New small molecule agonists to the thyrotropin receptor.

PubWeight™: 0.82‹?›

🔗 View Article (PMID 25333622)

Published in Thyroid on January 01, 2015

Authors

Rauf Latif1, M Rejwan Ali, Risheng Ma, Martine David, Syed A Morshed, Michael Ohlmeyer, Dan P Felsenfeld, Zerlina Lau, Mihaly Mezei, Terry F Davies

Author Affiliations

1: 1 Thyroid Research Unit, Department of Medicine, Icahn School of Medicine at Mount Sinai and the James J. Peters VA Medical Center , New York, New York.

Articles cited by this

VMD: visual molecular dynamics. J Mol Graph (1996) 117.02

A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. J Biomol Screen (1999) 32.67

Crystal structure of rhodopsin: A G protein-coupled receptor. Science (2000) 28.60

Development and testing of a general amber force field. J Comput Chem (2004) 23.29

Automatic atom type and bond type perception in molecular mechanical calculations. J Mol Graph Model (2006) 7.93

High-throughput screening assays for the identification of chemical probes. Nat Chem Biol (2007) 4.50

TSH is a negative regulator of skeletal remodeling. Cell (2003) 4.34

Bioluminescent assays for high-throughput screening. Assay Drug Dev Technol (2007) 2.90

Thyroid-stimulating immunoglobulins in Graves' disease. Lancet (1974) 2.84

The thyrotropin (TSH) receptor: interaction with TSH and autoantibodies. Endocr Rev (1998) 2.43

Comparison of administration of recombinant human thyrotropin with withdrawal of thyroid hormone for radioactive iodine scanning in patients with thyroid carcinoma. N Engl J Med (1997) 2.20

Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. Trends Pharmacol Sci (2007) 2.10

Is diagnostic iodine-131 scanning with recombinant human TSH useful in the follow-up of differentiated thyroid cancer after thyroid ablation? J Clin Endocrinol Metab (2002) 1.91

Thyrotropin receptor-associated diseases: from adenomata to Graves disease. J Clin Invest (2005) 1.86

Restructuring G-protein- coupled receptor activation. Cell (2012) 1.83

Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns. J Med Chem (2006) 1.71

Crystal structure of the TSH receptor in complex with a thyroid-stimulating autoantibody. Thyroid (2007) 1.64

Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice. Proc Natl Acad Sci U S A (2009) 1.61

The TSH receptor reveals itself. J Clin Invest (2002) 1.42

Role of the thyroid-stimulating hormone receptor signaling in development and differentiation of the thyroid gland. Proc Natl Acad Sci U S A (2002) 1.41

A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR). J Biol Chem (2006) 1.38

Structure of follicle-stimulating hormone in complex with the entire ectodomain of its receptor. Proc Natl Acad Sci U S A (2012) 1.37

Characterization of thyrotropin receptor antibody-induced signaling cascades. Endocrinology (2008) 1.37

A conserved Asn in transmembrane helix 7 is an on/off switch in the activation of the thyrotropin receptor. J Biol Chem (2001) 1.29

Simulaid: a simulation facilitator and analysis program. J Comput Chem (2010) 1.21

The thyrotropin receptor hinge region is not simply a scaffold for the leucine-rich domain but contributes to ligand binding and signal transduction. Mol Endocrinol (2008) 1.21

Thyrotropin-luteinizing hormone/chorionic gonadotropin receptor extracellular domain chimeras as probes for thyrotropin receptor function. Proc Natl Acad Sci U S A (1991) 1.15

Thyrocyte-specific Gq/G11 deficiency impairs thyroid function and prevents goiter development. J Clin Invest (2007) 1.15

Neutral antibodies to the TSH receptor are present in Graves' disease and regulate selective signaling cascades. Endocrinology (2010) 1.08

The human thyrotropin receptor activates G-proteins Gs and Gq/11. J Biol Chem (1994) 1.07

