A Novel Treatment for Metastatic Prostate Cancer

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Ieva Sutkeviciute

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Small Molecule Allosteric Modulators of Class B GPCRs in the PTHR and Method to Identify Them

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A structure-guided computational approach was used to identify allosteric druggable sites in PTHR and to predict compounds that would bind to this site, and Pitt researchers discovered four small-molecule compounds that act as negative allosteric modulators of PTHR signaling.

Parathyroid hormone (PTH) type 1 receptor (PTHR) is an indispensable G protein-coupled receptor (GPCR) of class B that functions to regulate blood levels of vitamin D, calcium, and phosphate ions in the body, as well as bone turnover.

A structure-guided computational approach was used to identify allosteric druggable sites in PTHR and to predict compounds that would bind to this site, and Pitt researchers discovered four small-molecule compounds that act as negative allosteric modulators of PTHR signaling.

Therapeutic Modality

Small Molecule

Musculoskeletal Endocrinology and Metabolic Diseases

Bioinformatics Small molecule

Ieva Sutkeviciute

Med-Pharmacology and Chemical Biology

2020-11-19