Synonyms: IL-17 modulator 4
Compound class:
Synthetic organic
Comment: This is a small synthetic molecule that has been demonstrated to disrupt the interaction between the two monomer peptides of the functional interleukin 17A (IL-17A) homodimer (IL-17AA) [1]. Compound 23 was designed as an orally bioavailable agent, for potential to disrupt IL-17A signalling via the IL-17 receptor (principally the IL-17RA/IL-17RC heterodimer), to induce an anti-inflammatory effect in diseases like psoriasis, which are driven by abnormally high IL-17AA expression levels. The 3D structure of compound 23 in complex with the human IL-17AA dimer has been resolved by X-ray crystallography (PDB ID 7AMA). The chemical and physical properties of compound 23 satisfy Lipinski's rule of five for druglikeness [2].
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References |
1. Andrews MD, Dack KN, de Groot MJ, Lambert M, Sennbro CJ, Larsen M, Stahlhut M. (2022)
Discovery of an Oral, Rule of 5 Compliant, Interleukin 17A Protein-Protein Interaction Modulator for the Potential Treatment of Psoriasis and Other Inflammatory Diseases. J Med Chem, 65 (13): 8828-8842. [PMID:35767390] |
2. Lipinski CA. (2004)
Lead- and drug-like compounds: the rule-of-five revolution. Drug Discov Today Technol, 1 (4): 337-41. [PMID:24981612] |