• Although a number of studies have shown that patients with activating mutations in exons 18-21 of the epidermal growth factor receptor (EGFR) gene respond particularly well to gefitinib and erlotinib, a prospective, randomised study was needed to differentiate between the prognostic and predictive value of EGFR mutations. (ersjournals.com)
  • Clinically relevant improvements in survival have been attained by administering targeted therapy to the appropriate patient population: for example, the addition of trastuzumab to standard first-line chemotherapy in patients with human epidermal growth factor receptor-positive (HER2+) metastatic breast cancer 3 . (ersjournals.com)
  • This review considers the current evidence linking biomarker profile to efficacy of epidermal growth factor receptor (EGFR)-targeted therapy in advanced nonsmall cell lung cancer (NSCLC) and the clinical implications of recent findings. (ersjournals.com)
  • The present study evaluated the prognostic value of the epidermal growth factor receptor (EGFR) mutation status, and excision repair cross-complementation group 1 (ERCC1) and thymidylate synthase (TS) expression following intercalated tyrosine kinase inhibitor (TKI) therapy and platinum- and pemetrexed-based chemotherapies (subsequent second-line treatment) for patients with adenocarcinoma non-small-cell lung cancer (AC-NSCLC). (medsci.org)
  • The standard therapies for lung adenocarcinoma include epidermal growth factor receptor (EGFR) mutation targeted therapy and conventional chemotherapy, such as platinum- and pemetrexed-based chemotherapies. (medsci.org)
  • Amplification of the human epidermal growth factor receptor 2 ( HER2 ) gene and overexpression of the HER2 protein is found in 15%-20% of patients with gastric and gastroesophageal junction cancer. (wjgnet.com)
  • While ligands for many receptors are still not known, researchers are utilizing drug libraries to investigate compounds that can activate GPCRs and using these data for future ligand research. (wikipedia.org)
  • The advent of functional screening assays allowed the identification of ligands, such as 77-LH-28-1, which bound to an allosteric site and selectively activated the M1 mAChR (1). (unicam.it)
  • Receptor proteins have specific sites into which certain other proteins, called ligands, fit like keys into locks. (medlineplus.gov)
  • Together, ligands and their receptors trigger signals that affect cell development and function. (medlineplus.gov)
  • The protein produced from the LHCGR gene acts as a receptor for two ligands: luteinizing hormone and a similar hormone called chorionic gonadotropin. (medlineplus.gov)
  • The GDNF family ligands (GFLs) function through a glycosyl-phosphatidylinositol-(GPI) anchored coreceptor, GDNF family receptor alpha (GFRα), and rearranged during transfection (RET), a well-known receptor tyrosine kinase involved in kidney development, spermatogonial stem cell maintenance, and the development and maintenance of the sympathetic, parasympathetic, and enteric nervous systems [ 1 , 2 ]. (medsci.org)
  • Although these receptors are structurally similar, they determine specificity for four ligands-GDNF, Neurturin (NRTN), Artemin (ARTN) and Persephin (PSPN). (medsci.org)
  • The biosensor makes use of a yeast organism that is genetically engineered with the sequences needed to express estrogen and LH receptors and the attached color-producing ligands. (diwou.com)
  • Developing computational methods to relate receptors by the similarity of their ligands, rather than by protein sequence or structure. (ucsf.edu)
  • Since the new relationships are articulated by ligands, they may be directly tested both on isolated receptors and, increasingly, against model whole organisms, such as zebra fish, C. elegans and mice. (ucsf.edu)
  • The hormonal activation occurs through specific ligand-receptor interactions on the surface of the target cells. (biomedcentral.com)
  • A different experimental approach by West and Cooke [ 10 ] demonstrated the secretion of M r 80-90K hCG-LH receptor complex into the culture media from ligand-induced rat and mouse leydig cells. (biomedcentral.com)
  • instead, a specific intra-cellular role of truncated receptor in regulating the cell surface expression of a full-length ligand-binding Lhcgr has been proposed [ 15 ]. (biomedcentral.com)
