non-competitive inhibitor

• 非競合的阻害薬、非競合的阻害剤

関

noncompetitive inhibitor

WordNet

1. used to express refusal or denial or disagreement etc or especially to emphasize a negative statement; "no, you are wrong"
2. a negative; "his no was loud and clear"
3. referring to the degree to which a certain quality is present; "he was no heavier than a child" (同)no more
4. not in any degree or manner; not at all; "he is no better today"
5. quantifier; used with either mass nouns or plural count nouns for indicating a complete or almost complete lack or zero quantity of; "we have no bananas"; "no eggs left and no money to buy any"; "have you no decency?"; "did it with no help"; "Ill get you there in no time"
6. limit, block, or decrease the action or function of; "inhibit the action of the enzyme"; "inhibit the rate of a chemical reaction"
7. control and refrain from showing; of emotions, desires, impulses, or behavior (同)bottle up, suppress
8. limit the range or extent of; "Contact between the young was inhibited by strict social customs"
9. showing a fighting disposition; "highly competitive sales representative"; "militant in fighting for better wages for workers"; "his self-assertive and ubiquitous energy" (同)militant
10. involving competition or competitiveness; "competitive games"; "to improve ones competitive position" (同)competitory
11. subscribing to capitalistic competition (同)free-enterprise, private-enterprise
12. a substance that retards or stops an activity

PrepTutorEJDIC

1. 《名詞の前に置いて》『一つも』(『一人も,少しも』)・・・『ない』 / 《補語につけて》『決して・・・でない』 / 《省略文で》・・・なし;・・・お断り / 《話》少ししか(あまり)・・・ない / (肯定の問いに対して)『いいえ』;(否定の問いに対して)はい,ええ / 《not, norの前に挿入して》『いや』,否 / 《形容詞の前に置その形容詞を否定して》…どころではない / 《比較級の前に置いて》ちっとも…でない,…と全く同じ / 《… or no の形で》…であってもなくても / 《驚き・困惑・不信などを表して》とんでもない / 《単数形で》『拒否』,「『いいえ』」という返事 / 《複数形で》反対[投]票
2. 〈感情・欲望・行動・作用など〉‘を'抑制する / (…しないように)〈人〉‘を'抑制する,妨げる《+『名』+『from』+『名』(do『ing』)》
3. 競争の,競争による
4. 抑制する人(物) / 化学反応抑制剤

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/08/15 07:35:23」(JST)

wiki en

[Wiki en表示]

"Non-competitive" redirects here. For other uses, see Competition.

Non-competitive inhibition is a type of enzyme inhibition where the inhibitor reduces the activity of the enzyme and binds equally well to the enzyme whether or not it has already bound the substrate.

If the inhibitor may bind to the enzyme whether or not the substrate has already been bound, but has a higher affinity for binding the enzyme in one state or the other, it is called a mixed inhibitor.

Terminology

It is important to note that, while all non-competitive inhibitors bind at allosteric sites-- i.e. any site on the enzyme other than its active site-- not all inhibitors that bind at allosteric sites are non-competitive inhibitors. In fact, allosteric inhibitors may act as competitive, non-competitive, or uncompetitive inhibitors.

Many sources continue to conflate these two terms, or state the definition of allosteric inhibition as the definition for non-competitive inhibition.

Mechanism

Illustration of a possible mechanism of non-competitive or mixed inhibition.

Non-competitive inhibition models a system where the inhibitor and the substrate may both be bound to the enzyme at any given time. When both the substrate and the inhibitor are bound, the enzyme-substrate-inhibitor complex cannot form product and can only be converted back to the enzyme-substrate complex or the enzyme-inhibitor complex. Non-competitive inhibition is distinguished from general mixed inhibition in that the inhibitor has an equal affinity for the enzyme and the enzyme-substrate complex.

The most common mechanism of non-competitive inhibition involves reversible binding of the inhibitor to an allosteric site, but it is possible for the inhibitor to operate via other means including direct binding to the active site. It differs from competitive inhibition in that the binding of the inhibitor does not prevent binding of substrate, and vice versa, it simply prevents product formation for a limited time.

This type of inhibition reduces the maximum rate of a chemical reaction without changing the apparent binding affinity of the catalyst for the substrate (K_m^app – see Michaelis-Menten kinetics).

Equation

In the presence of a non-competitive inhibitor, the apparent enzyme affinity is equivalent to the actual affinity. In terms of Michaelis-Menten kinetics, K_m^app = K_m. This can be seen as a consequence of Le Chatelier's Principle because the inhibitor binds to both the enzyme and the enzyme-substrate complex equally so that the equilibrium is maintained. However, since some enzyme is always inhibited from converting the substrate to product, the effective enzyme concentration is lowered.

Mathematically,

Example: noncompetitive inhibitors of CYP2C9 enzyme

Noncompetitive inhibitors of CYP2C9 enzyme include nifedipine, tranylcypromine, phenethyl isothiocyanate, and 6-hydroxyflavone. Computer docking simulation and constructed mutants substituted indicate that the noncompetitive binding site of 6-hydroxyflavone is the reported allosteric binding site of CYP2C9 enzyme.