Prediction of protein loop structures using a local move Monte Carlo approach and a grid-based force field. Protein Eng Des Sel (2008) 1.06

Luciferase Reporter Assay System for Deciphering GPCR Pathways. Curr Chem Genomics (2010) 1.05

Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor. Br J Pharmacol (2012) 1.04

Extended hormone binding site of the human thyroid stimulating hormone receptor: distinctive acidic residues in the hinge region are involved in bovine thyroid stimulating hormone binding and receptor activation. J Biol Chem (2008) 1.03

A drug-like antagonist inhibits thyrotropin receptor-mediated stimulation of cAMP production in Graves' orbital fibroblasts. Thyroid (2012) 1.00

Novel insights on thyroid-stimulating hormone receptor signal transduction. Endocr Rev (2013) 0.97

Tissue-specific knockout of TSHr in white adipose tissue increases adipocyte size and decreases TSH-induced lipolysis. Biochem Biophys Res Commun (2010) 0.96

TSH Receptor Mutations and Thyroid Disease. Trends Endocrinol Metab (2008) 0.96

Update in TSH receptor agonists and antagonists. J Clin Endocrinol Metab (2012) 0.95

Signaling-sensitive amino acids surround the allosteric ligand binding site of the thyrotropin receptor. FASEB J (2010) 0.94

TSH receptor monoclonal antibodies with agonist, antagonist, and inverse agonist activities. Methods Enzymol (2010) 0.90

Characterization of the thyrotropin binding pocket. Thyroid (2002) 0.90

Dockres: a computer program that analyzes the output of virtual screening of small molecules. Source Code Biol Med (2010) 0.89

TSH receptor expression in orbital tissue and its role in the pathogenesis of Graves' ophthalmopathy. J Endocrinol Invest (2004) 0.88

How one TSH receptor antibody induces thyrocyte proliferation while another induces apoptosis. J Autoimmun (2013) 0.87

Mutations that silence constitutive signaling activity in the allosteric ligand-binding site of the thyrotropin receptor. Cell Mol Life Sci (2010) 0.86

A selective TSH receptor antagonist inhibits stimulation of thyroid function in female mice. Endocrinology (2013) 0.86

Extended and structurally supported insights into extracellular hormone binding, signal transduction and organization of the thyrotropin receptor. PLoS One (2012) 0.86

From molecular details of the interplay between transmembrane helices of the thyrotropin receptor to general aspects of signal transduction in family a G-protein-coupled receptors (GPCRs). J Biol Chem (2011) 0.86

Monomerization as a prerequisite for intramolecular cleavage and shedding of the thyrotropin receptor. Endocrinology (2004) 0.84

Small molecule TSHR agonists and antagonists. Ann Endocrinol (Paris) (2011) 0.84

Molecular sampling of the allosteric binding pocket of the TSH receptor provides discriminative pharmacophores for antagonist and agonists. Biochem Soc Trans (2013) 0.82

The thyrotropin receptor hinge region as a surrogate ligand: identification of loci contributing to the coupling of thyrotropin binding and receptor activation. Endocrinology (2012) 0.81

Allosteric modulators hit the TSH receptor. Endocrinology (2014) 0.80

Antibody protection reveals extended epitopes on the human TSH receptor. PLoS One (2012) 0.79

Monte Carlo loop refinement and virtual screening of the thyroid-stimulating hormone receptor transmembrane domain. J Biomol Struct Dyn (2014) 0.78

Articles by these authors

TSH is a negative regulator of skeletal remodeling. Cell (2003) 4.34

Searching for the autoimmune thyroid disease susceptibility genes: from gene mapping to gene function. Endocr Rev (2003) 1.85

Thyrotrophin receptor signaling dependence of Braf-induced thyroid tumor initiation in mice. Proc Natl Acad Sci U S A (2011) 1.82

The thyroid and pregnancy: a novel risk factor for very preterm delivery. Thyroid (2005) 1.82

Hyperthyroid-associated osteoporosis is exacerbated by the loss of TSH signaling. J Clin Invest (2012) 1.77

