オフターゲットの、非特異的な
- 関
- non-specific、nonspecific、nonspecifically、unspecific
WordNet
- not caused by a specific agent; used also of staining in making microscope slides; "nonspecific enteritis"
- without specificity; "nonspecifically staining substances"
- not performing or scheduled for duties; "Hes off every Tuesday"
- at a distance in space or time; "the boat was 5 miles off (or away)"; "the party is still 2 weeks off (or away)"; "away back in the 18th century" (同)away
- (of events) no longer planned or scheduled; "the wedding is definitely off" (同)cancelled
- in an unpalatable state; "sour milk" (同)sour, turned
- below a satisfactory level; "an off year for tennis"; "his performance was off"
- no longer on or in contact or attached; "clean off the dirt"; "he shaved off his mustache"
- not in operation or operational; "the oven is off"; "the lights are off"
- intend (something) to move towards a certain goal; "He aimed his fists towards his opponents face"; "criticism directed at her superior"; "direct your anger towards others, not towards yourself" (同)aim, place, direct, point
- sports equipment consisting of an object set up for a marksman or archer to aim at (同)butt
- a reference point to shoot at; "his arrow hit the mark" (同)mark
- the location of the target that is to be hit (同)target area
- the near or foreseeable future; "there was a wedding in the offing"
- the part of the sea that can be seen from the shore and is beyond the anchoring area; "there was a ship in the offing"
PrepTutorEJDIC
- 《分離》(接触しているところ)『から』,から離れて,からはずれて / 《位置》…『から離れたところで』(『に』) / (本来の状態など)からはずれて,…が狂って,がなくなって / (本道など)からそれて,から横道にはいったところに / 《eat, dineなどと共に》…からとって[食べる] / 《『from off』の形で》《話》…から / (ある値段)から割り引いて / 《話》…をやめて,慎んで《+『名』(do『ing』)》 / (仕事義務など)から離れて,を休んで / (人)をたよって,にやっかいになって / (1)《運動・移動を表す動詞と共に》『離れて』,向こうへ / 《状態の動詞と共に》『離れて』 / 《瞬間の動作を表す動詞と共に》『離して』 / 『去って』,出かけて / (電気・ガス・水道などが)『切れて』 / (本来の位置・状態などから)『はずれて』 / (仕事・勤務などを)『旧んで』 / (時間的・空間的に)『離れて』 / 《動作の完了》『すっかり』,完全に / 割り引いて / (中心・的などから)『それた』,『離れた』,はずれた / 『時期はずれの』,(時期などが)いつもほどよくない,シーズン外の / (状態が)水準以下の,いつも調子(状態)でない / 《補語にのみ用いて》(予定・用意されたことが)取りやめになって / 《補語にのみ用いて》(電気器具などが)電源が切れて;(ガス・水道が)切れて,止まって / (人が)…の暮らしぶりで / 勤務のない,休みの / 取れて,ぬげて,はずれて / (馬・車の1対のうち)右側の / 《補語にのみ用いて》(走者が)すでに走り出して / 《おもに英》《補語にのみ用いて》(食物などが)いたんで食べられない;飲めない / 《英》《補語にのみ用いて》(食堂などでメニューには載っているが料理が)もう品切れで / 《英》《補語にのみ用いて》(人の態度が)誠意のない,不親切な,ひどい / 《名詞の前にのみ用いて》《the ~》(クリケットで)打者の右前方の
- 《所有・所属》…『の』,…のものである,…に属する・《材料・要素》…『でできた』,から成る・《部分》…『の』[『中の』] ・《数量・単位・種類を表す名詞に付いて》…の・《原因・動機》…『で』,のために(because of) ・《主格関係》…『の』,による,によって・《目的格関係》…『を』,の・《同格関係》…『という』・《関係・関連》…『についての』[『の』],の点で・《抽象名詞などと共に》…の[性質をもつ] ・《『It is』+『形』+『of』+『名』+『to』 doの形で,ofの後の名詞を意味上の主語として》・《分離》…『から』・《起原・出所》…『から』[『の』](out of) ・《『名』+『of』+『a』(『an』)+『名』の形で》…のような・《『名』+『of』+『mine』(『yours, his』など独立所有格)の形で》…の…・《時》(1)《副詞句を作って》…に《形容詞句を作って》…の・《時刻》《米》…前(to,《米》before)
- (鉄砲などの)『標的』,的,攻撃目標 / (批評・軽べつなどの)的,種《+of+名》 / (行為などの)目標,到達目標
- (陸から見える)沖,沖合い
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/02/11 11:13:45」(JST)
[Wiki en表示]
In pharmacology, an antitarget is a receptor, enzyme, or other biological target that, when affected by a drug, causes undesirable side-effects. During drug design and development, it is important for pharmaceutical companies to ensure that new drugs do not show significant activity at any of a range of antitargets, most of which are discovered largely by chance.[1][2]
