2024
DOI: 10.1021/acs.jmedchem.3c02039
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Design, Synthesis, and Antitumor Activity Evaluation of Novel VISTA Small Molecule Inhibitors

Chengliang Sun,
Yuling He,
Gefei Wang
et al.

Abstract: VISTA (V-domain Ig suppressor of T cell activation) is a novel immune checkpoint protein and represents a promising target for cancer immunotherapy. Here, we report the design, synthesis, and evaluation of a series of methoxy-pyrimidinebased VISTA small molecule inhibitors with potent antitumor activity. By employing molecular docking and microscale thermophoresis (MST) assay, we identified a lead compound A1 that binds to VISTA protein with high affinity and optimized its structure. A4 was then obtained, whic… Show more

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Cited by 6 publications
(1 citation statement)
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“…Besides, the absence of in vivo pharmacokinetic and pharmacological experiments to directly ascertain the bioavailability and activity of curcumin derivatives posed a concern that would be addressed in our subsequent research. However, based on the literature reports, when combined with in vitro enzyme inhibition experiments and MST validation of the CADD screening results, this screening strategy had demonstrated a certain degree of efficient and reliable characteristics.…”
Section: Discussionmentioning
confidence: 99%
“…Besides, the absence of in vivo pharmacokinetic and pharmacological experiments to directly ascertain the bioavailability and activity of curcumin derivatives posed a concern that would be addressed in our subsequent research. However, based on the literature reports, when combined with in vitro enzyme inhibition experiments and MST validation of the CADD screening results, this screening strategy had demonstrated a certain degree of efficient and reliable characteristics.…”
Section: Discussionmentioning
confidence: 99%