title: Middle East respiratory syndrome coronavirus (MERS-CoV) entry inhibitors targeting spike protein.
abstract: The recent outbreak of Middle East respiratory syndrome (MERS) coronavirus (MERS-CoV) infection has led to more than 800 laboratory-confirmed MERS cases with a high case fatality rate (∼35%), posing a serious threat to global public health and calling for the development of effective and safe therapeutic and prophylactic strategies to treat and prevent MERS-CoV infection. Here we discuss the most recent studies on the structure of the MERS-CoV spike protein and its role in virus binding and entry, and the development of MERS-CoV entry/fusion inhibitors targeting the S1 subunit, particularly the receptor-binding domain (RBD), and the S2 subunit, especially the HR1 region, of the MERS-CoV spike protein. We then look ahead to future applications of these viral entry/fusion inhibitors, either alone or in combination with specific and nonspecific MERS-CoV replication inhibitors, for the treatment and prevention of MERS-CoV infection.
authors.affiliation: Key Lab of Medical Molecular Virology of MOE/MOH, Shanghai Medical College, Fudan University, 130 Dong An Road, Xuhui District, Shanghai 200032, China.
authors.forename: Shuai
authors.initials: S
authors.lastname: Xia
authors.affiliation: Key Lab of Medical Molecular Virology of MOE/MOH, Shanghai Medical College, Fudan University, 130 Dong An Road, Xuhui District, Shanghai 200032, China; Department of Medical Microbiology and Immunology, School of Basic Medicine, Dali University, Dali 671000, China.
authors.forename: Qi
authors.initials: Q
authors.lastname: Liu
authors.affiliation: Key Lab of Medical Molecular Virology of MOE/MOH, Shanghai Medical College, Fudan University, 130 Dong An Road, Xuhui District, Shanghai 200032, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Wang
authors.affiliation: Key Lab of Medical Molecular Virology of MOE/MOH, Shanghai Medical College, Fudan University, 130 Dong An Road, Xuhui District, Shanghai 200032, China.
authors.forename: Zhiwu
authors.initials: Z
authors.lastname: Sun
authors.affiliation: Key Lab of Medical Molecular Virology of MOE/MOH, Shanghai Medical College, Fudan University, 130 Dong An Road, Xuhui District, Shanghai 200032, China.
authors.forename: Shan
authors.initials: S
authors.lastname: Su
authors.affiliation: Lindsley F. Kimball Research Institute, New York Blood Center, New York, NY 10065, USA.
authors.forename: Lanying
authors.initials: L
authors.lastname: Du
authors.affiliation: Key Lab of Medical Molecular Virology of MOE/MOH, Shanghai Medical College, Fudan University, 130 Dong An Road, Xuhui District, Shanghai 200032, China.
authors.forename: Tianlei
authors.initials: T
authors.lastname: Ying
authors.affiliation: Key Lab of Medical Molecular Virology of MOE/MOH, Shanghai Medical College, Fudan University, 130 Dong An Road, Xuhui District, Shanghai 200032, China. Electronic address: lul@fudan.edu.cn.
authors.forename: Lu
authors.initials: L
authors.lastname: Lu
authors.affiliation: Key Lab of Medical Molecular Virology of MOE/MOH, Shanghai Medical College, Fudan University, 130 Dong An Road, Xuhui District, Shanghai 200032, China; Lindsley F. Kimball Research Institute, New York Blood Center, New York, NY 10065, USA. Electronic address: shibojiang@fudan.edu.cn.
authors.forename: Shibo
authors.initials: S
authors.lastname: Jiang
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology* / Q000627:therapeutic use; D018352:Coronavirus Infections / Q000188:drug therapy; D006801:Humans; D065207:Middle East Respiratory Syndrome Coronavirus / Q000187:drug effects* / Q000502:physiology*; D064370:Spike Glycoprotein, Coronavirus / Q000037:antagonists & inhibitors*; D053585:Virus Attachment / Q000187:drug effects*; D053586:Virus Internalization / Q000187:drug effects*
chemical_list: D000998:Antiviral Agents; D064370:Spike Glycoprotein, Coronavirus
keywords: Entry inhibitor; Fusion inhibitor; MERS-CoV; Middle East respiratory syndrome coronavirus; Receptor-binding domain; Six-helix bundle