Structure-optimized dihydropyranoindole derivative GIBH-LRA002 potentially reactivated viral latency in primary CD4+ T lymphocytes of chronic HIV-1 patients,RSC Medicinal Chemistry

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Structure-optimized dihydropyranoindole derivative GIBH-LRA002 potentially reactivated viral latency in primary CD4+ T lymphocytes of chronic HIV-1 patients
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-07-25 00:00:00 , DOI: 10.1039/c7md00327g
Qing Yang _{1,

2,

3,

4,

5} , Yuyang Ding _{1,

2,

3,

4,

6} , Fengling Feng _{1,

2,

3,

4,

7} , Enxiang Pan _{1,

2,

3,

4,

6} , Xiaozhen Fan _{1,

2,

3,

4,

7} , Xiuchang Ma _{1,

2,

3,

4} , Ling Chen _{1,

2,

3,

4,

5} , Junling Zhao _{8,

9,

10,

11,

12} , Caijun Sun _{1,

2,

3,

4}

Affiliation

Based on structure modification and a high-throughput Jurkat-Lat cell screening model, we found that GIBH-LRA002, ethyl-2-amino-3-cyano-9-methyl-4-(trifluoromethyl)-4,9-dihydropyrano[2,3-b]indole-4-carboxylate, effectively reactivated the latent proviruses in a Jurkat-Lat cell line and primary CD4+ T cells from both chronic SIV-infected rhesus macaques and HIV-1 patients but without inducing systemic activation, making this compound attractive for potentially treating HIV-1 infection.

中文翻译：

结构优化的二氢吡喃并吲哚衍生物GIBH-LRA002可能重新激活慢性HIV-1患者原发性CD4 + T淋巴细胞中的病毒潜伏期

基于结构修饰和高通量Jurkat-Lat细胞筛选模型，我们发现GIBH-LRA002，乙基-2-氨基-3-氰基-9-甲基-4-（三氟甲基）-4,9-二氢吡喃[2] ，3 - b ]吲哚-4-羧酸盐可有效地激活Jurkat-Lat细胞系和慢性SIV感染的猕猴和HIV-1患者的原代CD4 + T细胞中的潜伏原病毒，但不会诱导系统活化，因此使该化合物对潜在治疗HIV-1感染具有吸引力。

更新日期：2017-08-03

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