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Farnesyltransferase Inhibitors: From Squalene Synthase Inhibitors to the Clinical Agent BMS-214662

机译：法呢基转移酶抑制剂：从Squalene合酶抑制剂到临床药物BMS-214662

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We have discovered a number of distinct classes of inhibitors of the enzyme farnesyltransferase, an attractive new therapeutic target in oncology. The inhibitor classes include ones that are farnesylpyrophosphate-based, bisubstrates, thiol- and imidazole-based tetrapeptides, imidazole-based dipeptides and ultimately imidazole-based tetrahydrobenzodiazepines. The latter class yielded (R)-7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenmylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), which has entered clinical trials.

机译：我们已经发现了许多不同的酶法抑制剂类抑制剂，肿瘤学中有吸引力的新治疗靶标。抑制剂类别包括法氧杂磷酸磷酸酯的，基于Bisubstres，基于咪唑基的四肽，基于咪唑基的二肽，最终基于咪唑基的四氢苯并二氮杂噻嗪。后一种类得到（R）-7-氰基-2,3,4,5-四氢-1-（1H-咪唑-4-基甲基）-3-（Phenmylmethyl甲基）-4-（2-噻吩基磺酰基）-1H- 1,4-苯二氮卓（BMS-214662），已进入临床试验。

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《American Chemical Society》|2001年||共15页
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John T. Hunt;
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1. Enautioselective Synthesis of α-Phosphono Sulfonate Squalene Synthase Inhibitors: Chiral Recognition in the Interactions of an a-Phosphono Sulfonate Inhibitor with Squalene Synthase [J] . R. Michael Lawrence, Scott A. Biller, John K. Dickson Jr., Journal of the American Chemical Society . 1996,第46期

机译：α-膦磺酸角鲨烯合酶抑制剂的对映选择性合成：α-磺酸磺酸盐抑制剂与角鲨烯合酶相互作用的手性识别
2. RPR 107393, a potent squalene synthase inhibitor and orally effective cholesterol-lowering agent: comparison with inhibitors of HMG-CoA reductase. [J] . Amin D, Rutledge RZ, Needle SN, The Journal of Pharmacology and Experimental Therapeutics: Official Publication of the American Society for Pharmacology and Experimental Therapeutics . 1997,第2期

机译：RPR 107393，一种有效的角鲨烯合酶抑制剂和口服有效的降胆固醇剂：与HMG-CoA还原酶抑制剂的比较。
3. Ethyl methanesulphonate in a parenteral formulation of BMS-214662 mesylate, a selective farnesyltransferase inhibitor: formation and rate of hydrolysis. [J] . Nassar MN, Cucolo M, Miller SA Pharmaceutical development and technology . 2009,第6期

机译：选择性磺基法呢基转移酶抑制剂BMS-214662甲磺酸盐的肠胃外制剂中的甲磺酸乙酯：水解的形成和速率。
4. Farnesyltransferase Inhibitors: From Squalene Synthase Inhibitors to the Clinical Agent BMS-214662 [C] . John T. Hunt American Chemical Society . 2001

机译：法呢基转移酶抑制剂：从Squalene合酶抑制剂到临床药物BMS-214662
5. Development of farnesyltransferase and geranylgeranyltransferase-I inhibitors as potential antimalarial and anticancer agents. [D] . Pusateri, Erin E. 2006

机译：法呢基转移酶和香叶基香叶基转移酶-I抑制剂作为潜在的抗疟药和抗癌药的开发。
6. Partial blockage of sterol biosynthesis with a squalene synthase inhibitor in early postnatal Niemann-Pick type C npcnih null mice brains reduces neuronal cholesterol accumulation abrogates astrogliosis but may inhibit myelin maturation [O] . Patrick C. Reid, Song Lin, Marie T. Vanier, -1

机译：在出生后早期的Niemann-Pick C型npcnih无效小鼠的大脑中使用角鲨烯合酶抑制剂部分固醇生物合成可减少神经元胆固醇的积聚消除星形胶质变但可能会抑制髓磷脂的成熟
7. Effect of ER-27856, a novel squalene synthase inhibitor, on plasma cholesterol in rhesus monkeys: comparison with 3-hydroxy-3-methylglutaryl-CoA reductase inhibitors [O] . Hironobu Hiyoshi, Mamoru Yanagimachi, Masashi Ito, 2000

机译：ER-27856，一种新型角鲨烯合酶抑制剂，对岩浆中的血浆胆固醇的影响：与3-羟基-3-甲基戊族-CoA还原酶抑制剂的比较
8. Elucidating Mechanisms of Farnesyltransferase Inhibitor Action and Resistance in Breast Cancer by Bioluminescence Imaging [R] . Piwnica-Worms, D. 2010

机译：生物发光成像法研究法尼基转移酶抑制剂在乳腺癌中的作用及耐药机制

Farnesyltransferase Inhibitors: From Squalene Synthase Inhibitors to the Clinical Agent BMS-214662

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