Selectivity of pyripyropene derivatives in inhibition toward acyl-CoA:cholesterol acyltransferase 2 isozyme.

Ohshiro T; Ohte S; Matsuda D; Ohtawa M; Nagamitsu T; Sunazuka T; Harigaya Y; Rudel LL; Omura S; Tomoda H

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Selectivity of pyripyropene derivatives in inhibition toward acyl-CoA:cholesterol acyltransferase 2 isozyme.

机译：吡y烯衍生物对酰基-CoA：胆固醇酰基转移酶2同工酶的抑制作用。

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Selectivity of 96 semisynthetic derivatives prepared from fungal pyripyropene A, originally isolated as a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), toward ACAT1 and ACAT2 isozymes was investigated in the cell-based assay using ACAT1- and ACAT2-expressing CHO cells. Eighteen derivatives including PR-71 (7-O-isocaproyl derivative) showed much more potent ACAT2 inhibition (IC50: 6.0 to 62 nM) than pyripyropene A (IC50: 70 nM). Among them, however, natural pyripyropene A showed the highest selectivity toward ACAT2 with a selectivity index (SI) of >1000, followed by PR-71 (SI, 667).

机译：在使用ACAT1和ACAT2的CHO细胞进行基于细胞的测定中，研究了最初作为酰基辅酶A：胆固醇酰基转移酶（ACAT）的一种有效抑制剂的真菌吡啶吡喃二烯A制备的96种半合成衍生物对ACAT1和ACAT2同工酶的选择性。。包括PR-71在内的18种衍生物（7-O-异己酰基衍生物）显示的ACAT2抑制作用（IC50：6.0至62 nM）比吡啶并戊二烯A（IC50：70 nM）强得多。但是，其中天然的吡啶并戊二烯A对ACAT2的选择性最高，选择性指数（SI）> 1000，其次是PR-71（SI，667）。

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《The Journal of Antibiotics: An International Journal》 |2008年第8期|共6页
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Ohshiro T; Ohte S; Matsuda D; Ohtawa M; Nagamitsu T; Sunazuka T; Harigaya Y; Rudel LL; Omura S; Tomoda H;
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1. Selectivity of pyripyropene derivatives in inhibition toward acyl-CoA:cholesterol acyltransferase 2 isozyme. [J] . Ohshiro T, Ohte S, Matsuda D, The Journal of Antibiotics: An International Journal . 2008,第8期

机译：吡y烯衍生物对酰基-CoA：胆固醇酰基转移酶2同工酶的抑制作用。
2. Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 2 [J] . OhtawaM., YamazakiH., MatsudaD., Bioorganic and Medicinal Chemistry Letters . 2013,第9期

机译：作为有效和选择性的酰基辅酶A：胆固醇酰基转移酶2（ACAT2）抑制剂的吡pyr烯A衍生物的合成及其构效关系：第2部分
3. Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 3 [J] . OhtawaM., YamazakiH., OhteS., Bioorganic and Medicinal Chemistry Letters . 2013,第13期

机译：作为有效和选择性的酰基辅酶A：胆固醇酰基转移酶2（ACAT2）抑制剂的吡pyr烯A衍生物的合成及其构效关系：第3部分
4. INSIGHTS INTO THE STRUCTURE AND function OF ACYL-CoA: DIACYLGLYCEROL ACYLTRANSFERASE [C] . RODRIGO M.P. SILOTO, QIN LIU, RANDALL J. WESELAKE, International Symposium on Biocatalysis and Biotechnology . 2010

机译：酰基 - CoA的结构和功能见解：二酰基甘油酰基转移酶
5. Mouse acyl-CoA binding protein: Effect on acyl-CoA utilization by microsomal acyl-CoA:cholesterol acyltransferase and membrane interactions. [D] . Chao, Hsu. 2002

机译：小鼠酰基辅酶A结合蛋白：微粒体酰基辅酶A：胆固醇酰基转移酶和膜相互作用对酰基辅酶A利用的影响。
6. Identification of the Interaction Site within Acyl-CoA:Cholesterol Acyltransferase 2 for the Isoform-specific Inhibitor Pyripyropene A [O] . Akash Das, Matthew A. Davis, Hiroshi Tomoda, 2008

机译：酰基辅酶A：胆固醇中相互作用位点的鉴定酰基转移酶2用于同工型特异性抑制剂Pyripyropene 一个
7. Identification of the Interaction Site within Acyl-CoA:Cholesterol Acyltransferase 2 for the Isoform-specific Inhibitor Pyripyropene A*S⃞ [O] . Das, Akash, Davis, Matthew A., Tomoda, Hiroshi, 2008

机译：酰基辅酶A：胆固醇中相互作用位点的鉴定酰基转移酶2用于同工型特异性抑制剂Pyripyropene A *S⃞
8. Imidazole Mediated Acylation of Cholesterol in Functional Vesicles: A Simple Analogue of Lecithin: Cholesterol Acyltransferase. [R] . Moss, R. A., Bhattacharya, S., Okumura, Y. 1989

机译：咪唑介导的功能性囊泡中胆固醇的酰化：卵磷脂的简单类似物：胆固醇酰基转移酶。

Selectivity of pyripyropene derivatives in inhibition toward acyl-CoA:cholesterol acyltransferase 2 isozyme.

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