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The S3 binding pocket is also well-defined, whereas the S4 pocket is very large and can tolerate a range of capping groups that are likely to contribute to potency by picking up further hydrophobic interactions.
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The possible relevance of these results in contributing to potency of phage lysins is discussed.
However, occupation of this site clearly strongly contributes to potency.
Together efficacy, toxicity and adherence contribute to the potency of the antiretroviral regimen, where potency is defined as the ability to succeed.
Taken together, our findings indicate that HDAC inhibitors have an immunomodulatory potential that may contribute to the potency and specificity of these antineoplastic compounds and might be useful in the treatment of autoimmune disorders.
Briefly, our findings show that HDACIs have a strong immunomodulatory potential that may contribute to the potency and specificity of these antineoplastic compounds and suggest that the immunosuppressive vs. increased tumor immunity effect of HDACIs might be important for targeting tumor cell proliferation and survival, which may impinge on the future clinical use of these drugs.
We discuss how particular chemical moieties contribute to inhibitor potency and suggest strategies that might be utilized in the successful design of selective and potent epigenetic inhibitors.
4-, 4β-, 6-, 6α-and 6β-substituents accommodated in the accessible channel formed extensive hydrophobic interactions with Thr310, Phe221, Val369, Val370, Ser478, but could not contribute to inhibition potency (Fig. 5b).
As with compound 8 (Supplementary Figure S3), the P1 ortho-chlorine of compound 16 is also likely to contribute to the potency by accessing the S1 sub-pocket.
Our findings in primary neurons indicated that mitochondrial retention of Smac could contribute to the potency of XIAP in such scenarios.
We note in this scenario, two ISRIB molecules binding to two identical interfaces of opposite polarity (eIF2B2 → eIF2B4 and eIF2B4 → eIF2B2) may bind and stabilize one (eIF2B 2, which may contribute to its potency.
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