1. Academic Validation
  2. Glyoxalase 1 inhibitor BBGC suppresses the progression of chronic lymphocytic leukemia and promotes the efficacy of Palbociclib

Glyoxalase 1 inhibitor BBGC suppresses the progression of chronic lymphocytic leukemia and promotes the efficacy of Palbociclib

  • Biochem Biophys Res Commun. 2023 Apr 2;650:96-102. doi: 10.1016/j.bbrc.2023.01.034.
Jiameng Tang 1 Jialing Zhong 1 Zheng Yang 1 Qisheng Su 1 Wuning Mo 2
Affiliations

Affiliations

  • 1 Department of Clinical Laboratory, First Affiliated Hospital of Guangxi Medical University, Guangxi Zhuang Autonomous Region, Nanning, 530000, China.
  • 2 Department of Clinical Laboratory, First Affiliated Hospital of Guangxi Medical University, Guangxi Zhuang Autonomous Region, Nanning, 530000, China. Electronic address: mown16300@126.com.
Abstract

Chronic lymphocytic leukemia (CLL) is a highly heterogeneous disease. Despite recent tremen-dous progress in managing CLL, the disease remains incurable with clinical therapies, and relapse is inevitable. To overcome this, new diagnostic and prognostic markers need to be investigated. We thus screened through the public database for genes with diagnostic, prognostic, and therapeutic implications in CLL. We further performed RT-qPCR and Western blot analysis to measure the candidate gene and protein expression levels, respectively, in peripheral blood mononuclear cells. Our results indicated that Glyoxalase 1 (GLO1) expression was significantly higher in patients with CLL than in healthy controls. Furthermore, cell proliferation, Apoptosis, and cell cycle assay results together indicated that S-p-bromobenzylglutathione cyclopentyl diester (BBGC), an effective inhibitor of GLO1, suppresses the progression of CLL. Bioinformatics analysis revealed that GLO1 expression is closely associated with CDK4 expression in a wide variety of Cancer types, and inhibition of CDK4 through silencing of genes or inhibitors can downregulate GLO1 expression. Subsequent validation experiments demonstrated that GLO1 protein levels were downregulated in MEC-1 and Jurkat cell lines after palbociclib exposure, and combination treatment of palbociclib with GLO1 inhibitor BBGC effectively delayed the growth of tumor cell lines.

Keywords

BBGC; CDK4; Chronic lymphocytic leukemia; GLO1; GLO1 inhibitor; Palbociclib.

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Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-50767
    99.94%, CDK4/6抑制剂
    CDK