  • The addition of antibodies that precipitate hCG did not affect the activity of LH receptor ligand molecules in serum samples collected during the early luteal phase of conceptive cycles, as measured by bioassay. (nih.gov)
  • M-type phospholipase A2 receptor as target antigen in idiopathic membranous nephropathy. (bu.edu)
  • The M-type phospholipase A2 receptor (PLA2R) in the glomerular podocyte has been identified as the major target antigen in deposited immune-complexes. (msdmanuals.com)
  • The action of BDNF on CB 1 R (GABA) function was tyrosine kinase dependent and was complete even after receptor sensitization with cocaine or environmental manipulations activating the dopamine (DA)-dependent reward system. (jneurosci.org)
  • In addition, one of the direct targets of miR-31 was found to be receptor tyrosine kinase MET, and upregulation of MET caused the chemoresistance to PTX. (nature.com)
  • In mice lacking one copy of the BDNF gene ( BDNF +/− ), CB 1 R (GABA) responses were potentiated and were preserved from the action of haloperidol, a DA D 2 receptor (D 2 R) antagonist able to fully abolish CB 1 R (GABA) function in rewarded animals. (jneurosci.org)
  • Current concepts of follicle-stimulating hormone receptor gene regulation. (ac.ir)
  • The LHCGR gene provides instructions for making a protein called the luteinizing hormone/chorionic gonadotropin receptor. (medlineplus.gov)
  • The LHCGR gene mutations that cause Leydig cell hypoplasia disrupt luteinizing hormone/chorionic gonadotropin receptor function, impeding the body's ability to react to these hormones. (medlineplus.gov)
  • 1997). „Isolation and chromosomal localization of GPR31, a human gene encoding a putative G protein-coupled receptor. (wikipedia.org)
  • Endothelial protein C receptor (EPCR) also known as activated protein C receptor (APC receptor) is a protein that in humans is encoded by the PROCR gene . (wikidoc.org)
  • The protein encoded by this gene is a receptor for protein C that enhances its activation. (wikidoc.org)
  • To better understand the structural features required for the selective interaction with D4R, the aliphatic butyl chain of 77-LH-28-1 was modified and the novel compounds 1-6 were prepared. (unicam.it)
  • Methods Using an extensive range of pharmacological tools, the relaxant potential of PGE 2 and selective agonists for the EP 1-4 receptors in the presence and absence of selective antagonists in guinea pig, murine, monkey, rat and human isolated airways was investigated. (bmj.com)
  • These data explain the lack of bronchodilator activity observed with selective EP 2 receptor agonists in clinical studies. (bmj.com)
  • Pharmacologic therapy for osteoporosis includes most commonly the use of antiresorptive agents to decrease bone resorption, such as bisphosphonates, denosumab, and the selective estrogen-receptor modulator (SERM) raloxifene. (medscape.com)
  • How Do Selective Estrogen Receptor Modulators Work? (rxlist.com)
  • Selective estrogen receptor modulators (SERM) are a class of medications used to relieve postmenopausal symptoms and to prevent bone loss ( osteoporosis ) associated with menopause . (rxlist.com)
  • Selective estrogen receptor modulators work by modulating the activity of estrogen receptors, proteins in cells that are activated by estrogen. (rxlist.com)
  • Selective estrogen receptor modulators have both estrogen agonistic and antagonistic properties, depending on the type of tissue. (rxlist.com)
  • Selective estrogen receptor modulators may also be combined with estrogen for postmenopausal women with an intact uterus, who are undergoing estrogen replacement therapy. (rxlist.com)
  • How are selective estrogen receptor modulators used? (rxlist.com)
  • What are side effects of selective estrogen receptor modulators? (rxlist.com)
  • DACT appeared to cause a selective decrease in caffeine-sensitive ryanodine receptor-operated calcium stores in LbetaT2 cells, rather than in thapsigargin-sensitive ER calcium stores. (cdc.gov)
  • 4. Ni Y, Zhou Y, Lu L, Grossmann R, Zhao R. Developmental changes of FSH-R, LH-R, ER-beta and GnRH-I expression in the ovary of prepubertal ducks (Anas platyrhynchos). (ac.ir)
  • The pulsatile release of GnRH stimulates the synthesis and secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). (nih.gov)
