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Pyrazines

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Linsitinib inhibits proliferation and induces apoptosis of both IGF-1R and TSH-R expressing cells.

Frontiers in immunology
BACKGROUND: The insulin-like growth factor 1 receptor (IGF-1R) and the thyrotropin receptor (TSH-R) are expressed on orbital cells and thyrocytes. These receptors are targeted in autoimmune-induced thyroid eye disease (TED). Effective therapeutic tre...

Correcting the impact of docking pose generation error on binding affinity prediction.

BMC bioinformatics
BACKGROUND: Pose generation error is usually quantified as the difference between the geometry of the pose generated by the docking software and that of the same molecule co-crystallised with the considered protein. Surprisingly, the impact of this e...

Optimal extraction bioactive components of tetramethylpyrazine in Chinese herbal medicine jointly using back propagation neural network and genetic algorithm in R language.

Pakistan journal of pharmaceutical sciences
A combinational approach of back propagation neural network (BPNN) and genetic algorithm (GA) was proposed in the present study to optimize the extraction technology of tetramethylpyrazine (TMP) in Ligusticum wallichii Franchat. Based on the single f...

Deep learning-based design and screening of benzimidazole-pyrazine derivatives as adenosine A receptor antagonists.

Journal of biomolecular structure & dynamics
The Adenosine A receptor (AAR) is considered a novel potential target for the immunotherapy of cancer, and AAR antagonists have an inhibitory effect on tumor growth, proliferation, and metastasis. In our previous studies, we identified a class of ben...

Antivirals for monkeypox virus: Proposing an effective machine/deep learning framework.

PloS one
Monkeypox (MPXV) is one of the infectious viruses which caused morbidity and mortality problems in these years. Despite its danger to public health, there is no approved drug to stand and handle MPXV. On the other hand, drug repurposing is a promisin...

Determination of Novel SARS-CoV-2 Inhibitors by Combination of Machine Learning and Molecular Modeling Methods.

Medicinal chemistry (Shariqah (United Arab Emirates))
INTRODUCTION: Within the scope of the project, this study aimed to find novel inhibitors by combining computational methods. In order to design inhibitors, it was aimed to produce molecules similar to the RdRp inhibitor drug Favipiravir by using the ...