Thyroid-stimulating hormone induces a Wnt-dependent, feed-forward loop for osteoblastogenesis in embryonic stem cell cultures. Proc Natl Acad Sci U S A (2011) 1.67

Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition. J Biol Chem (2012) 1.66

Common and unique susceptibility loci in Graves and Hashimoto diseases: results of whole-genome screening in a data set of 102 multiplex families. Am J Hum Genet (2003) 1.59

Molecular docking: a powerful approach for structure-based drug discovery. Curr Comput Aided Drug Des (2011) 1.53

A novel method reveals that solvent water favors polyproline II over beta-strand conformation in peptides and unfolded proteins: conditional hydrophobic accessible surface area (CHASA). Protein Sci (2004) 1.52

Intermittent recombinant TSH injections prevent ovariectomy-induced bone loss. Proc Natl Acad Sci U S A (2008) 1.46

A comparison of short-term changes in health-related quality of life in thyroid carcinoma patients undergoing diagnostic evaluation with recombinant human thyrotropin compared with thyroid hormone withdrawal. J Clin Endocrinol Metab (2006) 1.45

BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy. Cancer Res (2013) 1.43

Ord-Hashimoto's disease: renaming a common disorder--again. Thyroid (2003) 1.41

Characterization of thyrotropin receptor antibody-induced signaling cascades. Endocrinology (2008) 1.37

Directed differentiation of mouse embryonic stem cells into thyroid follicular cells. Endocrinology (2006) 1.35

Severe anemia in the Nan mutant mouse caused by sequence-selective disruption of erythroid Kruppel-like factor. Proc Natl Acad Sci U S A (2010) 1.34

Ankyrin binding mediates L1CAM interactions with static components of the cytoskeleton and inhibits retrograde movement of L1CAM on the cell surface. J Cell Biol (2003) 1.30

TNFalpha mediates the skeletal effects of thyroid-stimulating hormone. Proc Natl Acad Sci U S A (2006) 1.27

Activating autoantibodies to the beta-1 adrenergic and m2 muscarinic receptors facilitate atrial fibrillation in patients with Graves' hyperthyroidism. J Am Coll Cardiol (2009) 1.26

Committing embryonic stem cells to differentiate into thyrocyte-like cells in vitro. Endocrinology (2003) 1.25

Unfolded state of polyalanine is a segmented polyproline II helix. Proteins (2004) 1.25

A monoclonal thyroid-stimulating antibody. J Clin Invest (2002) 1.22

Dissecting genetic heterogeneity in autoimmune thyroid diseases by subset analysis. J Autoimmun (2007) 1.18

Thyroglobulin is a thyroid specific gene for the familial autoimmune thyroid diseases. J Clin Endocrinol Metab (2002) 1.17

Ligand-dependent inhibition of oligomerization at the human thyrotropin receptor. J Biol Chem (2002) 1.16

Possible interaction between HLA-DRbeta1 and thyroglobulin variants in Graves' disease. Thyroid (2006) 1.15

Thyrotropin-independent induction of thyroid endoderm from embryonic stem cells by activin A. Endocrinology (2008) 1.14

TSH and bone loss. Ann N Y Acad Sci (2006) 1.12

A molecular dynamics investigation of lipid bilayer perturbation by PIP2. Biophys J (2010) 1.12

American Thyroid Association statement on optimal surgical management of goiter. Thyroid (2014) 1.11

The thyroid-stimulating hormone receptor: impact of thyroid-stimulating hormone and thyroid-stimulating hormone receptor antibodies on multimerization, cleavage, and signaling. Endocrinol Metab Clin North Am (2009) 1.08

Neutral antibodies to the TSH receptor are present in Graves' disease and regulate selective signaling cascades. Endocrinology (2010) 1.08

TSH receptor autoantibodies. Autoimmun Rev (2009) 1.08

Molecular amino acid signatures in the MHC class II peptide-binding pocket predispose to autoimmune thyroiditis in humans and in mice. Proc Natl Acad Sci U S A (2008) 1.08

