ホルミルペプチド受容体、ホルミルペプチドレセプター

WordNet

develop into a distinctive entity; "our plans began to take shape" (同)take form, take shape, spring
assume a form or shape; "the water formed little beads"
the visual appearance of something or someone; "the delicate cast of his features" (同)shape, cast
a mold for setting concrete; "they built elaborate forms for pouring the foundation"
a particular mode in which something is manifested; "his resentment took the form of extreme hostility"
a perceptual structure; "the composition presents problems for students of musical form"; "a visual pattern must include not only objects but the spaces between them" (同)shape, pattern
(biology) a group of organisms within a species that differ in trivial ways from similar groups; "a new strain of microorganisms" (同)variant, strain, var.
the phonological or orthographic sound or appearance of a word that can be used to describe or identify something; "the inflected forms of a word can be represented by a stem and a list of inflections to be attached" (同)word form, signifier, descriptor
a printed document with spaces in which to write; "he filled out his tax form"
an ability to perform well; "he was at the top of his form"; "the team was off form last night"
an arrangement of the elements in a composition or discourse; "the essay was in the form of a dialogue"; "he first sketches the plot in outline form"
to compose or represent:"This wall forms the background of the stage setting"; "The branches made a roof"; "This makes a fine introduction" (同)constitute, make
create (as an entity); "social groups form everywhere"; "They formed a company" (同)organize, organise
a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
amide combining the amino group of one amino acid with the carboxyl group of another; usually obtained by partial hydrolysis of protein

PrepTutorEJDIC

〈C〉〈U〉(色・材質に対して)『形』,形状,姿 / 〈C〉『人体』,体つき / 〈C〉〈U〉『外観』,格好,人影 / 〈C〉〈U〉(ものの現れる)『形態』,形式 / 〈C〉(生物などの)『種類』,品種 / 〈U〉(芸術作品の)表現形式 / 〈U〉(特にスポーツで)(競技者の)フォーム / 〈U〉(心身の)調子,元気 / 〈C〉(印刷された)書き込み用紙,ひな形 / 〈U〉《話》(ある集団などの)やり方,仕方,方式 / 〈C〉〈U〉しきたり,伝統的な儀式 / 〈C〉(英国の学校・米国のある学校で)学年,学級 / 〈U〉〈C〉(意味に対する)形態,形;語形 / 〈C〉(通例寄りかかりのない)長い木のいす / 〈素材〉‘に'形を与える,(…に)…‘を'形作る《+『名』+『into』+『名』》 / (素材から)…‘を'形作る《+『名』+『out of』+『名』》 / …‘を'組織する,構成する / 〈考えなど〉‘を'まとめる,思い付く;〈計画など〉‘を'立てる / 〈習慣など〉‘を'身に付ける;〈交際など〉‘を'結ぶ / 〈文章など〉‘を'組み立てる;〈複数形など〉‘を'作る / (ある順序に)配列する,整列させる / 〈物が〉形を成す / 生じる,現れる / (…に)なる《+『into』+『名』》
=sense organ / 受信装置

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/05/20 00:18:12」(JST)

wiki en

The formyl peptide receptors (FPR) are a members of a class of G protein-coupled receptors involved in chemotaxis.^[1]^[2] These receptors where originally identified by their ability to bind N-formyl peptides such as N-formylmethionine produced by the degradation of either bacterial or host cells.^[3]^[4] Hence formyl peptide receptors are involved in mediating immune cell response to infection. These receptors may also act to suppress the immune system under certain conditions.^[5] The close phylogenetical relation of signaling in chemotaxis and olfaction was recently proved by detection formyl peptide receptor like proteins as a distinct family of vomeronasal organ chemosensors in mice ^[6]

Structure - function

The formyl peptide receptor (FPR) belongs to the class of receptors possessing seven hydrophobic transmembrane domains. The conformation of the FPR is stabilized by several interactions. These include potential salt bridge formation between Arg84-Arg205, Lys85-Arg205, and Lys85-Asp284 which help determine the three-dimensional structure of transmembrane domains, as well as positively charged residues (Arg, Lys) which interact with negatively charged phosphates. Furthermore residue Arg163 may interact with the ligand binding pocket of the second extracellular loop of the FPR.

