Molecular Cloning of the Human Histamine H1 Receptor Gene

Fukui, Hirokazu; Fujimoto, Katsumi; Mizuguchi, Hiroyuki; Sakamoto, Kenya; Horio, Yoshiyuki; Takai, Shin‐ichiro; Yamada, Kyoko; Ito, Shunsuke

doi:10.1006/bbrc.1994.1786

Cited by 125 publications

(84 citation statements)

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“…No potential tumor suppressor genes, however, have yet been identified at chromosome 3p25. Genes that have been localized to 3p25 include the histamine H1 receptor (40), oxytocin receptor (41), xeroderma pigmentosum-C (42), and the IL-5 receptor alpha (43), none of which appears to be an attractive candidate as a pancreatic tumor suppressor gene. The putative novel tumor suppressor gene on 3p25 involved in pancreatic endocrine cell tumorigenesis may or may not be the same one implicated in other tumors such as head and neck or esophageal cancer.…”

Section: Discussionmentioning

confidence: 99%

A novel pancreatic endocrine tumor suppressor gene locus on chromosome 3p with clinical prognostic implications.

Chung¹,

Smith²,

Louis³

et al. 1997

J. Clin. Invest.

124

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The molecular pathogenesis of pancreatic endocrine tumors is largely unknown. Such tumors are more likely to develop in individuals with the von Hippel-Lindau (VHL) syndrome. We sought to determine whether allelic loss of the recently identified VHL tumor suppressor gene on chromosome 3p25-26 occurs in the more common sporadic forms of these tumors. Allelic loss on chromosome 3p was identified in 33% of 43 patients with endocrine tumors of the pancreas. The smallest common region of allelic loss, however, centered not at the VHL locus, but rather at 3p25, centromeric to VHL . Furthermore, no mutations of the VHL gene were identified in these tumors. Loss of alleles on chromosome 3p was associated with clinically malignant disease, whereas tumors with retained 3p alleles were more likely to be benign. Thus, the VHL gene does not appear to play a pathogenic role in the development of sporadic pancreatic endocrine tumors. Instead, a locus at chromosome 3p25 may harbor a novel pancreatic endocrine tumor suppressor gene, and allelic loss of this chromosomal region may serve as a molecular marker that helps distinguish benign from clinically malignant disease. ( J. Clin. Invest. 1997. 100:404-410.)

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Section: Discussionmentioning

confidence: 99%

A novel pancreatic endocrine tumor suppressor gene locus on chromosome 3p with clinical prognostic implications.

Chung¹,

Smith²,

Louis³

et al. 1997

J. Clin. Invest.

124

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“…Gifts of mianserin hydrochloride (Organon NV, Oss, The Netherlands), pcDEF 3 (Dr. J. Langer; Goldman et al, 1996), and the cDNA encoding the human histamine H 1 R (Dr. H. Fukui;Fukui et al, 1994) are greatly acknowledged. pNF-B-Luc was obtained from Stratagene (La Jolla, CA), ATP disodium salt, bovine serum albumin, chloroquine diphosphate, DEAE-dextran (chloride form), histamine dihydrochloride, mepyramine (pyrilamine maleate), and polyethylenimine were purchased from Sigma-Aldrich (St. Louis, MO).…”

Section: Methodsmentioning

confidence: 99%

A Structural Insight into the Reorientation of Transmembrane Domains 3 and 5 during Family A G Protein-Coupled Receptor Activation

Sansuk¹,

Deupí²,

Torrecillas³

et al. 2010

Mol Pharmacol

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Rearrangement of transmembrane domains (TMs) 3 and 5 after agonist binding is necessary for stabilization of the active state of class A G protein-coupled receptors (GPCRs). Using sitedirected mutagenesis and functional assays, we provide the first evidence that the TAS(I/V) sequence motif at positions 3.37 to 3.40, highly conserved in aminergic receptors, plays a key role in the activation of the histamine H 1 receptor. By combining these data with structural information from X-ray crystallography and computational modeling, we suggest that Thr 3.37 interacts with TM5, stabilizing the inactive state of the receptor, whereas the hydrophobic side chain at position 3.40, highly conserved in the whole class A GPCR family, facilitates the reorientation of TM5. We propose that the structural change of TM5 during the process of GPCR activation involves a local Pro 5.50 -induced unwinding of the helix, acting as a hinge, and the highly conserved hydrophobic Ile 3.40 side chain, acting as a pivot.

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“…Cells from stable clonal lines expressing the human histamine H 1 R (Fukui et al, 1994) or H 2 R (Gantz et al, 1991) were harvested and homogenized in TE buffer as described above, and final membrane preparations were obtained by re-homogenizing the pellets in 6.25 vol of TE buffer and frozen at Ϫ70°C until used. Membranes were prepared from HEK cells transiently transfected with the pCINeo expression vector harboring the human histamine H 4 R (Liu et al, 2001), as described above for the H 3 R. Radioligand Binding Assays.…”

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confidence: 99%

Two Novel and Selective Nonimidazole Histamine H₃ Receptor Antagonists A-304121 and A-317920: I. In Vitro Pharmacological Effects

Esbenshade

Krueger²,

Miller³

et al. 2003

J Pharmacol Exp Ther

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Histamine H 3 receptor (H 3 R) antagonists enhance neurotransmitter release and are being developed for the treatment of a variety of neurological and cognitive disorders. Many potent histamine H 3 R antagonists contain an imidazole moiety that limits receptor selectivity and the tolerability of this class of compounds. Here we present the in vitro pharmacological data for two novel piperazine amide ligands,

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Molecular Cloning of the Human Histamine H1 Receptor Gene

Cited by 125 publications

References 0 publications

A novel pancreatic endocrine tumor suppressor gene locus on chromosome 3p with clinical prognostic implications.

A novel pancreatic endocrine tumor suppressor gene locus on chromosome 3p with clinical prognostic implications.

A Structural Insight into the Reorientation of Transmembrane Domains 3 and 5 during Family A G Protein-Coupled Receptor Activation

Two Novel and Selective Nonimidazole Histamine H₃ Receptor Antagonists A-304121 and A-317920: I. In Vitro Pharmacological Effects

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Molecular Cloning of the Human Histamine H1 Receptor Gene

Cited by 125 publications

References 0 publications

A novel pancreatic endocrine tumor suppressor gene locus on chromosome 3p with clinical prognostic implications.

A novel pancreatic endocrine tumor suppressor gene locus on chromosome 3p with clinical prognostic implications.

A Structural Insight into the Reorientation of Transmembrane Domains 3 and 5 during Family A G Protein-Coupled Receptor Activation

Two Novel and Selective Nonimidazole Histamine H3 Receptor Antagonists A-304121 and A-317920: I. In Vitro Pharmacological Effects

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Two Novel and Selective Nonimidazole Histamine H₃ Receptor Antagonists A-304121 and A-317920: I. In Vitro Pharmacological Effects