Biomedical subjects

Dennis Heyer

Publications and source records attributed to Dennis Heyer.

3 recordsLinked to original sources

PubMed2005

Recent advances in estrogen receptor modulators.

Modulation of estrogen action is an effective treatment for alleviating the symptoms associated with menopause, and also provides an alternative to ablative surgery for the treatment of breast cancer. The side effects associated with the currently used estrogen receptor-modulating drugs have resulted in the pursuit of agents with an improved therapeutic profile. Recent advances in understanding the molecular determinants of estrogen receptor signaling have contributed to the continued discovery and development of novel chemical compounds designed to exploit this knowledge. This review focuses on the recent clinical and preclinical development of novel classes of ligands that modulate the two estrogen receptor subtypes.

Animals↗

PubMed2004

Synthesis and structure activity relationship of guanidines as NPY Y5 antagonists.

A series of bis-aryl substituted guanidines have been discovered as potent NPY Y5 antagonists. The SAR and in vitro metabolic stability of these compounds are discussed.

Animals↗

PubMedDate not supplied

High-throughput manual parallel synthesis using SynPhase crowns and lanterns.

The high-throughput manual solid-phase parallel synthesis of libraries comprising thousands of discrete samples using pellicular supports (i.e. SynPhase crowns and lanterns) and a suite of novel tools and techniques is described. Key aspects of this approach include the combination of a split-split-split synthesis strategy with spatial encoding to differentiate thousands of crowns, the rapid washing and filtration of up to 48 reaction vessels in parallel, the application of an inexpensive and environmentally friendly technique to remove trifluoroacetic acid from sixteen 96-well plates in parallel, and a high-throughput method for removing cleaved crowns from reusable pin racks. Tens of thousands of discrete samples have been produced in-house using this conceptually and operationally straightforward strategy.

Journal Article↗