IndraLab

Statements

COV1 binds OTUB2. 7 / 7
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reach
"In contrast to the co-crystal structure of the OTUB2-COV-1 complex (PDB 5QIO), a clear density for the cyclopropyl-phenyl moiety in our OTUB2-LN5P45 co-crystal structure was detected, which is likely due to the fact that LN5P45 has the defined (1S,2S) configuration."
37642399
sparser
"In contrast to the co-crystal structure of the OTUB2-COV-1 complex (PDB), a clear density for the cyclopropyl-phenyl moiety in our OTUB2- LN5P45 co-crystal structure was detected, which is likely due to the fact that LN5P45 has the defined (1 S ,2 S ) configuration."
37642399
sparser
"For example, OTUB2-COV-1 targets the active Cys51 of OTUB2, and NUDT7-COV-1 targets C73 of NUDT7 [ xref ]."
36431829
sparser
"Further fragment analogue evaluation yielded the best inhibitor OTUB2-COV-1 ( xref ) with the k inact / K I value of 3.75 M −1 s −1 ."
34458789
sparser
"IsoTOP-ABPP demonstrated that OTUB2-COV-1 (10 μM compound, 2 h incubation) labeled <1% probe-accessible cysteines (Heavy/Light ratio >4) in HEK293T cells suggesting promising selectivity profile suitable for further development."
34458789
sparser
"Small molecule inhibitors for OTUB2 (OTUB2-COV-1) [ xref ] and USP4 (NR) [ xref ] have also been identified."
35204803
sparser
"Recently, the first highly selective OTUB2 covalent inhibitor named OTUB2-COV-1 ( 38 , xref ) was identified by combining a new high-throughput thiol-reactivity assay with high-throughput crystallography [ xref ]."
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