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Article title picture
The article reviews the clinical molecules of oral PROTAC, including IND
.
The article summarizes the general optimization process
of the ARV-110.
The article summarizes the general optimization process
of ARV-471.
VHL binder is generally more difficult to make orally, but it does
.
The physicochemical properties
of some oral PROTACs are summarized in this article.
VHL binder's HMG-CoA reductase degrader, although used as an oral example, is not very efficient in oral administration, and in addition, the cpd 11 drawn here is lactone (cpd 36 is open-loop), which seems to be different
from the rest of the article.
The article exemplifies molecules, and summarizes the oral "rules"
of PROTAC.
CPD 9 uses a prodrug strategy to reduce the CRBN binder by one HB donor, while possibly masking the adjacent carbonyl group a little, at least in this case, the increase in oral availability still seems obvious
.
Finally, these "rules" are very reasonable suggestions, but of course they are not "golden rules", it can only be said that those who meet these rules can be made orally with greater hope, beyond these rules may be doubly difficult
.
