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Synergized with X-ray crystallography, NMR spectroscopy and isothermal titration calorimetry (ITC), structure-based virtual screening has been used to complement experimental high-throughput screening (HTS) methods to improve the efficiency and efficacy of discovering lead inhibitors[7] [11].
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The high failure rate of new therapies tested in clinical development accentuates the critical importance of discovering biomarker readouts that can predict efficacy.
On the other hand, ineffective interventions may have apparent positive effects on surrogates (false-positive) leading to unnecessary confirmatory studies in which the true lack of efficacy is discovered after years of futile effort [ 1].
To further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds (1), a series of aromatic heterocyclic derivatives were designed, synthesized and evaluated for in vitro antifungal activity.
To further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compound 1, a series of benzoheterocycle analogues were designed, synthesized and evaluated for their in vitro antifungal activity.
In order to further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds (I), two series of novel azoles featuring thieno[2,3-c]pyrrolidone and thieno[3,2-c]pyrrolidone nuclei were designed and evaluated for their in vitro activity on the basis of the binding mode of albaconazole using molecular docking, along with SARs of antifungal triazoles.
In this study we examine the efficacy of Compstatin, a recently discovered peptide inhibitor of complement, in preventing heparin/protamine-induced complement activation in baboons.
Initially, putative metabolic biomarkers for cancer detection and/or assessment of efficacy of anticancer treatment are discovered in preclinical analyses, followed by the validation of these biomarkers in biofluids (blood, urine, prostatic secretions, etc).
In an effort to develop more effective medications, researchers increasingly are focusing on two goals: (1) improving the efficacy of existing medications and (2) discovering new drug targets.
We have demonstrated the efficacy of SFPA for translating signatures discovered in vitro into factors which are clearly related to specific biological processes and which can be used to assess important clinical outcomes.
In 2009, Bishop et al. discovered the efficacy of chloramphenicol in the treatment of chytridiomycosis [ 13].
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