9mhw | pdb_00009mhw

Human TLR8 ectodomain with small molecule agonist 9

spinqualitylabelsall models 9mhw, resolution 1.52Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 9mhw is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 1.52Å Ligands: A1BLT, BMA, MAN, NAG, NI Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function TLR8_HUMAN Key component of innate and adaptive immunity. TLRs (Toll-like receptors) control host immune response against pathogens through recognition of molecular patterns specific to microorganisms. Acts via MYD88 and TRAF6, leading to NF-kappa-B activation, cytokine secretion and the inflammatory response. Publication Abstract from PubMed Dual activation of the TLR7 and TLR8 pathways leads to the production of type I interferon and proinflammatory cytokines, resulting in efficient antigen presentation by dendritic cells to promote T-cell priming and antitumor immunity. We developed a novel series of TLR7/8 dual agonists with varying ratios of TLR7 and TLR8 activity for use as payloads for an antibody-drug conjugate approach. The agonist-induced production of several cytokines in human whole blood confirmed their functional activity. Structure-activity relationship studies guided by structure-based drug design are described. Structure-Based Design of Novel TLR7/8 Agonist Payloads Enabling an Immunomodulatory Conjugate Approach.,Poudel YB, Lo JC, Norris DJ, Cox M, He L, Johnson WL, A M Subbaiah M, Mondal S, Thangavel S, Subramani L, Reddy M, Jain S, Weiss DR, Sivaprakasam P, Critton D, Mulligan D, Xie C, Dhar P, Li Y, Sega E, Yamazoe S, Gavai AV, Mathur A, Zapf CW, Chekler EP ACS Med Chem Lett. 2024 Dec 19;16(1):80-88. doi: 10.1021/acsmedchemlett.4c00463. , eCollection 2025 Jan 9. PMID:39811121 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

Proteopedia Page Contributors and Editors (what is this?)

OCA