WordNet

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
use recreational drugs (同)do drugs
administer a drug to; "They drugged the kidnapped tourist" (同)dose
a substance that is used as a medicine or narcotic

PrepTutorEJDIC

(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
『薬』,薬品,薬剤 / 『麻薬』,麻酔剤 / 〈人〉‘に'薬(特に麻酔剤)を与える / 〈飲食物〉‘に'(麻酔薬・毒薬などの)薬を混ぜる

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/11/29 20:33:30」(JST)

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A biological target is anything within a living organism to which some other entity, like an endogenous ligand or a drug is directed and/or binds. Examples of common classes of biological targets are proteins and nucleic acids. The definition is context-dependent and can refer to the biological target of a pharmacologically active drug compound, the receptor target of a hormone (like insulin), or some other target of an external stimulus. The implication is that a target is "hit" by a signal and its behavior or function is then changed. Biological targets are most commonly proteins such as enzymes, ion channels, and receptors.

Mechanism

The external stimulus (i.e., chemical substance) physically binds to the biological target.^[1]^[2] The interaction between the substance and the target may be:

noncovalent – A relatively weak interaction between the stimulus and the target where no chemical bond is formed between the two interacting partners and hence the interaction is completely reversible.
reversible covalent - A chemical reaction occurs between the stimulus and target in which the stimulus becomes chemically bonded to the target, but the reverse reaction also readily occurs in which the bond can be broken.
irreversible covalent - The stimulus is permanently bound to the target through irreversible chemical bond formation.

Depending on the nature of the stimulus, the following can occur:^[3]

There is no direct change in the biological target, except that the binding of the substance prevents other endogenous substances such as activating hormone to bind to the target. Depending on the nature of the target, this effect is referred as receptor antagonism, enzyme inhibition, or ion channel blockade.
A conformational change in the target is induced by the stimulus which results in a change in target function. This change in function can mimic the effect of the endogenous substance in which case the effect is referred to as receptor agonism (or channel or enzyme activation) or be the opposite of the endogenous substance which in the case of receptors is referred to as inverse agonism.

Drug targets

The term biological target is frequently used in pharmaceutical research to describe the native protein in the body whose activity is modified by a drug resulting in a specific effect, which may be a desirable therapeutic effect or an unwanted adverse effect. In this context, the biological target is often referred to as a drug target. The most common drug targets of currently marketed drugs include:^[4]^[5]^[6]

proteins
- G protein-coupled receptors (target of 50% of drugs)^[7]
- enzymes (especially protein kinases, proteases, esterases, and phosphatases)
- ion channels
  - ligand-gated ion channels
  - voltage-gated ion channels
- nuclear hormone receptors
- structural proteins such as tubulin
- membrane transport proteins
nucleic acids

Drug target identification

Identifying the biological origin of a disease, and the potential targets for intervention, is the first step in the discovery of a medicine. This has been a great challenge for both academia and industry. Number of different approaches and technologies are reviewed.^[8]

Databases

Databases containing biological targets information:

