State of the art paper T lymphocytes as a target of histamine action

Kmiecik, Tomasz; Otocka-Kmiecik, Aneta; Górska-Ciebiada, Małgorzata; Ciebiada, Maciej

doi:10.5114/aoms.2012.27295

Cited by 24 publications

(16 citation statements)

References 40 publications

(39 reference statements)

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“…However, it has been demonstrated that alcaftadine has H4 receptor inverse agonist activity, which in turn could inhibit H4 receptor-mediated Th2-lymphocyte-driven allergic response on the conjunctiva. 29 , 32 , 36 Because activation of H1 and H4 receptors are associated with Th2-lymphocyte-driven allergen-induced inflammation of the conjunctiva, antiallergic therapeutic agents with inverse agonist activity on H1 and H4 receptors could provide therapeutic benefits to patients with allergic conjunctivitis. 35 , 48 Additionally, reducing the activation and migration of allergen-bearing DCs to regional lymph nodes via H4 receptor inverse agonism is associated with dampening of Th2-dependent conjunctival inflammation and pruritus.…”

Section: Discussionmentioning

confidence: 99%

“… 34 , 35 H2 receptors are expressed on nerve cells, vascular smooth muscles, endothelial cells, epithelial cells, neutrophils, eosinophils, macrophages, monocytes, DCs, T-cells, and B-cells. 34 , 36 H3 receptors are usually expressed on nerve cells and goblet cells. It is of note that histamine receptors 1, 2, and 4 are also expressed on goblet cells of the conjunctiva.…”

Section: Histaminementioning

confidence: 99%

“… 48 The interaction of histamine with histamine receptors expressed on immature DCs recruits and activates DCs to become mature antigen-presenting cells capable of activating naïve T lymphocytes to become activated CD4 T lymphocytes that subsequently differentiate into Th2-lymphocytes. 29 , 32 , 36 Thus, Th2-lymphocytes along with mast cells are the major immune cells involved in allergic inflammatory response in allergic conjunctivitis. 4 The binding of released histamine from degranulated mast cells to histamine receptors on vascular endothelial cells, neuronal fibers, goblet cells, immune cells, and conjunctival epithelium culminates in the clinical manifestation of allergic conjunctivitis (redness, itching, tearing, chemosis, and eyelid edema).…”

Section: Immunopathological Mechanismsmentioning

confidence: 99%

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Update and clinical utility of alcaftadine ophthalmic solution 0.25% in the treatment of allergic conjunctivitis

Chigbu¹,

Coyne²

2015

OPTH

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Allergic disorders of the ocular surface are primarily characterized as IgE- and/or T-lymphocyte-mediated disorders that affect the cornea, conjunctiva, and eyelid. Approximately 40% of individuals in the developed countries have allergic conjunctivitis, and as such, it is the most common form of ocular allergy. Seasonal allergic conjunctivitis is the most prevalent type of allergic conjunctivitis that impacts the quality of life of patients. This article reviews the pharmacology, pharmacodynamics, pharmacokinetics, clinical trials, clinical efficacy, and safety of alcaftadine. Histamine and the pathological mechanism of ocular allergy will be briefly reviewed with the intent of providing a background for the detailed discussion on the clinical utility of alcaftadine in allergic conjunctivitis. The Medline PubMed, Elsevier Science Direct, and Google Scholar databases were used to search for evidence-based literature on histamine and immunopathological mechanism of allergic conjunctivitis, as well as on pharmacology, pharmacodynamics, pharmacokinetics, clinical trials, and clinical efficacy of alcaftadine. The treatment and management goals of allergic conjunctivitis are to prevent or minimize the inflammatory cascade associated with allergic response in the early stages of the pathological mechanism. It is of note that activation of histamine receptors on immune and nonimmune cells are associated with allergen-induced inflammation of the conjunctiva and its associated ocular allergic manifestations, including itching, edema, hyperemia, and tearing. Alcaftadine is an efficacious multiple action antiallergic therapeutic agent with inverse agonist activity on H1, H2, and H4 receptors, as well as anti-inflammatory and mast cell stabilizing effects that could provide therapeutic benefits to patients with allergic conjunctivitis.