With respect to binding of the formyl Met-Leu-Phe peptide, there are additional potential interactions which include hydrogen bonding interactions between Arg84 and Lys85 of the first extracellular loop and the N-formyl group of the ligand as well as the peptide backbone of formyl Met-Leu-Phe which can form similar interactions. The formyl-Met moiety of the ligand was shown to form disulfide bridges with Cys residues, and an interaction with Arg163 was also demonstrated. (It is important to mention that some interaction which stabilize the conformation of the receptor may also influence ligand-binding.) Some oligopeptides were also described as characteristic constituents linked to Asn-s of the extracellular N terminal part and to the ligand binding pocket of the second extracellular loop. These components can also determine or make more specific the ligand-receptor interaction.^[7]

Schematic diagram of the formyl peptide receptor 1. Transmembrane helices of the receptor are represented by blue-green cylinders while the cell membrane in which the receptor is imbedded is depicted in yellow. The extracellular face of the cell membrane is on top while the intracellular (cytoplasmic) face is on the bottom. Extracellular loops of the FPR responsible for N-for-Met-Leu-Phe (Nfor-MLF) binding are shown in red.

Formyl peptide receptor (FPR) signaling pathways.

Signaling pathways

Induction of FPR triggers multiple changes in eukaryotic cells including rearrangement of the cytoskeleton which in turn facilitates cell migration and the synthesis of chemokines. Important FPR regulated pathways include:

G protein dependent activation of phospholipase C (PLC) which results in the breakdown of the membrane constituent phospholipid, phosphatidylinositol (4,5)-bisphosphate (PIP2) into phosphatidylinositol (3,4,5)-trisphosphate (IP3) and diacyl glycerol (DAG). IP3 is one of the most effective inducer of Ca²⁺ increase from cytoplasmic pools and from outside the cell via opening Ca²⁺ channels. DAG in turn is an inducer of protein kinase C (PKC).
Activation of the regulatory small GTPase, RAS. The active RAS can in turn activate RAF, a Ser/Thr kinase. In the next step mitogen-activated protein kinases (MAP kinases) are activated. (Also known as extracellular signal-regulated kinases - ERKs or MAP/ERK kinase (MEK)). As a result of the last step, ERK1 and ERK2 are activated. The phosphorylated forms of ERKs can continue the cascade by triggering activation more interacting kinases which results in altered transcriptional activity in the nucleus.
Ligand binding to FPR can also induce the activation of CD38, an ectoenzyme of the surface membrane. As a result of activation NAD⁺ molecules will enter the cytoplasm. NAD⁺ is converted into cyclic ADP ribose (cADPR), a second messenger which interacts with ryanodine receptors (RyR) on the surface of the rough endoplasmic reticulum. The overal result of the process is increased cytoplasmic Ca²⁺ levels via the direct pathway described above and also via indirect pathways such as opening of Ca²⁺ channels in the cell membrane. The sustained increase of Ca²⁺ is required for directed migration of the cells.^[8]

