5hi5

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Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists

Structural highlights

5hi5 is a 7 chain structure with sequence from Homo sapiens and Synthetic construct. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.8Å
Ligands:63Q, ACE
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

IL17_HUMAN Induces stromal cells to produce proinflammatory and hematopoietic cytokines. Enhances the surface expression of ICAM1/intracellular adhesion molecule 1 in fibroblasts.

Publication Abstract from PubMed

Interleukin-17A (IL-17A) is a principal driver of multiple inflammatory and immune disorders. Antibodies that neutralize IL-17A or its receptor (IL-17RA) deliver efficacy in autoimmune diseases, but no small-molecule IL-17A antagonists have yet progressed into clinical trials. Investigation of a series of linear peptide ligands to IL-17A and characterization of their binding site has enabled the design of novel macrocyclic ligands that are themselves potent IL-17A antagonists.

Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists.,Liu S, Dakin LA, Xing L, Withka JM, Sahasrabudhe PV, Li W, Banker ME, Balbo P, Shanker S, Chrunyk BA, Guo Z, Chen JM, Young JA, Bai G, Starr JT, Wright SW, Bussenius J, Tan S, Gopalsamy A, Lefker BA, Vincent F, Jones LH, Xu H, Hoth LR, Geoghegan KF, Qiu X, Bunnage ME, Thorarensen A Sci Rep. 2016 Aug 16;6:30859. doi: 10.1038/srep30859. PMID:27527709[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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See Also

References

  1. ↑ Liu S, Dakin LA, Xing L, Withka JM, Sahasrabudhe PV, Li W, Banker ME, Balbo P, Shanker S, Chrunyk BA, Guo Z, Chen JM, Young JA, Bai G, Starr JT, Wright SW, Bussenius J, Tan S, Gopalsamy A, Lefker BA, Vincent F, Jones LH, Xu H, Hoth LR, Geoghegan KF, Qiu X, Bunnage ME, Thorarensen A. Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists. Sci Rep. 2016 Aug 16;6:30859. doi: 10.1038/srep30859. PMID:27527709 doi:http://dx.doi.org/10.1038/srep30859

Contents


PDB ID 5hi5

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OCA

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