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Section: Discussionmentioning

confidence: 99%

Section: Histaminementioning

confidence: 99%

Section: Immunopathological Mechanismsmentioning

confidence: 99%

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Update and clinical utility of alcaftadine ophthalmic solution 0.25% in the treatment of allergic conjunctivitis

Chigbu¹,

Coyne²

2015

OPTH

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“…This was also observed in another benchmark study targeting 13 GPCR ECL2 using the CABS modeling software. 143 Scores alone were less effective than the combination of scores and use of the conserved disulfide bond between Cys3.25 in TM3 and Cys45.50 in ECL2 as a filter. Notably, selection of ten structures provided substantial improvement in model quality within the set over selection of only one structure, but inclusion of additional structures up to twenty-five did not provide significant additional gains.…”

Section: Resultsmentioning

confidence: 96%

A benchmark study of loop modeling methods applied to G protein-coupled receptors

Wink

Baker

Cole

et al. 2019

J Comput Aided Mol Des

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G protein-coupled receptors (GPCR) are important drug discovery targets. Despite progress, many GPCR structures have not yet been solved. For these targets, comparative modeling is used in virtual ligand screening to prioritize experimental efforts. However, the structure of extracellular loop 2 (ECL2) is often poorly predicted. This is significant due to involvement of ECL2 in ligand binding for many Class A GPCR. Here we examine the performance of loop modeling protocols available in the Rosetta (Cyclic Coordinate Descent [CCD], KIC with Fragments [KICF] and Next Generation KIC [NGK]) and Molecular Operating Environment (MOE) software suites (de novo search). ECL2 from GPCR crystal structures served as the structure prediction targets and were divided into four sets depending on loop length. Results suggest that KICF and NGK sampled and scored more loop models with sub-angstrom and near-atomic accuracy than CCD or de novo search for loops of 24 or fewer residues. None of the methods were able to sample loop conformations with near-atomic accuracy for the longest targets ranging from 25-32 residues based on 1000 models generated. For these long loop targets, increased conformational sampling is necessary. The strongly conserved disulfide bond between Cys3.25 and Cys45.50 in ECL2 proved an effective filter. Setting an upper limit of 5.1 Å on the S-S distance improved the lowest RMSD model included in the top 10 scored structures in Groups 1-4 on average between 0.33 and 1.27 Å. Disulfide bond formation and geometry optimization of ECL2 provided an additional incremental benefit in structure quality.

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“…We as Data mining is a study of delving the concealed data in a database and is also known as analysis steps of knowledge discovery in database [1]. Techniques of data mining help to process the data and turn them into useful information.…”

Section: Introductionmentioning

confidence: 99%

Big Data Analytics in Healthcare and Delve Bioinformatics Data Space for Health Amelioration

Joel¹,

Priya²

2018

IJCA

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The healthcare informatics focuses on health data, information and knowledge, including their collection, processing, analysis and use bioinformatics employs computational tools and techniques to study and analyze large biological databases and to understand disease and study of inherent genetic information molecular structure by relating them with healthcare data. This amassing of healthcare information will enable the biologist and scientist to improve health as drug discovery. This paper touches on big data in healthcare and analyzes of those big data in healthcare for the better improvement of healthcare system, bioinformatics data stored in secured manner. Finally, the paper looks on the helpful result, the beneficence of each of them in amelioration of healthcare system. To achieve this health amelioration in bioinformatics, we use Hadoop as tools which collect and analyze the huge amount of data in healthcare system.

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State of the art paper T lymphocytes as a target of histamine action

Cited by 24 publications

References 40 publications

Update and clinical utility of alcaftadine ophthalmic solution 0.25% in the treatment of allergic conjunctivitis

Update and clinical utility of alcaftadine ophthalmic solution 0.25% in the treatment of allergic conjunctivitis

A benchmark study of loop modeling methods applied to G protein-coupled receptors

Big Data Analytics in Healthcare and Delve Bioinformatics Data Space for Health Amelioration

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State of the art paper T lymphocytes as a target of histamine action

Cited by 24 publications

References 40 publications

Update and clinical utility of alcaftadine ophthalmic solution 0.25% in the treatment of&nbsp;allergic conjunctivitis

Update and clinical utility of alcaftadine ophthalmic solution 0.25% in the treatment of&nbsp;allergic conjunctivitis

A benchmark study of loop modeling methods applied to G protein-coupled receptors

Big Data Analytics in Healthcare and Delve Bioinformatics Data Space for Health Amelioration

Contact Info

Product

Resources

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Update and clinical utility of alcaftadine ophthalmic solution 0.25% in the treatment of allergic conjunctivitis

Update and clinical utility of alcaftadine ophthalmic solution 0.25% in the treatment of allergic conjunctivitis