A5103039409- Pharmacological Receptor Mechanisms and Effects
- Tryptophan and brain disorders
- Transgenic Plants and Applications
- Immune Cell Function and Interaction
- Bipolar Disorder and Treatment
- Cancer Immunotherapy and Biomarkers
- Toxin Mechanisms and Immunotoxins
- Dermatology and Skin Diseases
- CAR-T cell therapy research
China Pharmaceutical University
2024-2025
Inhibition of the PD-1/PD-L1 interaction through small-molecule inhibitors is a promising therapeutic approach in cancer immunotherapy. Herein, we utilized BMS-202 as lead compound to develop series novel with naphthyridin scaffold. Among these compounds, X14 displayed most potent inhibitory activity for (IC50 = 15.73 nM). Furthermore, exhibited good binding affinity both human PD-L1 (KD 14.62 nM) and mouse 392 In particular, showed favorable pharmacokinetic properties (oral bioavailability,...
Indoleamine 2,3-dioxygenase-1 (IDO1) plays a crucial role in tumor immune escape. However, the limited clinical efficacy of traditional IDO1 inhibitors has impeded their further development. Recently, apo-IDO1 that displace heme to target have been discovered, which exhibits slow dissociation rate reminiscent irreversible inhibitors. This characteristic suggests sustained engagement, offering pharmacodynamic advantage. Therefore, development emerges as promising strategy field IDO1-related...
Atopic dermatitis (AD) is a chronic, recurrent, and inflammatory skin condition that remains challenging to treat effectively safely with current therapies. Recent studies by multiple independent research groups have demonstrated poly(ADP-ribose) polymerase 14 (PARP14) has been implicated in the progression of diseases through its regulation Th2 Th17 signaling pathways, leading identification PARP14 as promising therapeutic target. Herein, we report discovery novel inhibitor Q22 exceptional...
CD73, an emerging immune checkpoint, plays a pivotal role in the adenosine (ADO) metabolic pathway by catalyzing conversion of AMP to ADO. This process has been shown inhibit functions T cells and natural killer (NK) cells, thereby exacerbating immunosuppressive effects within tumor microenvironment. These findings underscore critical CD73 modulating cell function represent promising therapeutic target for cancer treatment. Herein, series novel inhibitors featuring...