Structure elucidation of a human melanocortin-4 receptor specific orthosteric nanobody agonist

Autor: Thomas Fontaine, Andreas Busch, Toon Laeremans, Stéphane De Cesco, Yi-Lynn Liang, Veli-Pekka Jaakola, Zara Sands, Sarah Triest, Simonas Masiulis, Lies Dekeyzer, Noor Samyn, Nicolas Loeys, Lisa Perneel, Melanie Debaere, Murielle Martini, Charlotte Vantieghem, Richa Virmani, Kamila Skieterska, Stephanie Staelens, Rosa Barroco, Maarten Van Roy, Christel Menet

Publikováno v: Nature Communications, Vol 15, Iss 1, Pp 1-14 (2024)

Abstract The melanocortin receptor 4 (MC4R) belongs to the melanocortin receptor family of G-protein coupled receptors and is a key switch in the leptin-melanocortin molecular axis that controls hunger and satiety. Brain-produced hormones such as α-

Externí odkaz: https://doaj.org/article/f05dbb65117040f98bbf56edfbe2bf19

The Extended N-Terminal Domain Confers Atypical Chemokine Receptor Properties to CXCR3-B

Autor: Giulia D’Uonnolo, Nathan Reynders, Max Meyrath, Dayana Abboud, Tomasz Uchański, Toon Laeremans, Brian F. Volkman, Bassam Janji, Julien Hanson, Martyna Szpakowska, Andy Chevigné

Publikováno v: Frontiers in Immunology, Vol 13 (2022)

The chemokine receptor CXCR3 plays a critical role in immune cell recruitment and activation. CXCR3 exists as two main isoforms, CXCR3-A and CXCR3-B, resulting from alternative splicing. Although the two isoforms differ only by the presence of an N-t

Externí odkaz: https://doaj.org/article/97a267f9626b47b594598c4e259d2560

Domain-interface dynamics of CFTR revealed by stabilizing nanobodies

Autor: Maud Sigoillot, Marie Overtus, Magdalena Grodecka, Daniel Scholl, Abel Garcia-Pino, Toon Laeremans, Lihua He, Els Pardon, Ellen Hildebrandt, Ina Urbatsch, Jan Steyaert, John R. Riordan, Cedric Govaerts

Publikováno v: Nature Communications, Vol 10, Iss 1, Pp 1-12 (2019)

The leading cause of cystic fibrosis is the deletion of phenylalanine 508 (F508del) in the first nucleotide-binding domain (NBD1) of the cystic fibrosis transmembrane conductance regulator (CFTR). Here authors we develop nanobodies targeting NBD1 of

Externí odkaz: https://doaj.org/article/2a36a5cc137946bdbc014d5d58e302cb

A topological switch in CFTR modulates channel activity and sensitivity to unfolding

Autor: Cédric Govaerts, Rafael Colomer Martinez, Chloe Martens, Yiting Wang, Maud Sigoillot, Abel Garcia-Pino, Els Pardon, Marie Overtus, Toon Laeremans, Jelle Hendrix, Daniel Scholl, David N. Sheppard, Jan Steyaert

Publikováno v: Scholl, D, Wang, Y, Sheppard, D N, Govaerts, C & al., E 2021, ' A Topological Switch in CFTR Modulates Channel Activity and Sensitivity to Unfolding ', Nature Chemical Biology, vol. 17, no. 9, pp. 989-997 . https://doi.org/10.1038/s41589-021-00844-0

The cystic fibrosis transmembrane conductance regulator (CFTR) anion channel is essential to maintain fluid homeostasis in key organs. Functional impairment of CFTR due to mutations in the cftr gene leads to cystic fibrosis. Here, we show that the fi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8431236bc079a668b825f35b4bbe9230
https://doi.org/10.1038/s41589-021-00844-0

Development of Generic G Protein Peptidomimetics Able to Stabilize Active State G

Autor: Morgane, Mannes, Charlotte, Martin, Sarah, Triest, Marilisa, Pia Dimmito, Adriano, Mollica, Toon, Laeremans, Christel J, Menet, Steven, Ballet

Publikováno v: Angewandte Chemie (International ed. in English). 60(18)

G protein-coupled receptors (GPCRs) represent an important group of membrane proteins that play a central role in modern medicine. Unfortunately, conformational promiscuity hampers full therapeutic exploitation of GPCRs, since the largest population

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::76bb46fd059ba2f1dba4882ba3f4c56b
https://pubmed.ncbi.nlm.nih.gov/33596327