The influence of human leucocyte antigen (HLA) genes on autoimmune thyroid disease (AITD): results of studies in HLA-DR3 positive AITD families. Clin Endocrinol (Oxf) (2002) 1.07

Prediction of protein loop structures using a local move Monte Carlo approach and a grid-based force field. Protein Eng Des Sel (2008) 1.06

Autoimmune thyroid disease in pregnancy: a review. J Womens Health (Larchmt) (2009) 1.05

Intrathyroidal fetal microchimerism in Graves' disease. J Clin Endocrinol Metab (2002) 1.04

Targeting the FOXO1/KLF6 axis regulates EGFR signaling and treatment response. J Clin Invest (2012) 1.04

An animal model of Tourette's syndrome. Am J Psychiatry (2002) 1.04

Blocking antibody to the β-subunit of FSH prevents bone loss by inhibiting bone resorption and stimulating bone synthesis. Proc Natl Acad Sci U S A (2012) 1.04

MAP kinase pathway-dependent phosphorylation of the L1-CAM ankyrin binding site regulates neuronal growth. Mol Biol Cell (2006) 1.03

A multilocus model of the genetic architecture of autoimmune thyroid disorder, with clinical implications. Am J Hum Genet (2008) 1.03

Retarded developmental expression and patterning of retinal cone opsins in hypothyroid mice. Endocrinology (2008) 1.03

Selective functional inhibition of JAK-3 is sufficient for efficacy in collagen-induced arthritis in mice. Arthritis Rheum (2010) 1.03

Fine mapping of loci linked to autoimmune thyroid disease identifies novel susceptibility genes. J Clin Endocrinol Metab (2012) 1.01

Analysis of HLA genes in families with autoimmune diabetes and thyroiditis. Hum Immunol (2004) 1.01

Retracted G protein-induced trafficking of voltage-dependent calcium channels. J Biol Chem (2005) 1.00

Thyroid-stimulating hormone, thyroid hormones, and bone loss. Curr Osteoporos Rep (2009) 1.00

Skeletal receptors for steroid-family regulating glycoprotein hormones: A multilevel, integrated physiological control system. Ann N Y Acad Sci (2011) 1.00

Thyroid epigenetics: X chromosome inactivation in patients with autoimmune thyroid disease. Ann N Y Acad Sci (2007) 1.00

Interactions between the L1 cell adhesion molecule and ezrin support traction-force generation and can be regulated by tyrosine phosphorylation. J Neurosci Res (2008) 0.98

Influence of the TSH receptor gene on susceptibility to Graves' disease and Graves' ophthalmopathy. Thyroid (2008) 0.98

'Linkage analysis of thyroid antibody production: evidence for shared susceptibility to clinical autoimmune thyroid disease. J Clin Endocrinol Metab (2008) 0.97

A C/T single nucleotide polymorphism at the tyrosine kinase domain of the insulin receptor gene is associated with polycystic ovary syndrome. Fertil Steril (2002) 0.96

The ABCs of molecular dynamics simulations on B-DNA, circa 2012. J Biosci (2012) 0.96

Calculation of the free energy and cooperativity of protein folding. PLoS One (2007) 0.96

The influence of thyroid-stimulating hormone and thyroid-stimulating hormone receptor antibodies on osteoclastogenesis. Thyroid (2011) 0.95

Clinical Review 160: Postpartum autoimmune thyroid disease: the potential role of fetal microchimerism. J Clin Endocrinol Metab (2003) 0.95

Mechanism of PLC-mediated Kir3 current inhibition. Channels (Austin) (2007) 0.94

Thyroid follicle formation and thyroglobulin expression in multipotent endodermal stem cells. Thyroid (2013) 0.94

The eventual pain and joy of grant writing. Thyroid (2005) 0.93

Association free energy of dipalmitoylphosphatidylserines in a mixed dipalmitoylphosphatidylcholine membrane. Biophys J (2007) 0.93