  • At midcycle, a large increase in GnRH release results in an LH surge. (nih.gov)
  • Ganirelix Acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. (nih.gov)
  • The atrazine metabolite diaminochlorotriazine suppresses LH release from murine LbetaT2 cells by suppressing GnRH-induced intracellular calcium transients. (cdc.gov)
  • DACT is a reactive electrophile known to form covalent protein adducts both in vitro and in vivo following ATRA exposure and might therefore target proteins involved in GnRH-induced calcium signaling and subsequent LH release. (cdc.gov)
  • To test this hypothesis, LbetaT2 pituitary cells were exposed to 300 microM DACT for 24 h and examined by fluorescence microscopy for GnRH-induced changes in intracellular calcium and LH release. (cdc.gov)
  • LbetaT2 cells exposed to DACT had markedly diminished GnRH-induced intracellular calcium transients and a significant decreased LH release in response to GnRH. (cdc.gov)
  • ERp57 was identified by mass spectrometry as a target of DACT adduction in the ER that could potentially mediate the effects of DACT on inhibition of GnRH-induced calcium signaling and inhibition of LH release. (cdc.gov)
  • Intracellular calcium responses to GnRH and release of LH were restored in DACT-treated cells with the addition of a calcium ionophore (A23187). (cdc.gov)
  • These data suggest that DACT forms adducts on proteins involved in calcium handling within the ER and that dysfunction in this critical signaling system is associated with loss of normal sensitivity to GnRH and subsequent decreased release of LH. (cdc.gov)
  • A cell-based bioassay was used to determine whether the measurement of serum immunoreactive LH is a result of cross-reaction with human chorionic gonadotropin (hCG). (nih.gov)
  • After the cloning of the TSHR, the Kohn laboratory constructed human TSHR-rat luteinizing hormone/chorionic gonadotropin receptor chimeras. (unich.it)
  • In patients with ovarian tumors which possess gonadotropin receptors, relatively high estraiol (E_2) and progesterone (P_4) concentrations were found in peripheral or ovarian venous blood. (nii.ac.jp)
  • The earliest biochemical evidence on the existence of cell-free soluble LH receptor was the purification of an hCG-binding protein, relative molecular mass of 65K (M r , 65K) from porcine follicular fluid and was based on gel filtration followed by affinity chromatography [ 9 ]. (biomedcentral.com)
  • Therefore, how a complex LHCGR protein, embedded within the membrane lipid bilayer, could be secreted as soluble receptor remained unexplained. (biomedcentral.com)
  • Adhesion G protein-coupled receptors (adhesion GPCRs) are a class of 33 human protein receptors with a broad distribution in embryonic and larval cells, cells of the reproductive tract, neurons, leukocytes, and a variety of tumours. (wikipedia.org)
  • Formal G protein-coupled signalling has been demonstrated for a number for adhesion GPCRs, however, the orphan receptor status of many of the receptors still hampers full characterisation of potential signal transduction pathways. (wikipedia.org)
  • Lutropin-choriogonadotropin receptor: an unusual member of the G protein-coupled receptor family. (ac.ir)
  • Mutations that prevent the production of any functional receptor protein cause the more severe features of Leydig cell hypoplasia, and mutations that allow some receptor protein function cause milder signs and symptoms. (medlineplus.gov)
  • These antibodies belong to a network of natural antibodies against adrenergic, cholinergic and other G-protein coupled receptors (GPCR) which were shown to be dysregulated and dysfunctional in various autoimmune diseases ( 9 ). (frontiersin.org)
  • Niacinski receptor 2 , NIACR2 ili GPR109B , je protein koji je kod čoveka kodiran NIACR2 genom . (wikipedia.org)
  • GPR109B je G i / G o protein-spregnuti receptor. (wikipedia.org)
  • The protein is also involved in Plasmodium falciparum malaria as subtypes of the Plasmodium falciparum erythrocyte membrane protein 1 (PfEMP1) family use EPCR of the host as a receptor. (wikidoc.org)
  • 2001). "Identification of the protein C/activated protein C binding sites on the endothelial cell protein C receptor. (wikidoc.org)
