公开(公告)号：EP2575849A2

公开(公告)日：2013-04-10

申请号：EP11789349.5

申请日：2011-06-01

申请人： Ben-Gurion University Of The Negev Research And Development Authority

发明人： BRIK, Ashraf ,  KUMAR, Ajish ,  ERLICH, Leslie ,  SPASSER, Liat

IPC分类号： A61K38/00 ,  C07K5/00

CPC分类号： C07K1/04 ,  A61K47/62 ,  C07K1/026 ,  C07K1/1075

摘要： The present invention discloses a process for preparing ubiquinated peptide conjugates comprising a ubiquitin peptide residue UR attached at its C-terminus to a substrate peptide via a native isopeptide bond, this process comprising combining Native Chemical Ligation (NCL) and solid phase peptide synthesis (SPPS). Further are disclosed ubiquinated peptide conjugates containing a native isopeptide bond, as well as various uses thereof.

公开(公告)号：EP2533792A2

公开(公告)日：2012-12-19

申请号：EP11741975.4

申请日：2011-02-09

申请人： Ben-Gurion University Of The Negev Research And Development Authority

发明人： BRIK, Ashraf ,  HAJ-YAHYA, Mahmood ,  KUMAR, Ajish ,  ERLICH, Leslie ,  SPASSER, Liat

IPC分类号： A61K38/00

CPC分类号： C07K1/1077 ,  C07K1/1075 ,  C07K14/00 ,  C07K14/001 ,  C07K14/47

摘要： The present invention discloses latent thioester functionalities attached to the C-terminus of a first polypeptide, or a first fragment thereof having a Cys residue at its N-terminus, and a process using this functionality for the preparation of polypeptide thioesters, in particular of ubiquitin thioesters, this process comprising preparing a polypeptide or a fragment thereof, being attached to a latent thioester functionality, which can then be ligated with a second polypeptide fragment, followed by selective activation of the latent thioester functionality group, to provide the requested polypeptide thioester. There are also provided the polypeptides obtained by this method, specific unnatural amino acids useful to be incorporated within the polypeptide thioesters, and kits for preparing them.

公开(公告)号：EP2534168A2

公开(公告)日：2012-12-19

申请号：EP11741976.2

申请日：2011-02-09

申请人： Ben-Gurion University Of The Negev Research And Development Authority

发明人： BRIK, Ashraf ,  HAJ-YAHYA, Mahmood ,  KUMAR, Ajish ,  ERLICH, Leslie ,  SPASSER, Liat

IPC分类号： C07K1/10

CPC分类号： C07K1/1077 ,  C07K1/1075 ,  C07K14/00 ,  C07K14/001 ,  C07K14/47

摘要： The present invention discloses latent thioester functionalities attached to the C-terminus of a first polypeptide, or a first fragment thereof having a Cys residue at its N-terminus, and a process using this functionality for the preparation of polypeptide thioesters, in particular of ubiquitin thioesters, this process comprising preparing a polypeptide or a fragment thereof, being attached to a latent thioester functionality, which can then be ligated with a second polypeptide fragment, followed by selective activation of the latent thioester functionality group, to provide the requested polypeptide thioester. There are also provided the polypeptides obtained by this method, specific unnatural amino acids useful to be incorporated within the polypeptide thioesters, and kits for preparing them.