Among the best-known and most significant antitargets are the hERG channel and the 5-HT2B receptor, both of which causing long-term problems with heart function that can prove fatal (long QT syndrome and cardiac fibrosis, respectively), in a small but unpredictable proportion of users. Both of these targets were discovered as a result of high levels of distinctive side-effects during the marketing of certain medicines, and, while some older drugs with significant hERG activity are still used with caution, most drugs that have been found to be strong 5-HT2B agonists were withdrawn from the market, and any new compound will almost always be discontinued from further development if initial screening shows high affinity for these targets.[3][4][5][6][7][8]
References
- ^ Klabunde, T.; Evers, A. (2005). "GPCR antitarget modeling: pharmacophore models for biogenic amine binding GPCRs to avoid GPCR-mediated side effects". Chembiochem : a European journal of chemical biology 6 (5): 876–889. doi:10.1002/cbic.200400369. PMID 15791686. edit
- ^ Price, D.; Blagg, J.; Jones, L.; Greene, N.; Wager, T. (2009). "Physicochemical drug properties associated with in vivo toxicological outcomes: a review". Expert opinion on drug metabolism & toxicology 5 (8): 921–931. doi:10.1517/17425250903042318. PMID 19519283. edit
- ^ De Ponti, F.; Poluzzi, E.; Cavalli, A.; Recanatini, M.; Montanaro, N. (2002). "Safety of non-antiarrhythmic drugs that prolong the QT interval or induce torsade de pointes: an overview". Drug safety : an international journal of medical toxicology and drug experience 25 (4): 263–286. PMID 11994029. edit
- ^ Recanatini, M.; Poluzzi, E.; Masetti, M.; Cavalli, A.; De Ponti, F. (2005). "QT prolongation through hERG K(+) channel blockade: current knowledge and strategies for the early prediction during drug development". Medicinal Research Reviews 25 (2): 133–166. doi:10.1002/med.20019. PMID 15389727. edit
- ^ Raschi, E.; Vasina, V.; Poluzzi, E.; De Ponti, F. (2008). "The hERG K+ channel: target and antitarget strategies in drug development". Pharmacological research : the official journal of the Italian Pharmacological Society 57 (3): 181–195. doi:10.1016/j.phrs.2008.01.009. PMID 18329284. edit
- ^ Raschi, E.; Ceccarini, L.; De Ponti, F.; Recanatini, M. (2009). "hERG-related drug toxicity and models for predicting hERG liability and QT prolongation". Expert opinion on drug metabolism & toxicology 5 (9): 1005–1021. doi:10.1517/17425250903055070. PMID 19572824. edit
- ^ Huang, X.; Setola, V.; Yadav, P.; Allen, J.; Rogan, S.; Hanson, B.; Revankar, C.; Robers, M. et al. (2009). "Parallel Functional Activity Profiling Reveals Valvulopathogens Are Potent 5-Hydroxytryptamine2B Receptor Agonists: Implications for Drug Safety Assessment". Molecular Pharmacology 76 (4): 710–722. doi:10.1124/mol.109.058057. PMC 2769050. PMID 19570945. //www.ncbi.nlm.nih.gov/pmc/articles/PMC2769050/. edit
- ^ Bhattacharyya, S.; Schapira, A. H.; Mikhailidis, D. P.; Davar, J. (2009). "Drug-induced fibrotic valvular heart disease". The Lancet 374 (9689): 577. doi:10.1016/S0140-6736(09)60252-X. edit
UpToDate Contents
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English Journal
- Gap junctions propagate opposite effects in normal and tumor testicular cells in response to cisplatin.
- Hong X, Wang Q, Yang Y, Zheng S, Tong X, Zhang S, Tao L, Harris AL.SourceDepartment of Pharmacology, Zhongshan School of Medicine, Sun Yat-Sen University, Guangzhou 510080, People's Republic of China.
