Crystal Structures of Two Vancomycin Complexes with Phosphate andN-Acetyl–D-Ala. Structural Comparison between Low-Affinity and High-Affinity Ligand Complexes of Vancomycin

2010 ◽  
Vol 83 (4) ◽  
pp. 391-400 ◽  
Author(s):  
Takanori Kikuchi ◽  
Shyam Karki ◽  
Ikuhide Fujisawa ◽  
Yoshitaka Matsushima ◽  
Yasushi Nitanai ◽  
...  
Keyword(s):  
Crystal Structures ◽  
Structural Comparison ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

scholarly journals Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15

2019 ◽  
Author(s):  
Tyler Faust ◽  
Hojong Yoon ◽  
Radosław P. Nowak ◽  
Katherine A. Donovan ◽  
Zhengnian Li ◽  
...  
Keyword(s):  
Crystal Structures ◽  
De Novo ◽  
Splicing Factor ◽  
High Affinity ◽  
Affinity Ligand ◽  
Investigational Drugs ◽  
High Affinity Ligand ◽  
Dependent Mechanism

AbstractThe investigational drugs E7820, indisulam and tasisulam (aryl-sulfonamides) promote the degradation of the splicing factor RBM39 in a proteasome-dependent mechanism. While the activity critically depends on the Cullin RING ligase substrate receptor DCAF15, the molecular details remain elusive. Here we present the cryo-EM structure of the DDB1-DCAF15-DDA1 core ligase complex bound to RBM39 and E7820 at 4.4 Å resolution, together with crystal structures of engineered subcomplexes. We show that DCAF15 adopts a novel fold stabilized by DDA1, and that extensive protein-protein contacts between the ligase and substrate mitigate low affinity interactions between aryl-sulfonamides and DCAF15. Our data demonstrates how aryl-sulfonamides neo-functionalize a shallow, non-conserved pocket on DCAF15 to selectively bind and degrade RBM39 and the closely related splicing factor RBM23 without the requirement for a high affinity ligand, which has broad implications for the de novo discovery of molecular glue degraders.

scholarly journals A novel radioiodinated high affinity ligand for the D2 -dopamine receptor

FEBS Letters ◽  
1984 ◽  
Vol 176 (2) ◽  
pp. 436-440 ◽  
Author(s):  
Nourdine Amlaiky ◽  
Brian F. Kilpatrick ◽  
Marc G. Caron
Keyword(s):  
Dopamine Receptor ◽  
D2 Dopamine Receptor ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

scholarly journals High-Affinity Ligand Probes of CD22 Overcome the Threshold Set bycisLigands to Allow for Binding, Endocytosis, and Killing of B Cells

2006 ◽  
Vol 177 (5) ◽  
pp. 2994-3003 ◽  
Author(s):  
Brian E. Collins ◽  
Ola Blixt ◽  
Shoufa Han ◽  
Bao Duong ◽  
Hongyi Li ◽  
...  
Keyword(s):  
B Cells ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

scholarly journals RS-45041-190: a selective, high-affinity ligand for I2 imidazoline receptors

1995 ◽  
Vol 116 (2) ◽  
pp. 1737-1744 ◽  
Author(s):  
C.M. Brown ◽  
A.C. MacKinnon ◽  
W.S. Redfern ◽  
A. Williams ◽  
C. Linton ◽  
...  
Keyword(s):  
Imidazoline Receptors ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

Cortistatin A is a High-Affinity Ligand of Protein Kinases ROCK, CDK8, and CDK11

2009 ◽  
Vol 48 (47) ◽  
pp. 8952-8957 ◽  
Author(s):  
Victor J. Cee ◽  
David Y.-K. Chen ◽  
Matthew R. Lee ◽  
K. C. Nicolaou
Keyword(s):  
Protein Kinases ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand

scholarly journals An Antidiabetic Thiazolidinedione Is a High Affinity Ligand for Peroxisome Proliferator-activated Receptor γ (PPARγ)

1995 ◽  
Vol 270 (22) ◽  
pp. 12953-12956 ◽  
Author(s):  
Jürgen M. Lehmann ◽  
Linda B. Moore ◽  
Tracey A. Smith-Oliver ◽  
William O. Wilkison ◽  
Timothy M. Willson ◽  
...  
Keyword(s):  
Peroxisome Proliferator ◽  
Peroxisome Proliferator Activated Receptor ◽  
High Affinity ◽  
Affinity Ligand ◽  
High Affinity Ligand
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