Publications by authors named "Yong-jun Cheng"
Identification of YCH2823 as a novel USP7 inhibitor for cancer therapy.
Biochem Pharmacol
April 2024
Article Synopsis
- Inhibition of USP7, a key enzyme regulating p53, is targeted as an effective anticancer strategy, leading to the development of a new potent inhibitor, YCH2823.
- YCH2823 shows up to 5 times greater efficacy than the previous compound FT671 against certain cancer cell lines, promoting p53 and p21 expression, causing cell cycle arrest and apoptosis.
- The drug's efficacy is reduced when p53 or p21 is knocked down, indicating their importance, and there is a potential for combined use with mTOR inhibitors in cancer therapy.
Inhibition of the NEDD8-activating enzyme (NAE), the key E1 enzyme in the neddylation cascade, has been considered an attractive anticancer strategy with the discovery of the first-in-class NAE inhibitor, MLN4924. In this study, we identified SOMCL-19-133 as a highly potent, selective, and orally available NAE inhibitor, which is an analog to AMP. It effectively inhibited NAE with an IC value of 0.
View Article and Find Full Text PDFBased on the reported synthetic lethality of the combination of PARP inhibitor olaparib with the natural product alantolactone, we designed several series of new PARP1 inhibitors by structurally merging both compounds into a single hybrid compound. Among them, compounds 20e and 25a displayed not only high biochemical activity (IC = 2.99 nM and 5.
View Article and Find Full Text PDFObjective: To investigate the characteristics of supracondylar fracture of humerus in children and to explore the effect of closed reduction and internal fixation at radial side on the fracture.
Methods: The children with fractures of Gartland type II and type III in our hospital from June 2010 to June 2013 were reviewed. There were 28 males and 7 females, ranging in age from 1 year and 1 month to 2 years and 6 months, with an average of 2 years and 1 month.
Objective: To detect the presence of antibodies to cyclic citrullinated peptides (anti-CCP) in patients with chronic hepatitis B virus (HBV) infection and evaluate its potential clinical significance.
Methods: Serum samples of 280 patients with chronic HBV infection and 40 healthy controls were collected from May 2011 to October 2011 and tested for anti-CCP and IgM-rheumatoid factor (RF). Anti-CCP was detected by ELISA and RF by immunonephelometry.
Aim: To investigate the effects of dendritic cells (DCs) transfected with full-length wild-type p53 and stimulated by gastric cancer lysates on immune response.
Methods: The wild-type p53 was transduced to DCs with adenovirus, and the DCs were stimulated by gastric cancer lysates. The surface molecules (B7-1, B7-2, MHC-I, MHC-II) of all DCs were detected by FACS, and the ability of the DCs to induce efficient and specific immunological response in anti-51Cr-labeled target cells was studied.