TY - JOUR
T1 - Structural-functional analysis of the third transmembrane domain of the corticotropin-releasing factor type 1 receptor role in activation and allosteric antagonism
AU - Spyridaki, Katerina
AU - Matsoukas, Minos Timotheos
AU - Cordomi, Arnau
AU - Gkountelias, Kostas
AU - Papadokostaki, Maria
AU - Mavromoustakos, Thomas
AU - Logothetis, Diomedes E.
AU - Margioris, Andrew N.
AU - Pardo, Leonardo
AU - Liapakis, George
PY - 2014/7/4
Y1 - 2014/7/4
N2 - Background: The molecular mechanisms underlying activation of CRF1 receptor (CRF1R) were elusive. Results: We determined specific residues in the transmembrane domains (TMs) of CRF1R that are critical for receptor activation. Conclusion: A possible "transmission switch" involving TM interactions is important for CRF1R activation. Significance: This knowledge may aid in the development of nonpeptide CRF1R antagonists for use in stress-related disorders. © 2014 by The American Society for Biochemistry and Molecular Biology, Inc.
AB - Background: The molecular mechanisms underlying activation of CRF1 receptor (CRF1R) were elusive. Results: We determined specific residues in the transmembrane domains (TMs) of CRF1R that are critical for receptor activation. Conclusion: A possible "transmission switch" involving TM interactions is important for CRF1R activation. Significance: This knowledge may aid in the development of nonpeptide CRF1R antagonists for use in stress-related disorders. © 2014 by The American Society for Biochemistry and Molecular Biology, Inc.
U2 - 10.1074/jbc.M113.544460
DO - 10.1074/jbc.M113.544460
M3 - Article
VL - 289
SP - 18966
EP - 18977
IS - 27
ER -