プロテアソーム阻害剤、プロテアソーム阻害薬

WordNet

limit, block, or decrease the action or function of; "inhibit the action of the enzyme"; "inhibit the rate of a chemical reaction"
control and refrain from showing; of emotions, desires, impulses, or behavior (同)bottle up, suppress
limit the range or extent of; "Contact between the young was inhibited by strict social customs"
a substance that retards or stops an activity

PrepTutorEJDIC

〈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』)》
抑制する人(物) / 化学反応抑制剤

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/02/03 12:37:27」(JST)

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Chemical structure of bortezomib, the first proteasome inhibitor approved for use.

Proteasome inhibitors are drugs that block the action of proteasomes, cellular complexes that break down proteins, like the p53 protein. Proteasome inhibitors are being studied in the treatment of cancer, especially multiple myeloma.

Examples[edit]

The first non-peptidic proteasome inhibitor discovered was the natural product lactacystin.^[1]

In 2003, bortezomib was the first proteasome inhibitor to be approved for use in the U.S.

Disulfiram has been proposed as another proteasome inhibitor.^[2]^[3]^[4]

Epigallocatechin-3-gallate has also been proposed.^[5]

Salinosporamide A has started clinical trials for multiple myeloma.

carfilzomib was approved by the FDA for relapsed and refractory multiple myeloma on 20 July 2012.

ONX 0912, CEP-18770, and MLN9708 have also started clinical trials.^[6]

Epoxomicin is a naturally-occurring selective inhibitor.^[7]

MG132 is a synthesized peptide commonly used for in vitro studies.

References[edit]

^ Fenteany G, Standaert RF, Lane WS, Choi S, Corey EJ, Schreiber SL. (1995). "Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin". Science 268: 726–31. doi:10.1126/science.7732382. PMID 7732382.
^ Lövborg H, Oberg F, Rickardson L, Gullbo J, Nygren P, Larsson R (March 2006). "Inhibition of proteasome activity, nuclear factor-KappaB translocation and cell survival by the antialcoholism drug disulfiram". International Journal of Cancer 118 (6): 1577–80. doi:10.1002/ijc.21534. PMID 16206267.
^ Wickström M, Danielsson K, Rickardson L, et al. (January 2007). "Pharmacological profiling of disulfiram using human tumor cell lines and human tumor cells from patients". Biochemical Pharmacology 73 (1): 25–33. doi:10.1016/j.bcp.2006.08.016. PMID 17026967.
^ Cvek B, Dvorak Z (August 2008). "The value of proteasome inhibition in cancer. Can the old drug, disulfiram, have a bright new future as a novel proteasome inhibitor?". Drug Discovery Today 13 (15-16): 716–22. doi:10.1016/j.drudis.2008.05.003. PMID 18579431.
^ Osanai K, Landis-Piwowar KR, Dou QP, Chan TH (August 2007). "A para-amino substituent on the D-ring of green tea polyphenol epigallocatechin-3-gallate as a novel proteasome inhibitor and cancer cell apoptosis inducer". Bioorg. Med. Chem. 15 (15): 5076–82. doi:10.1016/j.bmc.2007.05.041. PMC 2963865. PMID 17544279.
^ "Current Advances in Novel Proteasome Inhibitor–Based Approaches to the Treatment of Relapsed/Refractory Multiple Myeloma". 2011.
^ Meng, L. et al. (1999). "Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity". Proc. Natl. Acad. Sci. U.S.A 96: 10403–10408. doi:10.1073/pnas.96.18.10403. PMC 17900. PMID 10468620.

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UpToDate Contents

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1. 再発性または難治性多発性骨髄腫の治療 treatment of relapsed or refractory multiple myeloma
2. 非プラチナ製剤ベースの癌化学療法の神経学的合併症の概要 overview of neurologic complications of non platinum cancer chemotherapy
3. 資源の乏しい状況での多発性骨髄腫のマネージメント management of multiple myeloma in resource poor settings
4. 移植候補患者における症候性多発性骨髄腫に対する初期化学療法 selection of initial chemotherapy for symptomatic multiple myeloma
5. 多発性骨髄腫の治療プロトコル treatment protocols for multiple myeloma

English Journal

LB-1 Exerts Antitumor Activity in Pancreatic Cancer by Inhibiting HIF-1α and Stat3 Signaling.

Niu F1, Li Y1, Lai FF1, Ni L1, Ji M1, Jin J1, Yang HZ1, Wang C1, Zhang DM1, Chen XG1.
Journal of cellular physiology.J Cell Physiol.2015 Sep;230(9):2212-23. doi: 10.1002/jcp.24949.
Hypoxia is widely present in pancreatic cancer and subsequently causes the overexpression of hypoxia-inducible factor-1α (HIF-1α) and signal transducer and activator of transcription-3 (Stat3). HIF-1α and Stat3 function cooperatively to regulate a number of downstream genes that are implicated in
PMID 25655308

The capture proteasome assay: A method to measure proteasome activity in vitro.

Vigneron N1, Abi Habib J2, Van den Eynde BJ2.
Analytical biochemistry.Anal Biochem.2015 Aug 1;482:7-15. doi: 10.1016/j.ab.2015.04.019. Epub 2015 Apr 23.
Because of its crucial role in various cellular processes, the proteasome is the focus of intensive research for the development of proteasome inhibitors to treat cancer and autoimmune diseases. Here, we describe a new and easy assay to measure the different proteasome activities in vitro (chymotryp
PMID 25912419

The proteasome inhibitor Bortezomib (Velcade) as potential inhibitor of estrogen receptor-positive breast cancer.

Thaler S1, Thiede G1, Hengstler JG2, Schad A3, Schmidt M4, Sleeman JP1,5.
International journal of cancer. Journal international du cancer.Int J Cancer.2015 Aug 1;137(3):686-97. doi: 10.1002/ijc.29404. Epub 2015 Jan 8.
Around 70% of breast cancers express the estrogen receptor α (ERα) and depend on estrogen for growth, survival and disease progression. The presence of hormone sensitivity is usually associated with a favorable prognosis. Use of adjuvant anti-endocrine therapy has significantly decreased breast ca
PMID 25530422