Homology modeling of MT1 and MT2 receptors.
Melatonin is a neurohormone synthesized and secreted mainly during the dark period of the circadian cycle by the pineal gland. It has already been proved to be involved in a number of chronobiological processes, most of them being mediated by its membranar receptors MT1 and MT2. Both are members of the GPCR class and, despite the interest they elicit, their 3D structure is still to be described. Models for both human MT1 and MT2 receptors have been constructed by homology modeling, using the X-ray structure of bovine rhodopsin as template. These models have been evaluated in terms of hydrophobic properties of the helices and refined to take into account the rearrangement of GPCRs necessary for their activation, thus leading to a putative activated model for each subtype.
Farce
Amaury
A
Faculté des Sciences Pharmaceutiques et Biologiques, Laboratoire de Chimie Thérapeutique, EA 1043, 3, rue du Professeur Laguesse, BP 83, 59006 Lille Cedex, France.
Chugunov
Anton O
AO
Logé
Cédric
C
Sabaouni
Ahmed
A
Yous
Saïd
S
Dilly
Sébastien
S
Renault
Nicolas
N
Vergoten
Gérard
G
Efremov
Roman G
RG
Lesieur
Daniel
D
Chavatte
Philippe
P
D000595:Amino Acid Sequence; D000818:Animals; D020134:Catalytic Domain; D002417:Cattle; D057927:Hydrophobic and Hydrophilic Interactions; D008024:Ligands; D008550:Melatonin / Q000737:chemistry / Q000378:metabolism; D008958:Models, Molecular; D008968:Molecular Conformation; D008969:Molecular Sequence Data; D044122:Receptor, Melatonin, MT1 / Q000737:chemistry* / Q000378:metabolism; D044123:Receptor, Melatonin, MT2 / Q000737:chemistry* / Q000378:metabolism; D012243:Rhodopsin / Q000737:chemistry / Q000378:metabolism; D016415:Sequence Alignment; D017386:Sequence Homology, Amino Acid
D008024:Ligands; D044122:Receptor, Melatonin, MT1; D044123:Receptor, Melatonin, MT2; D012243:Rhodopsin; D008550:Melatonin