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The cyclin-dependent kinases (CDKs) have been characterized in complex with a variety of inhibitors, but the majority of structures solved are in the inactive form.
While human cyclin A constructs have been extensively characterized in complex with cyclin dependent kinase 2 (CDK2), efforts to express the monomeric human cyclin A2 in Escherichia coli in a stable form, without the kinase subunit, have been laden with technical difficulties, including solubility, yield and purity.
Both highly optimized inhibitors 64 and 65 were structurally characterized in complex with the T. cruzi CYP51 target.
However, none of these inhibitors have yet been structurally characterized in complex with a GRK and thus their mechanisms of action are unknown.
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The complexes of Zn II 2,2′-bipyridine diacetate with salen (LH2) and salophen (L′H2) have been characterized in which complex with L′H2 in DMSO has yielded a novel one-dimensional molecular architecture of micrometer length.
Here we report a study on three newly synthesized Smac mimetics, which have been characterized in their complexes with XIAP BIR3 domain through X-ray crystallography and molecular modelling/docking simulations.
14, 15 The PBD has been well characterized crystallographically, both unliganded and in complex with various phosphopeptides: we have obtained ten new crystal forms, which supplement nine already in the public domain.
The sequence identity remains very high (46%) when compared with the R2 and R3 repeats of mouse c-MYB, a protein with its 3D structure already characterized in its free state or in complex with DNA [ 30].
Rhodniin is the only structurally characterized Kazal-type inhibitor with two domains in complex with thrombin (1∶1 ratio).
Subtype 7.3 is characterized by aberrations in Cyclin D, which drives passage from G1 to S in complex with CDK4 and CDK6.
HDX MS was used to study p110α and showed that p110α in complex with a regulatory subunit (p85α) constitutes a complex catalytic cycle characterized by distinct conformational steps.
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