotropic alterations of receptor properties. In this study we examined the effects of competitive inhibitors on the alpha7-L247T physiological responses. While the alpha7 competitive inhibitor dihydro-beta-erythroidine evoked a current comp...

The medical and surgical management of BPH/ LUTS can affect erectile function (EF), cause ejaculatory dysfunction (EjD) or affect libido. Five alpha reductase inhibitors, such as finasteride and dutasteride have good efficacy for benign prostatic hyperplasia, however they have also sexual side effects including loss of libido, erectile dysfunction and decreased ejaculatory volume. Also, alpha a...

Peripherally active anorectic agents represent a new approach to the pharmacological management of obesity. Two inhibitors of carbohydrate absorption: an alpha-glucosidase inhibitor, acarbose (Bay g 5421) and a alpha-amylase inhibitor, Ro 12-2272, were compared with two novel inhibitors of lipid metabolism: an inhibitor of human pancreatic lipase (Ro 20-0083) and of hepatic fatty acid synthesis...

Integration is a crucial step in the life cycle of human immunodeficiency virus type 1 (HIV-1); therefore, inhibitors of HIV-1 integrase are candidates for antiretroviral therapy. Two 7-hydroxytropolone derivatives (alpha-hydroxytropolones) were found to inhibit HIV-1 integrase. A structure-activity relationship investigation with several tropolone derivatives from The National Cancer Institute...

The medical and surgical management of BPH/ LUTS can affect erectile function (EF), cause ejaculatory dysfunction (EjD) or affect libido. Five alpha reductase inhibitors, such as finasteride and dutasteride have good efficacy for benign prostatic hyperplasia, however they have also sexual side effects including loss of libido, erectile dysfunction and decreased ejaculatory volume. Also, alpha a...