Computer aided identification of small molecules disrupting uPAR/alpha5beta1--integrin interaction: a new paradigm for metastasis prevention. PLoS One (2009) 0.93

Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J Med Chem (2013) 0.93

Analysis of immune regulatory genes in familial and sporadic Graves' disease. J Clin Endocrinol Metab (2004) 0.92

Delineating the autoimmune mechanisms in Graves' disease. Immunol Res (2012) 0.92

Structure-guided optimization of small molecules inhibiting human immunodeficiency virus 1 Tat association with the human coactivator p300/CREB binding protein-associated factor. J Med Chem (2007) 0.92

CCR7 deficiency in NOD mice leads to thyroiditis and primary hypothyroidism. J Immunol (2009) 0.92

Clinical review: The emerging cell biology of thyroid stem cells. J Clin Endocrinol Metab (2011) 0.92

Induction of thyroid-stimulating hormone receptor autoimmunity in hamsters. Endocrinology (2003) 0.91

Stemness in human thyroid cancers and derived cell lines: the role of asymmetrically dividing cancer stem cells resistant to chemotherapy. J Clin Endocrinol Metab (2014) 0.91

Estrogenic activity and estrogen receptor beta binding of the UV filter 3-benzylidene camphor. Comparison with 4-methylbenzylidene camphor. Toxicology (2004) 0.91

Homology modeling and site-directed mutagenesis to identify selective inhibitors of endothelin-converting enzyme-2. J Med Chem (2008) 0.90

E6a2 BCR-ABL fusion with BCR exon 5-deleted transcript in a Philadelphia positive CML responsive to Imatinib. Leuk Lymphoma (2005) 0.90

Derivation and characterization of thyrocyte-like cells from embryonic stem cells in vitro. Methods Mol Biol (2006) 0.90

Bone loss in thyroid disease: role of low TSH and high thyroid hormone. Ann N Y Acad Sci (2007) 0.89

Dissecting linear and conformational epitopes on the native thyrotropin receptor. Endocrinology (2004) 0.89

Concentration-dependent regulation of thyrotropin receptor function by thyroid-stimulating antibody. J Clin Invest (2004) 0.89

Genetic profiling in Graves' disease: further evidence for lack of a distinct genetic contribution to Graves' ophthalmopathy. Thyroid (2012) 0.89

Human embryonic stem cells form functional thyroid follicles. Thyroid (2015) 0.88

Human uroporphyrinogen III synthase: NMR-based mapping of the active site. Proteins (2008) 0.88

How one TSH receptor antibody induces thyrocyte proliferation while another induces apoptosis. J Autoimmun (2013) 0.87

Really significant genes for autoimmune thyroid disease do not exist--so how can we predict disease? Thyroid (2007) 0.87

Interlaboratory comparison of four in vitro assays for assessing androgenic and antiandrogenic activity of environmental chemicals. Environ Health Perspect (2004) 0.87

Thyrotropin receptor knockout mice: studies on immunological tolerance to a major thyroid autoantigen. Endocrinology (2003) 0.87

Thyroid autoantibodies in pregnancy: their role, regulation and clinical relevance. J Thyroid Res (2013) 0.86

Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor. J Pharmacol Exp Ther (2009) 0.86

Time for the American Thyroid Association to lead on thyroid screening in pregnancy. Thyroid (2007) 0.86

Studies of base pair sequence effects on DNA solvation based on all-atom molecular dynamics simulations. J Biosci (2012) 0.86

A tyrosine residue on the TSH receptor stabilizes multimer formation. PLoS One (2010) 0.85

mRNA-Seq reveals novel molecular mechanisms and a robust fingerprint in Graves' disease. J Clin Endocrinol Metab (2014) 0.85

Lucanthone and its derivative hycanthone inhibit apurinic endonuclease-1 (APE1) by direct protein binding. PLoS One (2011) 0.85