title: High-resolution crystal structure of FKBP12 from Aedes aegypti.
abstract: Dengue is one of the most infectious viral diseases prevalent mainly in tropical countries. The virus is transmitted by Aedes species of mosquito, primarily Aedes aegypti. Dengue remains a challenging drug target for years as the virus eludes the immune responses. Currently, no vaccines or antiviral drugs are available for dengue prevention. Previous studies suggested that the immunosuppressive drug FK506 shows antimalarial activity, and its molecular target, FK506-binding protein (FKBP), was identified in the Plasmodium parasite. Likewise, a FKBP family protein has been identified in A. aegypti (AaFKBP12) in which AaFKBP12 is assumed to play a similar role in its life cycle. FKBPs belong to a highly conserved class of proteins and are considered as an attractive pharmacological target. Herein, we present a high-resolution crystal structure of AaFKBP12 at 1.3 Å resolution and discuss its structural features throwing light in facilitating the design of potential antagonists against the dengue-transmitting mosquito.
authors.affiliation: Division of Structural Biology and Biochemistry, School of Biological Science, Nanyang Technological University, Singapore 637551.
authors.forename: Sreekanth
authors.initials: S
authors.lastname: Rajan
authors.forename: Kai Qian
authors.initials: KQ
authors.lastname: Saw
authors.forename: Quoc Toan
authors.initials: QT
authors.lastname: Nguyen
authors.forename: Kwanghee
authors.initials: K
authors.lastname: Baek
authors.forename: Ho Sup
authors.initials: HS
authors.lastname: Yoon
mesh_terms: D000330:Aedes / Q000737:chemistry* / Q000187:drug effects; D000595:Amino Acid Sequence; D000818:Animals; D020134:Catalytic Domain; D018360:Crystallography, X-Ray; D003715:Dengue / Q000517:prevention & control / Q000635:transmission*; D015195:Drug Design; D006801:Humans; D007303:Insect Vectors / Q000737:chemistry* / Q000187:drug effects; D008958:Models, Molecular; D008969:Molecular Sequence Data; D011487:Protein Conformation; D016415:Sequence Alignment; D022061:Tacrolimus Binding Protein 1A / Q000037:antagonists & inhibitors / Q000737:chemistry*
chemical_list: D022061:Tacrolimus Binding Protein 1A