Publications by authors named "Chenxia Gao"

Article Synopsis
  • Researchers are developing allosteric inhibitors as potential hypoglycemic drugs targeting the enzyme PTP1B to fight diabetes mellitus.
  • These inhibitors work by occupying a specific hydrophobic site (BB site) on PTP1B, keeping a loop in an open position, which prevents the enzyme from performing its normal dephosphorylation functions.
  • One impressive compound, LXQ-87, shows promise by effectively lowering blood glucose levels and enhancing glucose tolerance in diabetic mice while also improving insulin resistance.
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Traditional Chinese medicines (TCMs) are highly valued and widely used worldwide. However, their complex compositions and various preparation processes have brought considerable challenges to the quality evaluation of Chinese medicines. The traditional methods for TCM quality evaluation suffer from the problems of cumbersome sample preparation, a long detection time, low sensitivity, A more efficient and accurate evaluation method is urgently needed to ensure the stability and reliability of the quality of TCMs.

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Designing selective PARP-1 inhibitors has become a new strategy for anticancer drug development. By sequence comparison of PARP-1 and PARP-2, we identified a possible selective site (S site) consisting of several different amino acid residues of α-5 helix and D-loop. Targeting this S site, 140 compounds were designed, synthesized, and characterized for their anticancer activities and mechanisms.

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Article Synopsis
  • * PARP inhibitors, such as olaparib and niraparib, are designed to target DNA-damage repair pathways, but their clinical use is limited due to hematological toxicities from inhibiting PARP-1 and PARP-2 together.
  • * The review emphasizes the importance of developing selective PARP-1 inhibitors and discusses recent advances in design strategies that leverage structural insights and computer simulations to improve their effectiveness.
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Metal ions are indispensable elements in living organisms and are associated with regulating various biological processes. An imbalance in metal ion content can lead to disorders in normal physiological functions of the human body and cause various diseases. Genetically encoded fluorescent protein sensors have the advantages of low biotoxicity, high specificity, and a long imaging time and have become a powerful tool to visualize or quantify the concentration level of biomolecules and , temporal and spatial distribution, and life activity process.

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