  • LDL Receptor-Related Protein 2 (Megalin) as a Target Antigen in Human Kidney Anti-Brush Border Antibody Disease. (bu.edu)
  • The orexin receptors (orexin 1R and orexin 2R) belong to the Family of G-protein coupled receptors. (researchgate.net)
  • of G-protein coupled receptors. (researchgate.net)
  • Applying these to G-Protein Coupled Receptors (GPCRs), which are the single largest family of signaling receptors in human cells. (ucsf.edu)
  • Placental hCG and pitutary LH transduce signals in target tissues through a common receptor (LHCGR). (biomedcentral.com)
  • Additionally, the truncated Lhcgr, misrouted the full-length Lhcgr in ER, thereby decreasing the cell surface expression of the mature functional receptor. (biomedcentral.com)
  • Structurally, LHCGR is similar to thyroid and follicle stimulating hormone receptors (TSHR and FSHR respectively). (biomedcentral.com)
  • Angiotensin receptor. (bmj.com)
  • Objective To determine whether disrupting the renin angiotensin system with angiotensin receptor blockers will improve clinical outcomes in people with covid-19. (bmj.com)
  • Participants Participants were at least 18 years old, previously untreated with angiotensin receptor blockers, with a laboratory confirmed diagnosis of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) infection who had been admitted to hospital for management of covid-19. (bmj.com)
  • Intervention Oral angiotensin receptor blockers (telmisartan in India) or placebo (1:1) for 28 days. (bmj.com)
  • Results Between 3 May 2020 and 13 November 2021, 2930 people were screened for eligibility, with 393 randomly assigned to angiotensin receptor blockers (of which 388 (98.7%) to telmisartan 40 mg/day) and 394 to the control group. (bmj.com)
  • The peptides were tested for their ability to inhibit the binding of 125 I-labeled hCG or LH to rat ovarian membranes and for their ability to inhibit hCG-stimulated progesterone production in a Leydig cell bioassay. (elsevierpure.com)
  • 18. Abdennebi L, Lesport AS, Remy JJ, Grebert D, Pisselet C, Monniaux D, Salesse R. Differences in splicing of mRNA encoding LH receptor in theca cells according to breeding season in ewes. (ac.ir)
  • The most potent inhibitor of LH/ hCG binding was a peptide containing the sequence β81-95, a receptor binding site of the LH/hCG β subunit not previously described. (elsevierpure.com)
  • Recent research also has thrown lights upon a significant role of orexins, especially orexin A, in regulation of male reproductive functions owing to their receptor expressions in vital testicular cells, such as Leydig cells, Sertoli cells as well as spermatozoa at different developmental stages, even in the epididymis and penis. (researchgate.net)
  • 11 ] first reported the production and secretion of soluble LH receptor following transient transfection of a naturally truncated variant of the receptor in COS cells. (biomedcentral.com)
  • Moreover, the lack of a secreted form of the receptor was overcome by co-expression of hCG with the extra-cellular domain of porcine LH receptor leading to the secretion of a mixture of free as well as hCG-receptor complex [ 13 ]. (biomedcentral.com)
  • The suppression of pituitary LH secretion by Ganirelix Acetate is more pronounced than that of FSH. (nih.gov)
  • SERMs bind to estrogen receptors and activate estrogen pathways in some tissue while blocking its effects in other types of tissue. (rxlist.com)
  • The biosensor is meant to have LH receptors as well as estrogen receptors. (diwou.com)
  • When LH or estrogen levels increase, the biosensor is activated, resulting in the synthesis of a compound that causes the color of the gum to change in correlation with the hormone levels. (diwou.com)
  • The LH receptor (LHR) activates several families of heterotrimeric G proteins but only the activation of Gs and subsequent generation of cAMP are universally accepted as important mediators of LH actions. (researchtoactionforum.org)
  • Pimozide, a dopamine receptor blocker, was injected SC or implanted into the hypothalamus or adenohypophysis of ovariectomized rats to determine its effect on the release of LH and prolactin. (elsevierpure.com)
  • Among these receptors, 77-LH-28-1 has been reported to bind the short isoform of the dopamine D2 receptor (D2SR) (4). (unicam.it)
