A negative allosteric modulator demonstrates biased antagonism of the follicle stimulating hormone receptor

scientific article published on 22 December 2010

A negative allosteric modulator demonstrates biased antagonism of the follicle stimulating hormone receptor is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1016/J.MCE.2010.12.023
P932PMC publication ID4491433
P698PubMed publication ID21184806

P2093author name stringJames A Dias
Kerri Kluetzman
Vincent Mutel
Brice Campo
Sonia Poli
Richard M Thomas
Barbara A Weaver
Béatrice Bonnet
Julie Watts
P2860cites workThree-dimensional structure of human follicle-stimulating hormoneQ24290863
Mutation in the follicle-stimulating hormone receptor gene causes hereditary hypergonadotropic ovarian failureQ24309024
Structure of human follicle-stimulating hormone in complex with its receptorQ24338640
Persistent cAMP-signals triggered by internalized G-protein-coupled receptorsQ27329609
Crystal structure of opsin in its G-protein-interacting conformationQ27652301
Regulation of follitropin receptor cell surface residency by the ubiquitin-proteasome pathwayQ28205312
Multiple signaling pathways regulating steroidogenesis and steroidogenic acute regulatory protein expression: more complicated than we thoughtQ28245222
Allosteric modulation of the cannabinoid CB1 receptorQ28268355
Inhibition of rat granulosa cell differentiation by overexpression of GalphaqQ28566598
The testicular receptor for follicle stimulating hormone: structure and functional expression of cloned cDNAQ28566700
Follicle-stimulating hormone-induced aromatase in immature rat Sertoli cells requires an active phosphatidylinositol 3-kinase pathway and is inhibited via the mitogen-activated protein kinase signaling pathwayQ28567566
A novel follicle-stimulating hormone-induced G alpha h/phospholipase C-delta1 signaling pathway mediating rat sertoli cell Ca2+-influxQ28570933
Follicle stimulating hormone is required for ovarian follicle maturation but not male fertilityQ28586787
LIGAND: A versatile computerized approach for characterization of ligand-binding systemsQ29547346
Agonists of the follicle stimulating hormone receptor from an encoded thiazolidinone libraryQ30011082
Molecular, structural, and cellular biology of follitropin and follitropin receptor.Q30329979
Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesisQ33199694
Small molecule biaryl FSH receptor agonists. Part 2: Lead optimization via parallel synthesisQ33199695
Allosteric activation of the follicle-stimulating hormone (FSH) receptor by selective, nonpeptide agonists.Q33236674
Allosteric modulators of glycoprotein hormone receptors: discovery and therapeutic potentialQ33379828
Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7Q33520184
Partially deglycosylated equine LH preferentially activates beta-arrestin-dependent signaling at the follicle-stimulating hormone receptorQ33735942
Teaching old receptors new tricks: biasing seven-transmembrane receptorsQ33985759
Specificity of the cyclic adenosine 3',5'-monophosphate signal in granulosa cell functionQ35005429
Arrestin development: emerging roles for beta-arrestins in developmental signaling pathwaysQ35565885
Identifying protein interactors in gonadotropin action.Q36202093
New concepts in drug discovery: collateral efficacy and permissive antagonismQ36303814
Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.Q36880915
Multiple facets of follicle-stimulating hormone receptor function.Q37075995
Allosteric modulation of G protein-coupled receptors: a pharmacological perspective.Q37773544
Truncated equine LH beta and asparagine(56)-deglycosylated equine LH alpha combine to produce a potent FSH antagonistQ38291558
Regulation of ovarian steroidogenesis. The disparity between 125I-labelled choriogonadotropin binding cyclic adenosine 3',5'-monophosphate formation and progesterone synthesis in the rat ovaryQ40006304
Discovery of new molecules for future treatment of infertilityQ40419015
Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptorQ40446049
Protein kinase A-dependent cooperation between GATA and CCAAT/enhancer-binding protein transcription factors regulates steroidogenic acute regulatory protein promoter activityQ40703114
Human follicle stimulating hormone receptor trafficking and hormone binding sites in the amino terminusQ40853913
Hormone-induced conformational change of the purified soluble hormone binding domain of follitropin receptor complexed with single chain follitropinQ42054329
Adenovirus-directed expression of functional luteinizing hormone (LH) receptors in undifferentiated rat granulosa cells: evidence for differential signaling through follicle-stimulating hormone and LH receptorsQ42504409
The carboxyl terminus of the Galpha-subunit is the latch for triggered activation of heterotrimeric G proteinsQ42670035
Protein kinase B is obligatory for follicle-stimulating hormone-induced granulosa cell differentiationQ44559307
Pregnancy rates in varying age groups after in vitro fertilization: a comparison of follitropin alfa (Gonal F) and follitropin beta (Follistim)Q44603368
Sequence of interactions in receptor-G protein coupling.Q44790638
Analysis of allosterism in functional assaysQ46171612
Differing pharmacological activities of thiazolidinone analogs at the FSH receptorQ46770432
A comparison of the efficacy and tolerability of two recombinant human follicle-stimulating hormone preparations in patients undergoing in vitro fertilization-embryo transferQ48901697
Ovarian response to follicle-stimulating hormone (FSH) stimulation depends on the FSH receptor genotype.Q50723296
D-myo-inositol 1-phosphate as a surrogate of D-myo-inositol 1,4,5-tris phosphate to monitor G protein-coupled receptor activation.Q51804080
Operational models of pharmacological agonism.Q52699226
Steroid and plasminogen activator production by cultured rat granulosa cells in response to hormone treatmentQ71538047
Recombinant follicle-stimulating hormone (FSH; Puregon) is more efficient than urinary FSH (Metrodin) in women with clomiphene citrate-resistant, normogonadotropic, chronic anovulation: a prospective, multicenter, assessor-blind, randomized, clinicaQ74150197
P433issue2
P407language of work or nameEnglishQ1860
P304page(s)143-150
P577publication date2010-12-22
P1433published inMolecular and Cellular EndocrinologyQ1573600
P1476titleA negative allosteric modulator demonstrates biased antagonism of the follicle stimulating hormone receptor
P478volume333

