[HTML][HTML] Enforced covalent trimerization increases the activity of the TNF ligand family members TRAIL and CD95L

D Berg, M Lehne, N Müller, D Siegmund… - Cell Death & …, 2007 - nature.com
D Berg, M Lehne, N Müller, D Siegmund, S Münkel, W Sebald, K Pfizenmaier, H Wajant
Cell Death & Differentiation, 2007nature.com
Variants of human TRAIL (hTRAIL) and human CD95L (hCD95L), encompassing the TNF
homology domain (THD), interact with the corresponding receptors and stimulate CD95 and
TRAILR2 signaling after cross-linking. The murine counterparts (mTRAIL, mCD95L) showed
no or only low receptor binding and were inactive/poorly active after cross-linking. The stalk
region preceding the THD of mCD95L conferred secondary aggregation and restored CD95
activation in the absence of cross-linking. A corresponding variant of mTRAIL, however, was …
Abstract
Variants of human TRAIL (hTRAIL) and human CD95L (hCD95L), encompassing the TNF homology domain (THD), interact with the corresponding receptors and stimulate CD95 and TRAILR2 signaling after cross-linking. The murine counterparts (mTRAIL, mCD95L) showed no or only low receptor binding and were inactive/poorly active after cross-linking. The stalk region preceding the THD of mCD95L conferred secondary aggregation and restored CD95 activation in the absence of cross-linking. A corresponding variant of mTRAIL, however, was still not able to activate TRAIL death receptors, but gained good activity after cross-linking. Notably, disulfide-bonded fusion proteins of the THD of mTRAIL and mCD95L with a subdomain of the tenascin-C (TNC) oligomerization domain, which still assembled into trimers, efficiently interacted with their cognate cellular receptors and robustly stimulated CD95 and TRAILR2 signaling after secondary cross-linking. Introduction of the TNC domain also further enhanced the activity of THD encompassing variants of hTRAIL and hCD95L. Thus, spatial fixation of the N-terminus of the THD appears necessary in some TNF ligands to ensure proper receptor binding. This points to yet unanticipated functions of the stalk and/or transmembrane region of TNF ligands for the functionality of these molecules and offers a broadly applicable option to generate recombinant soluble ligands of the TNF family with superior activity.
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