SP4206

SP4206 is an experimental drug which is described as a small molecule protein-protein interaction inhibitor. It binds with high affinity to interleukin-2 at the precise residues which usually mediate binding between interleukin-2 and the IL-2 receptor, thereby preventing binding and blocking the action of interleukin-2 in the body. Interleukin-2 is a cytokine signalling molecule with an important role in the function of the immune system, and most medical interest has been in enhancing interleukin-2 activity for the treatment of cancer. However, it is also involved in some autoimmune disease processes, and blocking interleukin-2 activity with SP4206 has been researched for the treatment of atopic asthma, which is commonly associated with elevated interleukin-2 levels.^[1]^[2]^[3]^[4]^[5]

References

↑ "Hot-spot mimicry of a cytokine receptor by a small molecule". Proceedings of the National Academy of Sciences of the United States of America 103 (42): 15422–15427. October 2006. doi:10.1073/pnas.0607058103. PMID 17032757. Bibcode: 2006PNAS..10315422T.
↑ "Molecular modeling of the inhibition of protein–protein interactions with small molecules: The IL2–IL2Rα case". Chemical Physics Letters 517 (4–6): 217–222. 2011. doi:10.1016/j.cplett.2011.10.044. Bibcode: 2011CPL...517..217P.
↑ "Wrapping mimicking in drug-like small molecules disruptive of protein-protein interfaces". Proteins 80 (7): 1755–1765. July 2012. doi:10.1002/prot.24069. PMID 22422633.
↑ "Modulating Interleukins and their Receptors Interactions with Small Chemicals Using In Silico Approach for Asthma". Current Topics in Medicinal Chemistry 18 (13): 1123–1134. 2018. doi:10.2174/1568026618666180801092839. PMID 30068279.
↑ "How does a small molecule bind at a cryptic binding site?". PLOS Computational Biology 18 (3). March 2022. doi:10.1371/journal.pcbi.1009817. PMID 35239648. Bibcode: 2022PLSCB..18E9817S.

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[1] "Hot-spot mimicry of a cytokine receptor by a small molecule". Proceedings of the National Academy of Sciences of the United States of America 103 (42): 15422–15427. October 2006. doi:10.1073/pnas.0607058103. PMID 17032757. Bibcode: 2006PNAS..10315422T.

[2] "Molecular modeling of the inhibition of protein–protein interactions with small molecules: The IL2–IL2Rα case". Chemical Physics Letters 517 (4–6): 217–222. 2011. doi:10.1016/j.cplett.2011.10.044. Bibcode: 2011CPL...517..217P.

[3] "Wrapping mimicking in drug-like small molecules disruptive of protein-protein interfaces". Proteins 80 (7): 1755–1765. July 2012. doi:10.1002/prot.24069. PMID 22422633.

[4] "Modulating Interleukins and their Receptors Interactions with Small Chemicals Using In Silico Approach for Asthma". Current Topics in Medicinal Chemistry 18 (13): 1123–1134. 2018. doi:10.2174/1568026618666180801092839. PMID 30068279.

[5] "How does a small molecule bind at a cryptic binding site?". PLOS Computational Biology 18 (3). March 2022. doi:10.1371/journal.pcbi.1009817. PMID 35239648. Bibcode: 2022PLSCB..18E9817S.

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SP4206

Topic: Chemistry

References