- Cancer letters.Cancer Lett.2012 Apr 28;317(2):165-71. Epub 2011 Nov 22.
- Gap junctions propagate toxic effects among tumor cells during chemotherapy, but could also enhance killing of normal cells by the same mechanism. We show that the effect of gap junctional intercellular communication (GJIC) on cisplatin toxicity differs between normal and tumor testicular cells. Dow
- PMID 22115964
- Common Seed Analysis to Identify Off-Target Effects in siRNA Screens.
- Marine S, Bahl A, Ferrer M, Buehler E.Source1Department of Automated Biotechnology, Merck & Co. Inc., North Wales, Pennsylvania, USA.
- Journal of biomolecular screening.J Biomol Screen.2012 Mar;17(3):370-8. Epub 2011 Nov 15.
- Genome-scale small interfering RNA (siRNA) screens have become an increasingly popular approach to new target identification and pathway elucidation. However, the large data sets generated from siRNA screens have demonstrated high false-positive rates and the requirement for extensive experimental t
- PMID 22086724
- Autoreactive-Aβ antibodies promote APP β-secretase processing.
- Deng J, Hou H, Giunta B, Mori T, Wang YJ, Fernandez F, Weggen S, Araki W, Obregon D, Tan J.SourceRashid Laboratory for Developmental Neurobiology, Department of Psychiatry and Neurosciences, Morsani College of Medicine, University of South Florida, Tampa, Florida, USA Department of Neurology, Daping Hospital, Third Military Medical University, Chongqing, China Neuroimmunology Laboratory, Department of Psychiatry and Neurosciences, Morsani College of Medicine, University of South Florida, Tampa, Florida, USA Departments of Biomedical Sciences and Pathology, Saitama Medical Center and Saitama Medical University, Kawagoe, Saitama, Japan Department of Neuropathology, Heinrich-Heine-University, Düsseldorf, Germany Department of Demyelinating Disease and Aging, National Institute of Neuroscience, National Center of Neurology and Psychiatry, Kodaira, Tokyo, Japan James A. Haley Veterans' Hospital, Tampa, Florida, USA.
- Journal of neurochemistry.J Neurochem.2012 Mar;120(5):732-740. doi: 10.1111/j.1471-4159.2011.07629.x. Epub 2012 Jan 23.
- J. Neurochem. (2012) 120, 732-740. ABSTRACT: Several prior investigations of Alzheimer's disease (AD) patients have indicated naturally occurring autoantibodies against amyloid-β (Aβ) species are produced. Although many studies have focused on the relative concentrations or binding affinities of a
- PMID 22188568
Japanese Journal
- RNA-guided Cas9 nucleaseを用いたゲノム編集法の効率およびoff-target効果の検討 (第130回成医会総会一般演題)
- 創薬化学データペースReaxys Medicinal Chemistry(プロダクト・レビュー)
- 佐川 亜矢子
- 情報の科学と技術 63(10), 426-429, 2013-10-01
- エルゼビア社は,ライフサイエンス研究の上流から下流までサポートする様々なソリューションを提供しているが,今回新たに医薬品開発を効率化するデータベースとして,メディシナルケミスト向けのReaxys Medicinal Chemistryを開発した。これは反応・化合物データベースとして定評のあるReaxysからは独立した別のデータベースである。化合物情報としてReaxysの収録情報を一部活用し,さらに …
- NAID 110009636240
- プロダクト・レビュー 創薬化学データベースReaxys Medicinal Chemistry
- 佐川 亜矢子
- 情報の科学と技術 = The journal of Information Science and Technology Association 63(10), 426-429, 2013
- NAID 40019798537
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★リンクテーブル★
[★]
- 英
- nonspecific、non-specific、(遺伝子標的)off-target、unspecific、nonspecifically
- 関
- 非特異性、オフターゲット
[★]
- 関
- non-specific、nonspecifically、nonspecificity、off-target、unspecific
[★]
- 関
- nonspecific、nonspecifically、nonspecificity、off-target、unspecific
[★]
- 関
- non-specific、nonspecific、nonspecifically、off-target
[★]
- 関
- non-specific、nonspecific、off-target、unspecific
[★]
[★]
ターゲティング、標的指向化
[★]