Genetic and pharmacological aspects of histamine H3 receptor heterogeneity

Hancock, Arthur A.; Esbenshade, Timothy A.; Krueger, Kathleen M.; Yao, Betty B.

doi:10.1016/j.lfs.2003.06.003

Cited by 105 publications

(73 citation statements)

References 83 publications

(162 reference statements)

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“…[10][11][12]26,28,29,39 In the present study, we showed that histamine promotes migration of breast cancer cells and this effect was mimicked by Imetit while was inhibited by Clobenpropit, suggesting that histamine could stimulate breast cancer cell migration via H3R, playing an important role in invasion and metastasis of malignant tumors. In accordance to this, we have recently described that histamine induces migration while it decreases adhesion of PANC-1 pancreatic carcinoma cells.…”

Section: Discussionsupporting

confidence: 52%

“…The compounds used to address the H3R role in proliferation also bind to the H4R, therefore, despite they present a different rank order of affinity and potency, they do not allow the complete discrimination of the two receptors. [10][11][12]26,28,29,39 To allow the dissection of H3R and H4R signaling, a specific H3R antagonist, JNJ5207852, was used. 26 JNJ5207852 treatment blocked the proliferation increase triggered by 0.01 mM histamine, Imetit and Rα-MeH.…”

Section: Resultsmentioning

confidence: 99%

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The role of histamine in human mammary carcinogenesis: H3 and H4 receptors as potential therapeutic targets for breast cancer treatment.

Medina¹,

Croci²,

Crescenti³

et al. 2008

Cancer Biology & Therapy

108

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There is increasing evidence that describes a histamine role in normal and cancer cell proliferation. To better understand the importance of histamine in breast cancer development, the expression of histamine H3 (H3R) and H4 (H4R) receptors and their association with proliferating cell nuclear antigen (PCNA), histidine decarboxylase (HDC) and histamine content were explored in mammary biopsies. Additionally, we investigated whether H3R and

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Section: Discussionsupporting

confidence: 52%

Section: Resultsmentioning

confidence: 99%

The role of histamine in human mammary carcinogenesis: H3 and H4 receptors as potential therapeutic targets for breast cancer treatment.

Medina¹,

Croci²,

Crescenti³

et al. 2008

Cancer Biology & Therapy

108

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show abstract

“…Recently, several review articles have been published on the histamine H 3 receptor, [2] H 3 R isoforms, [3,4] on H 3 R antagonists [5,6] and agonists, [7] which summarise the current knowledge on this receptor. Briefly, the hH 3 R is a GPCR protein expressed presynaptically in several regions of the central and peripheral nervous system where it functions either as an autoreceptor regulating the release of histamine from histaminergic neurons or as an heteroreceptor regulating the release of several other neurotransmitters.…”

Section: Introductionmentioning

confidence: 99%

Generation of a homology model of the human histamine H3 receptor for ligand docking and pharmacophore-based screening

Schlegel

Laggner

Meier

et al. 2007

J Comput Aided Mol Des

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The human histamine H 3 receptor (hH 3 R) is a G-protein coupled receptor (GPCR), which modulates the release of various neurotransmitters in the central and peripheral nervous system and therefore is a potential target in the therapy of numerous diseases. Although ligands addressing this receptor are already known, the discovery of alternative lead structures represents an important goal in drug design. The goal of this work was to study the hH 3 R and its antagonists by means of molecular modelling tools. For this purpose, a strategy was pursued in which a homology model of the hH 3 R based on the crystal structure of bovine rhodopsin was generated and refined by molecular dynamics simulations in a dipalmitoylphosphatidylcholine (DPPC)/water membrane mimic before the resulting binding pocket was used for high-throughput docking using the program GOLD. Alternatively, a pharmacophore-based procedure was carried out where the alleged bioactive conformations of three different potent hH 3 R antagonists were used as templates for the generation of pharmacophore models. A pharmacophore-based screening was then carried out using the program Catalyst. Based upon a database of 418 validated hH 3 R antagonists both strategies could be validated in respect of their performance. Seven hits obtained during this screening procedure were commercially purchased, and experimentally tested in a [ 3 H]N a -methylhistamine binding assay. The compounds tested showed affinities at hH 3 R with K i values ranging from 0.079 to 6.3 lM.

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“…A negative coupling to phosphoinositide turnover in the human gastric cell line HGT has also been described (Cherifi et al, 1992). Moreover, at least 20 isoforms of the human H 3 R have been described and they vary in the length of the third intracellular loop, their distinct CNS localization, differential signalling pathways and ligand binding affinity, which contribute to the heterogeneity of H 3 R pharmacology (Bongers et al, 2007;Coge et al, 2001a;Hancock et al, 2003;Leurs et al, 2005). …”

Section: Histamine H 3 Rmentioning

confidence: 99%

Histamine Receptors as Potential Therapeutic Targets for Cancer Drug Development

Medina¹,

Lamas²,

Brenzoni³

et al. 2011

Drug Development - A Case Study Based Insight Into Modern Strategies

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Genetic and pharmacological aspects of histamine H3 receptor heterogeneity

Cited by 105 publications

References 83 publications

The role of histamine in human mammary carcinogenesis: H3 and H4 receptors as potential therapeutic targets for breast cancer treatment.

The role of histamine in human mammary carcinogenesis: H3 and H4 receptors as potential therapeutic targets for breast cancer treatment.

Generation of a homology model of the human histamine H3 receptor for ligand docking and pharmacophore-based screening

Histamine Receptors as Potential Therapeutic Targets for Cancer Drug Development

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