更新于：2024-11-21

Y-22

更新于：2024-11-21

概要

研发状态

概要

基本信息

药物类型

小分子化药

别名

靶点

ABCG2 x P-gp

作用机制

ABCG2抑制剂(ATP结合盒转运子亚家族G成员2抑制剂)、P-gp抑制剂(P-糖蛋白-1抑制剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构

中国药科大学

在研机构

中国药科大学

非在研机构-

最高研发阶段药物发现

首次获批日期-

最高研发阶段(中国)药物发现

特殊审评-

结构

分子式C37H38F3N7O2

InChIKeyQROHMVUFPPQUNN-UHFFFAOYSA-N

CAS号2848632-97-1

关联

100 项与 Y-22 相关的临床结果

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100 项与 Y-22 相关的转化医学

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100 项与 Y-22 相关的专利（医药）

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项与 Y-22 相关的文献（医药）

2023-02-23·Journal of Medicinal Chemistry1区 · 医学

Imidazo[1,2-a]Pyridine Derivatives as Novel Dual-Target Inhibitors of ABCB1 and ABCG2 for Reversing Multidrug Resistance

1区 · 医学

Article

作者: Zheng, Wei ; Xu, Xiao-Li ; You, Qi-Dong ; Jia, Yan-Han ; Li, Qian ; Chen, Ya-Qiong ; Feng, Zi-Wen ; Zhang, Sheng-Lie ; Li, Hui ; Zhou, Ye-Ling ; Li, Lin-Lin ; Zhang, Shi-Duo ; Liu, Xue-Chun ; Peng, Hui

ABCB1 and ABCG2 are the important ATP-binding cassette (ABC) transporters associated with multidrug resistance (MDR). Herein, we designed a series of imidazo[1,2-a]pyridine derivatives as dual-target inhibitors of ABCB1 and ABCG2 through the scaffold hopping strategy. Compound Y22 displayed potential efflux function inhibitory toward both ABCB1 and ABCG2 (reversal fold: ABCB1 = 8.35 and ABCG2 = 2.71) without obvious cytotoxicity. Y22 also enhanced the potency of antiproliferative drugs in vitro. Mechanistic studies demonstrated that Y22 slightly suppressed ATPase activity but did not affect the protein expression of ABCB1 or ABCG2. Notably, Y22 exhibited negligible CYP3A4 inhibition and enhanced the antiproliferative activity of adriamycin in vivo by restoring the sensitivity of resistant cells. Thus, Y22 may be effective clinically in combination with common chemotherapy agents. In summary, Y22 is a potential dual-target inhibitor that reverses MDR by blocking the efflux function of ABCB1 and ABCG2.

2019-12-01·BMC Plant Biology2区 · 生物学

The wild sweetpotato (Ipomoea trifida) genome provides insights into storage root development

2区 · 生物学

ArticleOA

作者: Feng, Junyan ; Lin, Honghui ; Xu, Wei ; Wang, Kai ; Wang, Zhangying ; Du, Chunguang ; Lin, Feng ; Peng, Meifang ; Tan, Wenfang ; Li, Yan ; Zhang, Cong ; Yang, Songtao ; Yang, Huan ; Zhang, Yizheng ; Li, Ji ; Liao, Anzhong ; Zou, Hongda ; Song, Wei ; Zhang, Lei ; Wei, Changhe ; Li, Ming ; Zhang, Jinbo ; Pu, Zhigang ; Qiao, Shuai ; Zhang, Zhongren

BACKGROUNDSweetpotato (Ipomoea batatas (L.) Lam.) is the seventh most important crop in the world and is mainly cultivated for its underground storage root (SR). The genetic studies of this species have been hindered by a lack of high-quality reference sequence due to its complex genome structure. Diploid Ipomoea trifida is the closest relative and putative progenitor of sweetpotato, which is considered a model species for sweetpotato, including genetic, cytological, and physiological analyses.RESULTSHere, we generated the chromosome-scale genome sequence of SR-forming diploid I. trifida var. Y22 with high heterozygosity (2.20%). Although the chromosome-based synteny analysis revealed that the I. trifida shared conserved karyotype with Ipomoea nil after the separation, I. trifida had a much smaller genome than I. nil due to more efficient eliminations of LTR-retrotransposons and lack of species-specific amplification bursts of LTR-RTs. A comparison with four non-SR-forming species showed that the evolution of the beta-amylase gene family may be related to SR formation. We further investigated the relationship of the key gene BMY11 (with identity 47.12% to beta-amylase 1) with this important agronomic trait by both gene expression profiling and quantitative trait locus (QTL) mapping. And combining SR morphology and structure, gene expression profiling and qPCR results, we deduced that the products of the activity of BMY11 in splitting starch granules and be recycled to synthesize larger granules, contributing to starch accumulation and SR swelling. Moreover, we found the expression pattern of BMY11, sporamin proteins and the key genes involved in carbohydrate metabolism and stele lignification were similar to that of sweetpotato during the SR development.CONCLUSIONSWe constructed the high-quality genome reference of the highly heterozygous I. trifida through a combined approach and this genome enables a better resolution of the genomics feature and genome evolutions of this species. Sweetpotato SR development genes can be identified in I. trifida and these genes perform similar functions and patterns, showed that the diploid I. trifida var. Y22 with typical SR could be considered an ideal model for the studies of sweetpotato SR development.

2018-02-01·World Journal of Microbiology and Biotechnology4区 · 工程技术

Oil-degrading properties of a psychrotolerant bacterial strain, Rhodococcus sp. Y2-2, in liquid and soil media

4区 · 工程技术

Article

作者: Chaudhary, Dhiraj Kumar ; Kim, Jaisoo ; Van Hong Thi Pham ; Jeong, Seung-Woo

The aim of this study was to investigate oil-degrading ability of newly isolated strain Rhodococcus Y2-2 at low temperature. Rhodococcus sp. Y2-2 was isolated from oil-contaminated soil sampled at the end of winter using a newly developed transwell plate method. In the liquid phase, the oil-degradation efficiency of strain Rhodococcus sp. Y2-2 was about 84% with an initial concentration of 1500 ppm TPH (500 ppm each of kerosene, gasoline, and diesel) when incubated for 2 weeks under optimal conditions: 10 °C, pH 7, and 0.5 g L^- 1 inoculum. In the soil phase, the isolate showed 80% oil degradation efficiency using glucose as a carbon source, with an initial concentration of 4000 ppm TPH and the addition of water during 14 days of incubation at 10 °C. Additionally, the degradation efficiency of the isolate was increased by the addition of mixture of surfactant alpha olefin sulfonate and gelatin, although strain Y2-2 also produced many biosurfactant components. This study shows Rhodococcus sp. Y2-2 can degrade oil components both in liquid and soil media by consuming kerosene, gasoline, and diesel as a carbon and energy source. Therefore, the crude oil-degrading ability of Rhodococcus sp. Y2-2 at low temperature provides proper bioremediation tool to clean up oil-contaminated sites especially in cold area or during winter season.

100 项与 Y-22 相关的药物交易

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