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Biomedical subjects

Gerrit H Veeneman

Publications and source records attributed to Gerrit H Veeneman.

3 recordsLinked to original sources

Non-steroidal steroid receptor modulators.

The discovery and launch of non-steroidal ligands for estrogen receptors (ERs) and for androgen receptors (ARs) demonstrated the potential of these ligands as therapeutic agents. Based on these successes, substantial attention in the past ten years has been focused on identifying non-steroidal ligands for all of the classic steroid receptors. Non-steroidal ligands are currently in the discovery phase or in early clinical development for glucocorticoid, mineralocorticoid and progesterone receptors, and therefore must still provide evidence of their beneficial features over their steroidal counterparts. Although many new compounds for ERs and ARs are also undergoing discovery phase investigation or (early) development, none have been launched in the past ten years. The complexity of steering functional selectivity remains an ongoing challenge in the development on non-steroidal ligands.

Animals↗

Non-steroidal subtype selective estrogens.

The biological effects of estrogens are thought to be mediated by two receptors referred to as ERalpha and ERbeta. In recent years significant efforts have been devoted to the design of subtype selective ligands. These ligands are valuable tools to establish the precise biological role of each of the subtypes and to develop new generations of therapeutics. The first part of this review briefly summarizes the biology behind the estrogen receptors. The second part addresses the structure-activity relationship of the subtype selective ER ligands that were reported up to now. In the third part, the current insights in the therapeutic prospects of the subtype selective estrogens will be discussed.

Estrogens, Non-Steroidal↗

Identification of "latent hits" in compound screening collections.

The relatively low hit rates found from high-throughput screening have raised a question on whether this technology alone is sufficient to maximally exploit the full potential of current corporate screening collections. The present study introduces a knowledge-based strategy for identifying "latent hits", i.e., inactive compounds that could potentially be promoted to hits through simple chemical transformations. Examples are given of submicromolar agonist hits derived from the corresponding latent hits for the estrogen receptor.

Animals↗