Drug insight: tumor necrosis factor-converting enzyme as a pharmaceutical target for rheumatoid arthritis.

Moss ML; Sklair-Tavron L; Nudelman R

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Drug insight: tumor necrosis factor-converting enzyme as a pharmaceutical target for rheumatoid arthritis.

机译：药物见解：肿瘤坏死因子转换酶作为类风湿关节炎的药物靶标。

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The success of agents that inhibit tumor necrosis factor (TNF), such as infliximab, adalimumab and etanercept, has led to a desire for orally available small molecules that have a better safety profile and are less costly to produce than current agents. One target for anti-TNF therapy that is currently under investigation is TNF-converting enzyme, which promotes the release of soluble TNF from its membrane-bound precursor. Inhibitors of this enzyme with drug-like properties have been made and tested in the clinic. These inhibitors include TMI-005 and BMS-561392, both of which have entered into phase II clinical trials. This article summarizes preclinical and clinical findings regarding the use of inhibitors of TNF-converting enzyme for the treatment of rheumatoid arthritis.

机译：抑制肿瘤坏死因子（TNF）的药物（例如英夫利昔单抗，阿达木单抗和依那西普）的成功，导致了对口服可用小分子的渴望，这种小分子的安全性好，生产成本比目前的药物低。目前正在研究的一种抗TNF治疗的靶标是TNF转换酶，它可以促进可溶性TNF从膜结合前体中释放出来。具有药物样特性的这种酶的抑制剂已经在临床上制备和测试。这些抑制剂包括TMI-005和BMS-561392，它们都已进入II期临床试验。本文总结了有关使用TNF转换酶抑制剂治疗类风湿关节炎的临床前和临床发现。

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《Nature clinical practice. Rheumatology》 |2008年第6期|共10页
作者
Moss ML; Sklair-Tavron L; Nudelman R;
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正文语种 eng
中图分类免疫性疾病;
关键词
Tumor Necrosis Factor; Enzymes; Rheumatoid Arthritis; inhibitors; Insight; NOS; 肿瘤坏死因子; 酶类;

机译：Tumor Necrosis Factor;Enzymes;Rheumatoid Arthritis;inhibitors;Insight;NOS;肿瘤坏死因子;酶类;

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1. Drug insight: tumor necrosis factor-converting enzyme as a pharmaceutical target for rheumatoid arthritis. [J] . Moss ML, Sklair-Tavron L, Nudelman R Nature clinical practice. Rheumatology . 2008,第6期

机译：药物见解：肿瘤坏死因子转换酶作为类风湿关节炎的药物靶标。
2. "Paradoxical" adverse effects caused by anti-tumor necrosis factor-alpha biological drugs: appearance of psoriasis in a patient treated with infliximab for rheumatoid arthritis. [J] . Satriano RA, Abbate G, Esposito S, Indian journal of dermatology, venereology and leprology . 2011,第4期

机译：由抗肿瘤坏死因子-α生物药物引起的“偏头痛”副作用：在用英夫利昔单抗治疗的类风湿性关节炎患者中出现牛皮癣。
3. Targeting cytokines beyond tumor necrosis factor-alpha and interleukin-1 in rheumatoid arthritis. [J] . McInnes IB, Gracie JA Current pain and headache reports. . 2005,第6期

机译：在类风湿关节炎中靶向肿瘤坏死因子-α和白介素-1以外的细胞因子。
4. Effect of Excipients on Lag Time of Press Coated Tablets in Pulsatile Drug Delivery For The Treatment of Rheumatoid Arthritis. [C] . Deepali V. Kaduskar, Bala Prabhakar Annual meeting exposition of the Controlled Release Society . 2010

机译：赋形剂对治疗类风湿关节炎的脉冲药物递送中压制包衣片的延迟时间的影响。
5. Kinetic characterization of protein arginine deiminase 4: An enzyme dysregulated in rheumatoid arthritis. [D] . Bhatia, Monica. 2007

机译：精氨酸脱亚氨酶4的动力学表征：类风湿关节炎中失调的一种酶。
6. Functional analysis of a human tumor necrosis factor alpha (TNF-alpha) promoter polymorphism related to joint damage in rheumatoid arthritis. [O] . E. L. Kaijzel, M. V. van Krugten, B. M. Brinkman, 1998

机译：类风湿关节炎的关节损伤相关的人类肿瘤坏死因子α（TNF-alpha）启动子多态性的功能分析。
7. Identification and characterization of 4-4-(2-butynyloxy)phenylsulfonyl-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis. [O] . Zhang Y, Xu J, Levin J, 2004

机译：新型双肿瘤坏死因子-α-转化的4-4-（2-丁炔氧基）苯基磺酰基 -N-羟基-2,2-二甲基-（3S）硫吗啉羧酰胺（TMI-1）的鉴定与表征酶/基质金属蛋白酶抑制剂，用于治疗类风湿关节炎。

Drug insight: tumor necrosis factor-converting enzyme as a pharmaceutical target for rheumatoid arthritis.

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