Therapeutic Targets Database (TTD)
DrugBank
Binding DB

References

^ Raffa RB, Porreca F (1989). "Thermodynamic analysis of the drug-receptor interaction". Life Sci. 44 (4): 245–58. doi:10.1016/0024-3205(89)90182-3. PMID 2536880.
^ Moy VT, Florin EL, Gaub HE (1994). "Intermolecular forces and energies between ligands and receptors". Science 266 (5183): 257–9. doi:10.1126/science.7939660. PMID 7939660.
^ Rang HP, Dale MM, Ritter JM, Flower RJ, Henderson G (2012). "Chapter 3: How drugs act: molecular aspects". Rang and Dale's Pharmacology. Edinburgh; New York: Elsevier/Churchill Livingstone. pp. 20–48. ISBN 0-7020-3471-1.
^ Rang HP, Dale MM, Ritter JM, Flower RJ, Henderson G (2012). "Chapter 2: How drugs act: general principles". Rang and Dale's Pharmacology. Edinburgh; New York: Elsevier/Churchill Livingstone. pp. 6–19. ISBN 0-7020-3471-1.
^ Overington JP, Al-Lazikani B, Hopkins AL (2006). "How many drug targets are there?". Nat Rev Drug Discov 5 (12): 993–6. doi:10.1038/nrd2199. PMID 17139284.
^ Landry Y, Gies JP (2008). "Drugs and their molecular targets: an updated overview". Fundam Clin Pharmacol. 22 (1): 1–18. doi:10.1111/j.1472-8206.2007.00548.x. PMID 18251718.
^ Lundstrom K (2009). "An overview on GPCRs and drug discovery: structure-based drug design and structural biology on GPCRs". Methods Mol. Biol. 552: 51–66. doi:10.1007/978-1-60327-317-6_4. PMID 19513641.
^ Lomenick, Brett; Olsen, Richard W.; Huang, Jing (21 January 2011). "Identification of Direct Protein Targets of Small Molecules". ACS Chemical Biology 6 (1): 34–46. doi:10.1021/cb100294v.

UpToDate Contents

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1. 抗マラリア剤：概要 antimalarial drugs an overview
2. Drug-induced thrombotic microangiopathy
3. 薬物アレルギー患者へのアプローチ an approach to the patient with drug allergy
4. リウマチ性疾患における免疫抑制剤および疾患修飾剤の使用の概要 overview of the use of immunosuppressive and disease modifying drugs in the rheumatic diseases
5. 成人における薬物中毒への一般的アプローチ general approach to drug poisoning in adults

English Journal

Inhibition of cell growth and up-regulation of MAD2 in human oesophageal squamous cell carcinoma after treatment with the Src/Abl inhibitor dasatinib.

Wang L, Guo B, Wang R, Jiang Y, Qin S, Liang S, Zhao Y, Guo W, Li K, Fan X.Source*Thoracic Surgery Center, Institute of Surgery Research, Daping Hospital, Third Military Medical University, Chongqing 400042, China.
Clinical science (London, England : 1979).Clin Sci (Lond).2012 Jan 1;122(1):13-24.
Aberrant expression and/or activity of the non-receptor protein tyrosine kinase SFK (Src family kinase) members are commonly observed in progressive stages of human tumours. The aim of the present study was to investigate whether Src is a potential drug target for treating oesophageal squamous cell
PMID 21751967

Integrin-Targeted Nanoparticles for siRNA Delivery.

Ben-Arie N, Kedmi R, Peer D.SourceLaboratory of Nanomedicine, Department of Cell Research and Immunology, George S. Wise Faculty of Life Sciences, Tel Aviv University, Tel Aviv, Israel.
Methods in molecular biology (Clifton, N.J.).Methods Mol Biol.2012;757:497-507.
Integrins are heterodimeric membrane glycoproteins composed of noncovalently associated α and β subunits. Integrins support cell attachment and migration on the surrounding extracellular matrix as well as mediate cell-cell interaction in physiological and pathological settings. Constant recycling
PMID 21909930

Japanese Journal

GISTに対する分子標的薬の開発 (特集ドライバー変異陽性がんを含む希少がんに対する分子標的治療の開発戦略)

小松嘉人
腫瘍内科 = Clinical oncology 15(4), 397-401, 2015-04
NAID 40020458441

悪性黒色腫に対する分子標的治療薬の開発 (特集ドライバー変異陽性がんを含む希少がんに対する分子標的治療の開発戦略)

山﨑直也
腫瘍内科 = Clinical oncology 15(4), 356-362, 2015-04
NAID 40020458382

3. 分子標的薬による自己免疫疾患治療(XVII. 免疫・アレルギー疾患の分子標的,専門医のためのアレルギー学講座)

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アレルギー 64(2), 97-102, 2015-03-01
NAID 110009917669

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★リンクテーブル★

リンク元	「創薬標的」「創薬ターゲット」「薬物標的」「薬物ターゲット」「ドラッグターゲット」
拡張検索	「potential drug target」「drug target discovery」
関連記事	「target」「targeting」「drug」