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Further development of the leads might result in potent PL inhibitors.
These results suggest that N-SMase and several ceramides can result in potent venular cerebrovasospasm, leukocyte endothelial chemoattraction, and microvessel wall permeability changes in the intact rat brain.
This initial SAR suggests pharmacophoric elements that may be modified to modulate/increase opioid affinity, while maintaining high affinity for the NOP receptor, to result in potent bifunctional small-molecule NOP/MOP ligands.
Moreover, targeting of the HER-2 receptor by the humanized antibody trastuzumab has been shown to result in potent growth inhibition of HER-2 overexpressing tumors [13], [14].
The results demonstrate that nonviral gene transfer by PB transposon combined with PEI might result in potent tumor growth inhibition.
Unfortunately, translational studies to the administration of solely anti-oxidants did not yet result in potent protection against apoptosis in human diabetic nephropathy as reviewed in [ 4].
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Microbial transformation of DHT (1) by using two fungal cultures resulted in potent butyrylcholinesterase (BChE) inhibitors.
CRM1 inhibition by the compounds also resulted in potent suppression of cardiomyocyte hypertrophy.
In the light of mild quantitative cell alterations, our results suggest that sepsis induces a functional modulation of immune cells resulting in potent anti-tumoral activity.
Optimization at the 1- and 5-positions of the uracil resulted in potent compounds such as 24 (Ki = 0.45 nM).
We present a successful design strategy using a conformational restriction approach resulting in potent and selective inhibitors of TAFIa.
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