  • To get more information about the pharmacological dopaminergic properties of 77-LH-28-1, this compound was evaluated for its affinity at dopamine D2-like receptor subtypes by radioligand binding assays. (unicam.it)
  • Implantation of Pimozide into the median eminence-arcuate region evoked a gradual consistent increase in prolactin which became significant at 1 hr, and was accompanied by a small decline in plasma LH at 4 hr. (elsevierpure.com)
  • Much smaller increases in plasma prolactin followed implantation of the drug into the adenohypophysis and these implantations were not associated with any alterations in plasma LH. (elsevierpure.com)
  • Ojeda, SR, Harms, PG & McCann, SM 1974, ' Effect of Blockade of Dopaminergic Receptors on Prolactin and LH Release: Median Eminence and Pituitary Sites of Action ', Endocrinology , vol. 94, no. 6, pp. 1650-1657. (elsevierpure.com)
  • Effect of prolactin and growth hormone on prolactin and lh receptors in the dwarf mouse. (jax.org)
  • M1 muscarinic acetylcholine receptor (M1 mAChR) represents an attractive target for the treatment of cognitive deficits associated with several pathologies, including Alzheimer's disease and schizophrenia. (unicam.it)
  • In patients with infection-triggered onset, the associations of low sCD26 with elevated autoantibodies (AAB) against alpha1 adrenergic (AR) and M3 muscarinic acetylcholine receptors (mAChR) point to a pathomechanism of infection-triggered autoimmune-mediated vascular and immunological dysregulation. (frontiersin.org)
  • Autoantibodies (AAB) against nuclear and membrane structures as well as neurotransmitter receptors including muscarinic cholinergic receptor M3/M4-antibodies (M3-mAChR/M4-mAChR) and beta-1 and -2-adrenergic receptor (beta1-AR/beta2-AR) have been described in patients with ME/CFS ( 3 , 6 - 8 ). (frontiersin.org)
  • Toxoplasma GRA15 Activates the NF-?B Pathway through Interactions with TNF Receptor-Associated Factors. (massgeneral.org)
  • As of today, many of the adhesion GPCRs are still orphan receptors and their signalling pathways have not been identified. (wikipedia.org)
  • In other words, the behavioral impact of LH stimulation may very well be on account of multisynaptic pathways originating in the LH, the activation of which might not be detected in brainstem structures applying Fos immunohistochemistry. (angiotensinreceptor.com)
  • Since the discovery 60 years ago of the 'long-acting thyroid stimulator' by Adams and Purves, great progress has been made in the detection of thyroid-stimulating hormone (TSH) receptor (TSHR) autoantibodies (TRAbs) in Graves' disease. (unich.it)
  • These pulses can be detected as transient rises in serum LH. (nih.gov)
  • There are 33 human adhesion GPCRs that can be broken down in the 8 groups and 2 independent receptors. (wikipedia.org)
  • Analysis of fungi showed that there were no secretin receptor family GPCRs, which suggests that they evolved from adhesion GPCRs in a later organism. (wikipedia.org)
  • In particular, a robust decrease in N -methyl- d -aspartate receptor (NMDAR)-mediated synaptic responses in the mPFC was correlated with several measures of attention. (jneurosci.org)
  • Autocatalytic processing gives rise to an extracellular (α) and a membrane-spanning (β) subunit, which are associated non-covalently, resulting in expression of a heterodimeric receptor at the cell surface. (wikipedia.org)
  • Two series of overlapping peptides comprising the entire sequences of the β-subunits of human lutropin (LH) and choriogonadotropin (hCG) were prepared by a comprehensive synthetic strategy in order to identify all linear regions of the subunit that may participate in binding of the hormone to its receptor. (elsevierpure.com)
  • These results affirm the presence of several binding regions in the LH/hCG β-subunit prominent among which is the sequence β81-95. (elsevierpure.com)
  • The aim of the study was to identify the receptor involved in prostaglandin E 2 (PGE 2 )-induced relaxation in guinea pig, murine, monkey, rat and human airways in vitro . (bmj.com)
  • Results In agreement with previous studies, it was found that the EP 2 receptor mediates PGE 2 -induced relaxation of guinea pig, murine and monkey trachea and that the EP 4 receptor mediates PGE 2 -induced relaxation of the rat trachea. (bmj.com)
