
PARP-7药物靶点研发进展 - 知乎 - 知乎专栏
parp7是一种聚腺苷二磷酸核糖聚合酶,其作用是催化将adp-核糖的单个单位转移到底物上,从而改变其功能。 作为肿瘤细胞核酸感知的负调控因子,抑制PARP7在肿瘤模型中显示出恢复I型干扰素(IFN)信号通路对核酸的响应…
选择性PARP7抑制剂研发进展 - MedSci
2023年1月16日 · PARP7已被证明在肿瘤中过度活跃并在癌细胞存活中起关键作用,抑制PARP7可有效抑制癌细胞生长,恢复干扰素信号,有效防止癌细胞逃避免疫系统。 PARP7选择性抑制剂开发. 开发PARP7或其它PARPs选择性抑制剂的主要障碍,都是PARP催化中的高结构保守域;虽然序列同源性只有大约50%,但它们的结构是高度保守的,特别是在NAD+结合位点(大多数PARP抑制剂的主要结合位点)。 到目前为止,只有一个PARP7选择性抑制剂RBN-2397(图2)进入 …
PARP7 as a new target for activating anti-tumor immunity in cancer
2025年3月24日 · PARP7 promotes ovarian cancer growth and motility. PARP7 knockdown in OVCAR4 cells reduces their proliferation, as well as their migration and invasion (Palavalli Parsons et al, 2021) (Table 2). RNA-seq data analysis further revealed that depletion of PARP7 in OVCAR4 cells leads to the upregulation of genes associated with cell-cell adhesion ...
PARP抑制剂:抗癌突破不断,实体瘤克星 - 知乎
parp7 :助力肿瘤躲避免疫监测. monoparp蛋白家族在与癌症、炎性疾病和神经退行性疾病发展相关的多种应激反应中起作用,其成员parp7被证明在肿瘤中过度活跃,且在癌细胞生存中起着关键作用。
PARP7 and nucleic acid-driven oncosuppression
2024年6月4日 · PARP7 is a poorly investigated member of the poly (ADP-ribose) polymerase (PARP) protein family that has been shown to suppress type I IFN signaling in malignant cells by ensuring proficient DNA...
实体瘤新靶点!靶向新药PARP7抑制剂RBN-2397最新数据公布!
2023年3月20日 · rbn-2397是一款parp7抑制剂,用于治疗实体瘤。 临床前研究显示, RBN-2397能够通过抑制肿瘤细胞中的PARP7,直接抑制细胞增殖并恢复I型干扰素信号,以刺激先天性或适应性抗肿瘤免疫应答。
PARP7 negatively regulates the type I interferon response in …
2021年9月13日 · PARP7 is a monoPARP that catalyzes the transfer of single units of ADP-ribose onto substrates to change their function. Here, we identify PARP7 as a negative regulator of nucleic acid sensing in tumor cells. Inhibition of PARP7 restores type I interferon (IFN) signaling responses to nucleic acids in …
PARP-7药物靶点研发进展一览 - synapse.zhihuiya.com
2023年6月28日 · parp7是一种聚腺苷二磷酸核糖聚合酶,其作用是催化将adp-核糖的单个单位转移到底物上,从而改变其功能。 作为肿瘤细胞核酸感知的负调控因子,抑制PARP7在肿瘤模型中显示出恢复I型干扰素(IFN)信号通路对核酸的响应的效果。
Discovery of the Potent and Highly Selective PARP7 Inhibitor as a …
2022年12月28日 · PARP7, a polyadenosine diphosphate-ribose polymerase, has been identified as a negative regulator in type I interferon (IFN) signaling. An overexpression of PARP7 is typically found in a wide range of cancers and can lead to the suppression of type I IFN signaling and innate immune response.
Immunomodulatory roles of PARPs: Shaping the tumor …
2023年12月1日 · PARP7 inhibitors enhance STING-dependent IFN-I signaling in cancer cells that express PARP7. Two models are proposed for the mechanism of action of PARP7 inhibitors on IFN-I signaling. In one model, PARP7 inhibitors reverse PARP7 MARylation-dependent suppression of IFNβ transcription.