The transmembrane activator and cyclophilin ligand interactor (TACI) receptor regulates the adaptive immune system and is involved in B-cell biology. TACI has been validated as a target for the treatment of chronic lymphocytic leukaemia. However, how TACI signals remains elusive. The TACI receptor has two extracellular domains, with the membrane-proximal domain binding to two cytokines, B-cell activating factor (BAFF) and A proliferation-inducing ligand (APRIL). It has been previously demonstrated that a trimer of APRIL binds to a trimer of the TACI receptor on the cell surface, activating signalling 1. On the other hand, BAFF has been reported to exist both as a trimer and a 60-mer 2,3 . This is the only known example of a cytokine adopting a 60-meric conformation, reminiscent of a viral capsid. The physiological and pathological relevances of the two oligomeric states of BAFF remains unknown, as well as the assembly/disassembly mechanism by which BAFF switches between its two forms.
We have used a multi-pronged approach including mutagenesis, biophysical assays, X-ray crystallography and cryo-electron microscopy to explore BAFF biology . For the first time, we have identified environmental conditions and mutations that cause disassembly of the BAFF 60-mer into a trimer. These studies have revealed a novel intermediate disassembly step consisting of a pentamer of trimers that has been captured by cryo-electron microscopy. Computational studies have led to the design of a peptide that prevents the BAFF trimers from assembling into the 60-mer. The binding affinity of this peptide to BAFF was determined using surface plasmon resonance and preliminary co-crystals were obtained. We have also successfully purified the ligand-binding domain of the TACI receptor to investigate its binding to the two forms of BAFF using biophysical assays, crystallography and electron microscopy. These studies provide a step-by-step mechanism for the activation of the TACI receptor by BAFF.