eprintid: 1466171 rev_number: 43 eprint_status: archive userid: 608 dir: disk0/01/46/61/71 datestamp: 2015-04-16 15:40:58 lastmod: 2021-10-04 00:55:34 status_changed: 2015-04-16 15:40:57 type: article metadata_visibility: show item_issues_count: 0 creators_name: Doro, F creators_name: Saladino, G creators_name: Belvisi, L creators_name: Civera, M creators_name: Gervasio, FL title: New Insights into the Molecular Mechanism of E-Cadherin-Mediated Cell Adhesion by Free Energy Calculations ispublished: pub divisions: UCL divisions: B04 divisions: C06 divisions: F56 note: This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Chemical Theory and Computation, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/ct5010164 abstract: Three-dimensional domain swapping is an important mode of protein association leading to the formation of stable dimers. Monomers associating via this mechanism mutually exchange a domain to form a homodimer. Classical cadherins, an increasingly important target for anticancer therapy, use domain swapping to mediate cell adhesion. However, despite its importance, the molecular mechanism of domain swapping is still debated. Here, we study the conformational changes that lead to activation and dimerization via domain swapping of E-cadherin. Using state-of-the-art enhanced sampling atomistic simulations, we reconstruct its conformational free energy landscape, obtaining the free energy profile connecting the inactive and active form. Our simulations predict that the E-cadherin monomer populates the open and closed forms almost equally, which is in agreement with the proposed “selected fit” mechanism in which monomers in an active conformational state bind to form a homodimer, analogous to the conformational selection mechanism often observed in ligand–target binding. Moreover, we find that the open state population is increased in the presence of calcium ions at the extracellular boundary, suggesting their possible role as allosteric activators of the conformational change. date: 2015-03-03 official_url: http://dx.doi.org/10.1021/ct5010164 vfaculties: VMPS oa_status: green full_text_type: other language: eng primo: open primo_central: open_green article_type_text: article verified: verified_manual elements_source: Manually entered elements_id: 1026399 doi: 10.1021/ct5010164 lyricists_name: Gervasio, Francesco Luigi lyricists_name: Saladino, Giorgio lyricists_id: FLGER36 lyricists_id: GSALA75 full_text_status: public publication: Journal of Chemical Theory and Computation volume: 11 article_number: 4 pagerange: 1354 - 1359 issn: 1549-9618 citation: Doro, F; Saladino, G; Belvisi, L; Civera, M; Gervasio, FL; (2015) New Insights into the Molecular Mechanism of E-Cadherin-Mediated Cell Adhesion by Free Energy Calculations. Journal of Chemical Theory and Computation , 11 , Article 4. 10.1021/ct5010164 <https://doi.org/10.1021/ct5010164>. Green open access document_url: https://discovery.ucl.ac.uk/id/eprint/1466171/1/Revised_manuscript.pdf