9.A.14.10.4 Dimeric oxytosin receptor, OxtR, of 389 aas and 7 TMSs. Superpotent behavior follows from the binding of oxytosin receptor-specific bivalent ligands to dimeric receptors
based on a TMS1-TMS2 interface, and in this arrangement, only analogues with a well-defined spacer length (approximately 25 Å) precisely fit inside a channel-like passage between the
two protomers of the dimer (Busnelli et al. 2016). The oxytocin receptor (OXTR) is involved in parturition and lactation of mammals as well as their emotional and social behaviors. Cholesterol acts on OXTR as an allosteric modulator, inducing a high-affinity state for orthosteric ligands. Stable binding of cholesterol to the receptor when it adopts an orthosteric ligand-bound state preserves the cholesterol-dependent activity of the receptor (Lemel et al. 2021).
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Accession Number: | P30559 |
Protein Name: | Oxytocin receptor |
Length: | 389 |
Molecular Weight: | 42772.00 |
Species: | Homo sapiens (Human) [9606] |
Number of TMSs: | 7 |
Location1 / Topology2 / Orientation3: |
Cell membrane1 / Multi-pass membrane protein2 |
Substrate |
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1: MEGALAANWS AEAANASAAP PGAEGNRTAG PPRRNEALAR VEVAVLCLIL LLALSGNACV
61: LLALRTTRQK HSRLFFFMKH LSIADLVVAV FQVLPQLLWD ITFRFYGPDL LCRLVKYLQV
121: VGMFASTYLL LLMSLDRCLA ICQPLRSLRR RTDRLAVLAT WLGCLVASAP QVHIFSLREV
181: ADGVFDCWAV FIQPWGPKAY ITWITLAVYI VPVIVLAACY GLISFKIWQN LRLKTAAAAA
241: AEAPEGAAAG DGGRVALARV SSVKLISKAK IRTVKMTFII VLAFIVCWTP FFFVQMWSVW
301: DANAPKEASA FIIVMLLASL NSCCNPWIYM LFTGHLFHEL VQRFLCCSAS YLKGRRLGET
361: SASKKSNSSS FVLSHRSSSQ RSCSQPSTA