… in at least three of the four nucleotide binding sites (sites 1, 3, 4). We have modeled an AMP
at site 4 (… to obtain an activator-bound structure at 3.3 Aresolution through a crystal soaking …

… In none of these instances did we observe reaction at the 4-position of the pyridine-N-oxide.
As shown in Table 2, primary and secondary aliphatic amines were very effective …

… In none of these instances did we observe addition at the 4-position, a result consistent with
… at the nitrogen. For entry 15, we saw both a regioselective and chemoselective reaction at …

Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a key role in regulating the
levels of plasma low-density lipoprotein cholesterol (LDL-C). Here, we demonstrate that the …

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Compounds that contain the 1-heteroaryl-3-azabicyclo[3.1.0]hexane architecture are of
particular interest to the pharmaceutical industry yet remain a challenge to synthesize. We report …

… one dimension from our lead optimization efforts and, at the same time, streamline our in vitro
… profiling (CEREP; tested at a dose of 10 μM, Figure 2) 11 was active at a number of targets …

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… A new X-ray crystal structure confirms direct binding of this chemical series to YEATS4 at
the lysine acetylation recognition site of the YEATS domain. Multiple analogues engage …