References

1. Berg, Jeremy M.; Tymoczko, John L.; Stryer, Lubert (2000), Biochemistry (5th ed.), New York: WH Freeman & Co., ISBN 0-7167-6766-X 

UpToDate Contents

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English Journal

• Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors.

• Makhaeva GF1, Boltneva NP1, Lushchekina SV2, Serebryakova OG1, Stupina TS3, Terentiev AA3, Serkov IV1, Proshin AN1, Bachurin SO1, Richardson RJ4.
• Bioorganic & medicinal chemistry.Bioorg Med Chem.2016 Mar 1;24(5):1050-62. doi: 10.1016/j.bmc.2016.01.031. Epub 2016 Jan 18.
• A series of 31 N,N-disubstituted 2-amino-5-halomethyl-2-thiazolines was designed, synthesized, and evaluated for inhibitory potential against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and carboxylesterase (CaE). The compounds did not inhibit AChE; the most active compounds inhibited
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• Identification and characterization of potent, selective and metabolically stable IKKβ inhibitor.

• Kim D1, Kim YG1, Seo JH1, Shin KJ2.
• Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2016 Feb 15;26(4):1120-3. doi: 10.1016/j.bmcl.2016.01.065. Epub 2016 Jan 22.
• We have previously reported the identification of a rhodanine compound (1) with well-balanced inhibitory activity against IKKβ and collagen-induced TNFα activated cells. However, we need more optimized compounds because of its instability over plasma and microsome. As part of a program directed to
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• Inhibitory Effects of Triptolide on Human Liver Cytochrome P450 Enzymes and P-Glycoprotein.

• Zhang H1, Ya G2, Rui H3.
• European journal of drug metabolism and pharmacokinetics.Eur J Drug Metab Pharmacokinet.2016 Feb 13. [Epub ahead of print]
• BACKGROUND AND OBJECTIVES: Triptolide is an active component derived from Tripterygium wilfordii and it possesses numerous pharmacological activities. However, it remains unclear how triptolide influences the activity of human liver cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp).METHODS: In
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Japanese Journal

• Melanogenesis Inhibition by Gallotannins from Chinese Galls in B16 Mouse Melanoma Cells

• Chen Lih-Geeng,Chang Wei-Ling,Lee Chia-Jung,Lee Lain-Tze,Shih Chwen-Ming,Wang Ching-Chiung
• Biological & Pharmaceutical Bulletin 32(8), 1447-1452, 2009
• … By the mushroom tyrosinase inhibition kinetics assay, the three gallotannins were all determined to be non-competitive inhibitors. …
• NAID 130000117262

• Chebulagic Acid Is a Potent α-Glucosidase Inhibitor

• GAO Hong,HUANG Yi-Na,GAO Bo,KAWABATA Jun
• Bioscience, biotechnology, and biochemistry 72(2), 601-603, 2008-02-23
• … Chebulagic acid, isolated form Terminalia chebula Retz, proved to be a reversible and non-competitive inhibitor of maltase with a Ki value of 6.6 μM. …
• NAID 10027524884

Related Links

• Non-competitive inhibition - Wikipedia, the free encyclopedia

Non-competitive inhibition is a type of enzyme inhibition where the inhibitor reduces the activity of the enzyme and binds equally well to the enzyme whether or not it has already bound the substrate. If the inhibitor may bind to the enzyme ...

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★リンクテーブル★

リンク元	「非競合的阻害剤」「非競合的阻害薬」「noncompetitive inhibitor」
関連記事	「inhibit」「inhibitor」「competitive」「n」「competitive inhibitor」

「非競合的阻害剤」

　　[★]

英

noncompetitive inhibitor、non-competitive inhibitor

関

非競合的阻害薬

「非競合的阻害薬」

　　[★]

英

noncompetitive inhibitor、non-competitive inhibitor

関

非競合的阻害剤

「noncompetitive inhibitor」

　　[★]

• 非競合的阻害薬、非競合的阻害剤

関

non-competitive inhibitor

「inhibit」

　　[★]

• v.

• 抑制する、阻害する、阻止する

関

abrogate、block、depress、depression、deter、inhibition、interdict、prevent、prevention、repress、repression、restrain、restraint、suppress、suppression

　 　 　 　

「inhibitor」

　　[★]

• n.

• 阻害剤、阻害薬、抑制薬、抑制剤、(内在性物質について)インヒビター、抑制物質

関

blocker、depressant、suppressant

　 　

「competitive」

　　[★]

• 競合的な、競合性の、競合する、競争の

関

compete、competition、competitively、competitiveness、contest、rival

　 　 　 　

「n」

　　[★]

• n.

• 例数

関

number of experiment、sample size

• pの前の[n]はmと記載する。synptom→symptom

「competitive inhibitor」

　　[★]

• 競合的阻害薬、競合的阻害剤