Diane Gesty-Palmer

Journal Article Br J Pharmacol · September 2011 'Functional selectivity' refers to the ability of a ligand to activate and/or inhibit only a subset of the signals capable of emanating from its cognate G-protein-coupled receptor (GPCR). Whereas conventional GPCR agonism and antagonism can be viewed as mo ... Full text Link to item Cite

Osteoporosis in lung transplant candidates compared to matched healthy controls.

Journal Article Clin Transplant · 2011 PURPOSE: Advanced lung disease increases the risk for diminished bone mineral density (BMD). The prevalence and severity of osteoporosis in lung transplant candidates is unclear. METHODS: We retrospectively evaluated BMD of subjects screened for lung trans ... Full text Link to item Cite

The endogenous selective estrogen receptor modulator 27-hydroxycholesterol is a negative regulator of bone homeostasis.

Journal Article Endocrinology · August 2010 Osteoporosis is an important clinical problem, affecting more than 50% of people over age 50 yr. Estrogen signaling is critical for maintaining proper bone density, and the identification of an endogenous selective estrogen receptor (ER) modulator, 27-hydr ... Full text Link to item Cite

Growth hormone mitigates against lethal irradiation and enhances hematologic and immune recovery in mice and nonhuman primates.

Journal Article PLoS One · June 16, 2010 Medications that can mitigate against radiation injury are limited. In this study, we investigated the ability of recombinant human growth hormone (rhGH) to mitigate against radiation injury in mice and nonhuman primates. BALB/c mice were irradiated with 7 ... Full text Open Access Link to item Cite

Beyond desensitization: physiological relevance of arrestin-dependent signaling.

Journal Article Pharmacol Rev · June 2010 Heptahelical G protein-coupled receptors are the most diverse and therapeutically important family of receptors in the human genome. Ligand binding activates heterotrimeric G proteins that transmit intracellular signals by regulating effector enzymes or io ... Full text Link to item Cite

A beta-arrestin-biased agonist of the parathyroid hormone receptor (PTH1R) promotes bone formation independent of G protein activation.

Journal Article Sci Transl Med · October 7, 2009 About 40% of the therapeutic agents in use today exert their effects through seven-transmembrane receptors (7TMRs). When activated by ligands, these receptors trigger two pathways that independently transduce signals to the cell: one through heterotrimeric ... Full text Link to item Cite

Inhibition of WNT signaling by G protein-coupled receptor (GPCR) kinase 2 (GRK2).

Journal Article Mol Endocrinol · September 2009 Activation of Wnt signaling pathways causes release and stabilization of the transcription regulator beta-catenin from a destruction complex composed of axin and the adenomatous polyposis coli (APC) protein (canonical signaling pathway). Assembly of this c ... Full text Link to item Cite

Distinct conformational changes in beta-arrestin report biased agonism at seven-transmembrane receptors.

Journal Article Proc Natl Acad Sci U S A · July 22, 2008 Beta-arrestins critically regulate G protein-coupled receptors (GPCRs), also known as seven-transmembrane receptors (7TMRs), both by inhibiting classical G protein signaling and by initiating distinct beta-arrestin-mediated signaling. The recent discovery ... Full text Link to item Cite

Heptahelical terpsichory. Who calls the tune?

Journal Article J Recept Signal Transduct Res · 2008 The discovery that arrestins can function as ligand-regulated signaling scaffolds has revealed a previously unappreciated level of complexity in G protein-coupled receptor (GPCR) signal transduction. Because arrestin-bound GPCRs are uncoupled from G protei ... Full text Link to item Cite

Distinct beta-arrestin- and G protein-dependent pathways for parathyroid hormone receptor-stimulated ERK1/2 activation.

Journal Article J Biol Chem · April 21, 2006 Parathyroid hormone (PTH) regulates calcium homeostasis via the type I PTH/PTH-related peptide (PTH/PTHrP) receptor (PTH1R). The purpose of the present study was to identify the contributions of distinct signaling mechanisms to PTH-stimulated activation of ... Full text Link to item Cite

beta-Arrestin 2 expression determines the transcriptional response to lysophosphatidic acid stimulation in murine embryo fibroblasts.

Journal Article J Biol Chem · September 16, 2005 G protein-coupled receptors often employ novel signaling mechanisms, such as transactivation of epidermal growth factor (EGF) receptors or G protein-independent signals transmitted by beta-arrestins, to control the activity of extracellular signal-regulate ... Full text Link to item Cite

Beta-arrestin- and G protein receptor kinase-mediated calcium-sensing receptor desensitization.

Journal Article Mol Endocrinol · April 2005 Extracellular calcium rapidly controls PTH secretion through binding to the G protein-coupled calcium-sensing receptor (CASR) expressed in parathyroid glands. Very little is known about the regulatory proteins involved in desensitization of CASR. G protein ... Full text Link to item Cite

Transactivation of the epidermal growth factor receptor mediates parathyroid hormone and prostaglandin F2 alpha-stimulated mitogen-activated protein kinase activation in cultured transgenic murine osteoblasts.

Journal Article Mol Endocrinol · August 2003 Recent data suggest that G protein-coupled receptors (GPCRs), including those for PTH and prostaglandins (PGs), contribute to the proliferation and differentiation of osteoblasts in vivo. To understand how these signals are transduced, we studied activatio ... Full text Link to item Cite

The stability of the G protein-coupled receptor-beta-arrestin interaction determines the mechanism and functional consequence of ERK activation.

Journal Article J Biol Chem · February 21, 2003 By binding to agonist-activated G protein-coupled receptors (GPCRs), beta-arrestins mediate homologous receptor desensitization and endocytosis via clathrin-coated pits. Recent data suggest that beta-arrestins also contribute to GPCR signaling by acting as ... Full text Link to item Cite