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Tankyrases as drug targets
Tankyrase 1 and tankyrase 2 are poly(ADP‐ribosyl)ases that are distinguishable from other members of the enzyme family by the structural features of the catalytic domain, and the presence of aExpand
Tankyrases: Structure, Function and Therapeutic Implications in Cancer
Several small molecule inhibitors have been described for Tankyrases; they compete with the co-substrate NAD+ for binding to the ARTD catalytic domain and possess several properties of lead compounds and can be used for proof-of-concept studies in cancer and other Tankyrase linked diseases. Expand
Completing the family portrait of the anti‐apoptotic Bcl‐2 proteins: Crystal structure of human Bfl‐1 in complex with Bim
The crystal structure of Bfl‐1, the last anti‐apoptotic Bcl‐2 family member to be structurally characterized, in complex with a peptide corresponding to the BH3 region of the pro‐ap optotic protein Bim reveals distinct features at the peptide‐binding site, likely to define the binding specificity for pro‐APoptotic proteins. Expand
Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3.
A structural and functional analysis of the PARP domain of human PARP-3 in complex with several inhibitors suggests routes for creating isoenzyme-specific PARP inhibitors and highlights key features for potent inhibitor binding. Expand
The DEXD/H-box RNA Helicase DDX19 Is Regulated by an α-Helical Switch*S⃞
The crystal structures of DDX19 reveal an α-helix that inserts between the conserved domains of the free protein to negatively regulate ATPase activity, corroborated by biochemical data that confirm an autoregulatory function of the N-terminal region of the protein. Expand
PARP-3 Is a Mono-ADP-ribosylase That Activates PARP-1 in the Absence of DNA*
It is reported that PARP-3 small interfering RNA-depleted cells are not sensitive to the topoisomerase I poison camptothecin, inducing DNA single-strand breaks, and repair these lesions as efficiently as wild-type cells. Expand
Crystal Structures of the ATPase Domains of Four Human Hsp70 Isoforms: HSPA1L/Hsp70-hom, HSPA2/Hsp70-2, HSPA6/Hsp70B', and HSPA5/BiP/GRP78
The structures presented here support the view that the NBDs of human Hsp70 function by conserved mechanisms and contribute little to isoform specificity, which instead is brought about by the SBDs and by accessory proteins. Expand
Zinc binding catalytic domain of human tankyrase 1.
The present structure reveals that tankyrases contain a short zinc-binding motif, which has not been predicted, which will be of great value to facilitate structure-based design of selective PARP inhibitors, in general, and tankyrase inhibitors in particular. Expand
Comparative Structural Analysis of Lipid Binding START Domains
Background Steroidogenic acute regulatory (StAR) protein related lipid transfer (START) domains are small globular modules that form a cavity where lipids and lipid hormones bind. These domains canExpand
Structure of Streptococcus agalactiae serine/threonine phosphatase
We solved the crystal structure of Streptococcus agalactiae serine/threonine phosphatase (SaSTP) using a combination of single‐wavelength anomalous dispersion phasing and molecular replacement. TheExpand