Current Topics in Medicinal Chemistry - Volume 8, Issue 16, 2008

Pain is defined as an unpleasant sensory and emotional experience associated with actual or potential tissue damage. It is a frequent reason for physician consultation, and a major symptom in many medical conditions, significantly interfering with a person's quality of life and general functioning. Inflammation is the sequence of events that characterizes the biological response of vascular tissues to harmful stimuli. It is Read More

Bradykinin B1 receptor antagonists embody a potentially novel approach for the treatment of chronic pain and inflammation. The identification of non-peptide B1 antagonists has been a notable advance in the kinin field that will allow evaluation of their therapeutic potential in the clinical realm. The current review is a high level summary of our contributions to the area that culminated in the discovery of a clinical candidate.

As last year marked the tenth anniversary of the cloning of TRPV1, no attenuation has been observed in the intense interest surrounding this ion channel by both academic labs and pharmaceutical companies alike. Patent searches provide an extensive list of novel TRPV1 antagonists generated within the last 7 years, while literature searches reveal a diverse collection of TRPV1 antagonists that have progressed into pr Read More

Following the cloning of the classical opioid receptors (μ, δ and κ), the opioid receptor like-1 (ORL-1) was identified as a G-protein coupled receptor (GPCR) with 65% structure homology to the other members of the opioid family. Its endogenous ligand nociception/orphanin FQ (N/OFQ) was discovered shortly thereafter, becoming the subject of investigation in numerous studies. Since activation of the ORL-1 receptor by N/OF Read More

The p38 mitogen-activated protein (MAP) kinase plays a central role in inflammation. It has been the subject of extensive efforts in both basic research and drug discovery for the treatment of inflammatory diseases such as rheumatoid arthritis, inflammatory bowel disease, and psoriasis, where aberrant cytokine signaling is the driver of the disease. This article reviews the patent and journal publication activities during 200 Read More

The critical role of Calcitonin Gene-Related Peptide (CGRP) in migraine has been validated, with two small molecule CGRP antagonists BIBN4096BS and MK-0974 demonstrating efficacy in the reversal of acute migraine attack [1,2]. Multiple approaches have been taken to find the ideal agent that most effectively inhibits CGRP's function. Here, we have summarized the progress made in recent years, including the identification and Read More

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