References

^ Migeotte I, Communi D, Parmentier M (2006). "Formyl peptide receptors: a promiscuous subfamily of G protein-coupled receptors controlling immune responses". Cytokine Growth Factor Rev. 17 (6): 501–19. doi:10.1016/j.cytogfr.2006.09.009. PMID 17084101.
^ Ye RD, Boulay F, Wang JM, Dahlgren C, Gerard C, Parmentier M, Serhan CN, Murphy PM (June 2009). "International Union of Basic and Clinical Pharmacology. LXXIII. Nomenclature for the formyl peptide receptor (FPR) family". Pharmacol. Rev. 61 (2): 119–61. doi:10.1124/pr.109.001578. PMC 2745437. PMID 19498085. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2745437.
^ Le Y, Murphy PM, Wang JM (2002). "Formyl-peptide receptors revisited". Trends Immunol. 23 (11): 541–8. doi:10.1016/S1471-4906(02)02316-5. PMID 12401407.
^ Panaro MA, Acquafredda A, Sisto M, Lisi S, Maffione AB, Mitolo V (2006). "Biological role of the N-formyl peptide receptors". Immunopharmacology and immunotoxicology 28 (1): 103–27. doi:10.1080/08923970600625975. PMID 16684671.
^ Braun MC, Wang JM, Lahey E, Rabin RL, Kelsall BL (2001). "Activation of the formyl peptide receptor by the HIV-derived peptide T-20 suppresses interleukin-12 p70 production by human monocytes". Blood 97 (11): 3531–6. doi:10.1182/blood.V97.11.3531. PMID 11369647.
^ Rivière S, Challet L, Fluegge D, Spehr M, Rodriguez I (2009). "Formyl peptide receptor-like proteins are a novel family of vomeronasal chemosensors.". Nature 459 (7246): 1–4. doi:10.1038/nature08029. PMID 19387439.
^ Lala A, Gwinn M, De Nardin E (1999). "Human formyl peptide receptor function role of conserved and nonconserved charged residues". Eur. J. Biochem. 264 (2): 495–9. doi:10.1046/j.1432-1327.1999.00647.x. PMID 10491096.
^ Partida-Sánchez S, Cockayne DA, Monard S, Jacobson EL, Oppenheimer N, Garvy B, Kusser K, Goodrich S, Howard M, Harmsen A, Randall TD, Lund FE (2001). "Cyclic ADP-ribose production by CD38 regulates intracellular calcium release, extracellular calcium influx and chemotaxis in neutrophils and is required for bacterial clearance in vivo". Nat. Med. 7 (11): 1209–16. doi:10.1038/nm1101-1209. PMID 11689885.

External links

"Formylpeptide Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1359.
MeSH Formyl+peptide+receptor

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 肥満の薬物療法 drug therapy of obesity
2. 心不全におけるナトリウム利尿ペプチド測定 natriuretic peptide measurement in heart failure
3. インスリン受容体の構造および機能 structure and function of the insulin receptor
4. ペプチドホルモンのシグナル伝達および調節 peptide hormone signal transduction and regulation
5. 膵神経内分泌腫瘍（膵島細胞腫瘍）の分類、疫学、臨床症状、局在、および病期分類 classification epidemiology clinical presentation localization and staging of pancreatic neuroendocrine tumors islet cell tumors

English Journal

Splenic leukocytes mediate the hyperglycemic exacerbation of myocardial infarct size in mice.

Tian Y1, French BA, Kron IL, Yang Z.
Basic research in cardiology.Basic Res Cardiol.2015 Jul;110(4):496. doi: 10.1007/s00395-015-0496-3. Epub 2015 May 27.
Acute hyperglycemia during acute myocardial infarction is associated with worse myocardial injury and increased mortality. Using a mouse model of myocardial ischemia/reperfusion injury, we tested the hypothesis that acute hyperglycemia activates splenic leukocytes and subsequently exacerbates myocar
PMID 26014921

Functional interaction between CTGF and FPRL1 regulates VEGF-A-induced angiogenesis.

Lee MS1, Ghim J1, Kim SJ1, Yun YS1, Yoo SA2, Suh PG1, Kim WU3, Ryu SH4.
Cellular signalling.Cell Signal.2015 Jul;27(7):1439-48. doi: 10.1016/j.cellsig.2015.04.001. Epub 2015 Apr 9.
Vascular endothelial growth factor-A (VEGF-A) is a master regulator of angiogenesis that controls several angiogenic processes in endothelial cells. However, the detailed mechanisms of VEGF-A responsible for pleiotropic functions and crosstalk with other signaling pathways have not been fully unders
PMID 25862954

Annexin A1 mimetic peptide controls the inflammatory and fibrotic effects of silica particles in mice.

Trentin PG1, Ferreira TP1, Arantes AC1, Ciambarella BT1, Cordeiro RS1, Flower RJ2, Perretti M2, Martins MA1, Silva PM1.
British journal of pharmacology.Br J Pharmacol.2015 Jun;172(12):3058-71. doi: 10.1111/bph.13109. Epub 2015 Apr 10.
BACKGROUND AND PURPOSE: Endogenous glucocorticoids are pro-resolving mediators, an example of which is the endogenous glucocorticoid-regulated protein annexin A1 (ANXA1). Because silicosis is an occupational lung disease characterized by unabated inflammation and fibrosis, in this study we tested th
PMID 25659822