  • These data have been confirmed in murine airways from EP 2 receptor-deficient mice ( Ptger2 ). (bmj.com)
  • Wild-type UDL-01/08 virus SKP and 3 contemporary wild-type viruses were generated by using reverse genetics, and receptor-binding to 3 receptor analogs was assayed by using biolayer interferometry. (cdc.gov)
  • In contrast to previous publications, a role for the EP 4 receptor in relaxant responses in human airways in vitro was found. (bmj.com)
  • Recent studies show that the human parathyroid calcium sensing receptor (CaSR) is expressed in human colon epithelium and functions to regulate epithelial proliferation and differentiation. (aacrjournals.org)
  • The human parathyroid calcium sensing receptor (CaSR) senses minute changes in extracellular Ca 2+ concentration and functions to tightly regulate systemic Ca 2+ homeostasis (1) . (aacrjournals.org)
  • Here, we addressed the functional interplay between BDNF and cannabinoid CB 1 receptors (CB 1 Rs) in the striatum, a brain area in which both BDNF and CB 1 s play a role in the emotional consequences of stress and of rewarding experiences. (jneurosci.org)
  • The midcycle LH surge initiates several physiologic actions including: ovulation, resumption of meiosis in the oocyte, and luteinization. (nih.gov)
  • The majority assess LH levels and can only answer Yes or No to the question of whether ovulation is occurring or not. (diwou.com)
  • In contrast, this LH receptor binding activity was completely removed when precipitating antibodies for LH were added. (nih.gov)
  • Detection of microbe-associated molecular patterns (MAMPs) by pattern recognition receptors (PRRs) induces currents mediated via slow-type (S-type) anion channels by a yet not understood mechanism. (elifesciences.org)
  • 2003). „Molecular identification of nicotinic acid receptor. (wikipedia.org)
  • The primary metabolite of the herbicide atrazine (ATRA), diaminochlorotriazine (DACT), has been suggested to cause disruption in the hypothalamic--pituitary--gonadal axis leading to inhibition of luteinizing hormone (LH) release. (cdc.gov)
  • When GFLs bind with GFRα, they form complexes and associate with the RET receptor, subsequently activating downstream signaling. (medsci.org)
  • Surprisingly, 77-LH-28-1 showed high affinity and selectivity for D4R over D2R and D3R. (unicam.it)
  • Conclusion Identification of the receptor mediating PGE 2 -induced relaxation represents a key step in developing a novel bronchodilator therapy. (bmj.com)
  • Pioneering work from this lab led to the identification of PLA 2 R (phospholipase A 2 receptor) as the major target antigen in membranous nephropathy in 2009 and THSD7A (thrombospondin type-1 domain-containing 7A) as a minor target antigen in membranous nephropathy in 2014. (bu.edu)
  • Intersubject analysis showed that mean serum LH levels were significantly higher in conceptive cycles on day 4 and day 5 after the FSH peak in urine, and this was confirmed by intrasubject analysis. (nih.gov)
  • In addition to site β81-95, other sites that inhibited hCG/LH binding but with significantly lower potencies included hCGβ 1-15, LHβ 41-55, and LHβ 91-105. (elsevierpure.com)
  • A number of clinical studies have reported beneficial effects of inhaled PGE 2 on airway calibre in normal subjects and patients with asthma and COPD, and we have identified a role for the EP 4 receptor in these relaxant responses. (bmj.com)
  • However, it is becoming increasingly clear that these factors and their receptors are also widely found to express across many different cancers with further research. (medsci.org)
  • They are believed to have evolved from the cAMP receptor family, arising approximately 1275 million years ago before the split of Unikonts from a common ancestor. (wikipedia.org)
  • Li Q, Cao Z, Zhao S. The Emerging Portrait of Glial Cell Line-derived Neurotrophic Factor Family Receptor Alpha (GFRα) in Cancers. (medsci.org)
  • Glial cell line-derived neurotrophic factor family receptor alpha (GFRα) members have been widely connected to the mechanisms contributing to cell growth, differentiation, cell migration and tissue maturation. (medsci.org)
  • Essentially the most striking behavioral effect of LH stimulation was a decrease in the quantity of aversive behaviors to QHCl (primarily gapes and chin rubs). (angiotensinreceptor.com)