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cites work (P2860)
Q37012088An Investigation on a Novel Anti-tumor Fusion Peptide of FSH33-53-IIKK.
Q64097803Biased Signaling and Allosteric Modulation at the FSHR
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Q26781438Discovery and Development of Small Molecule Allosteric Modulators of Glycoprotein Hormone Receptors
Q27682749Evidence for Follicle-stimulating Hormone Receptor as a Functional Trimer
Q90694637FSH for the Treatment of Male Infertility
Q60956605FSHR Trans-Activation and Oligomerization
Q92283308Follicle-Stimulating Hormone Glycobiology
Q37077742In Vitro Effects of the Endocrine Disruptor p,p'-DDT on Human Follitropin Receptor.
Q55365511In Vivo and In Vitro Impact of Carbohydrate Variation on Human Follicle-Stimulating Hormone Function.
Q35618348Inhibition of follicle-stimulating hormone-induced preovulatory follicles in rats treated with a nonsteroidal negative allosteric modulator of follicle-stimulating hormone receptor
Q35999305Mapping the follicle-stimulating hormone-induced signaling networks
Q41088748Modulation of the steroidogenic related activity according to the design of single-chain bovine FSH analogs
Q36773326Molecular mechanism of β-arrestin-biased agonism at seven-transmembrane receptors
Q37869835Novel pathways in gonadotropin receptor signaling and biased agonism.
Q35287319Pharmacological characterization of mGlu1 receptors in cerebellar granule cells reveals biased agonism.
Q37183072Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors
Q61811038Small Molecule Follicle-Stimulating Hormone Receptor Agonists and Antagonists
Q38887428The Follitropin Receptor: Matching Structure and Function
Q38003528The follicle-stimulating hormone receptor: a novel target in genitourinary malignancies

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