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UCHL5 binds Ubiquitin. 25 / 35
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sparser
"Indeed, the Ub-VS assay confirmed inhibitory activity for each ITC on the ubiquitin-binding activity of UCHL5 ( xref )."
30015387
sparser
"Similarly, BITC and PEITC also inhibited the Ub-binding activity of UCHL5 in a dose-dependent manner ( xref , lower panel , lanes 3–6 vs. 2)."
30015387
sparser
"Structural studies have elegantly shown that the DEUBAD domain of the INO80 subunit NFRKB/INO80G (INO80G DEUBAD ) inhibits binding of Ub to UCH37 by obscuring elements comprising the cS1 Ub-binding site ( xref ; xref )."
35451368
sparser
"For targets 99 and 100 the ubiquitin-propargyl was attached to UCH-L5 using ubiquitin bound to another deubiquitinase UCH37 (PDB ID 4I6N xref ) as a template."
27718275
sparser
"The X-ray structure of the Ubiquitin (Ub) bound to UCH-L5 shows a β-sheet hairpin in Ub that contains a crucial hydrophobic patch involved in the interaction with UCH-L5."
35720124
sparser
"In addition to Leu8 and Thr9, residues Phe5 and Ile13 were implicated to be essential in the binding of Ub to UCH-L5."
35720124
sparser
"To delineate the structural basis of the auto-inhibition of Uch37 and its activation by Rpn13C, we used a Uch37 dimer model derived from its crystal structure and compared it with the structure of the binary complex of ubiquitin-bound Uch37 (PDB ID 4IG7) and its homolog UCH-L3 (PDB ID 1XD3)."
24752541
reach
"According to Chen et al., the ubiquitin- and UCH37-binding domains of ADRM1 interact with each other, rendering the ADRM1 inactive [20]."
37946295
sparser
"The FRF hairpin inserts into the pocket of Uch37 that normally binds ubiquitin, and is clasped in place by binding of the long, C-terminal helix of NFRKB DEU to the catalytic domain of Uch37, which forces the second helix in the Uch37 ULD domain to bend [ xref , xref , xref ] ( xref )."
28988953
sparser
"It is also a reversible non‐selective competitive inhibitor of USP14, targeting the formation of Ub‐USP14 or Ub‐UCHL5 conjugates. xref  This is achieved by inhibiting the enzymatic activity of USP14 and UCHL5, and VLX1570 shows significant anti‐cancer impact in multiple myeloma and Waldenstrom's macroglobulinemia. xref Anchored in these findings, a phase 1/2 trial evaluating the efficacy and tolerability of VLX1570 in patients with relapsed or refractory multiple myeloma is currently under way (NCT02372240). xref "
34854221
sparser
"We compared the interactions of ubiquitin with UCHL1, UCHL3, and Ts UCH37 and tried to reciprocate on to UCHL5-based homology model of BAP1N ( xref )."
28935764
sparser
"Rpn13 binding to the proteasome releases this interaction and makes the domains available for ubiquitin binding and activation of Uch37 ( xref )."
29652515
sparser
"We next carried out NMR titration analyses with 0.1 mM UCH-L5 N240 and up to 0.15 mM ubiquitin to evaluate the binding processes under conditions that should significantly increase the population of ubiquitin-bound UCH-L5 N240 ."
28338014
reach
"In addition to Leu8 and Thr9, residues Phe5 and Ile13 were implicated to be essential in the binding of Ub to UCH-L5."
35720124
sparser
"We cannot, however, exclude the possibility that assembly of Uch37 into hINO80 affects DUB activity by a different mechanism, since our attempts to measure the binding of ubiquitin to Uch37 within hINO80 have been unsuccessful."
18922472
sparser
"The measured K d s for K6/K48 tri-Ub binding to either free or Ub-bound UCH37 are quite similar (see Deol et al. Mol Cell 2020 and data now shown in Figure 2 – Supplementary Figure 2), suggesting there is little cooperativity when Ub occupies the S1 site."
35451368
sparser
"An earlier attempt to study the thermodynamics of ubiquitin binding to full-length UCHL5 in its apo form was not effective because of the low concentration of enzyme and substrate."
28935764
sparser
"The binding parameters for UCHL5 and ubiquitin interaction were K d ~10.1 µM, ΔH ~ –18.6 kJ/mol, ΔS ~33.2 J/mol·K, and ΔG ~ –28.3 kJ M −1 ."
28935764
reach
"The X-ray structure of the Ubiquitin (Ub) bound to UCH-L5 shows a beta-sheet hairpin in Ub that contains a crucial hydrophobic patch involved in the interaction with UCH-L5."
35720124
reach
"It can be appreciated from the crystal structures of UCH-L5:RPN13:Ub (PDB:4UEL), that Ub binds to UCH-L5 using its hydrophobic patch consisting of residues Leu8, Thr9, and Ile44 in addition to its C-terminal tail (Figures 1A,B)."
35720124
reach
"Structural studies have elegantly shown that the DEUBAD domain of the INO80 subunit NFRKB/INO80G (INO80G ) inhibits binding of Ub to UCH37 by obscuring elements comprising the cS1 Ub-binding site (Sahtoe et al., 2015; Vander Linden et al., 2015)."
35451368
sparser
"An inspection of 39 DUB-ubiquitin structures in the protein data bank reveals the uniqueness of the salt bridge in ubiquitin bound to UCH37, an interaction that disappears when the ULD is deleted, as revealed in the structure of the catalytic domain alone bound to UbVME."
23617878
sparser
"Interestingly, the association of a Ub conjugate with Uch37 can also allosterically activate peptide entry."
28525752
sparser
"However, how ubiquitin binds to UCH37 has not been structurally characterized."
23617878
sparser
"Undoubtedly, DUB activity is a promising strategy for cancer therapy. xref  VLX1570 targets the Ub‐USP14 or Ub‐UCHL5 conjugates and is a reversible non‐selective competitive inhibitor of ubiquitin peptidase 14 (USP14) and ubiquitin carboxyl‐terminal hydrolase 5 (UCHL5) in multiple myeloma. xref  VLX1570 has been shown to have significant anti‐cancer efficacy with high potency and solubility."
34854221