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The proof of the pudding: A proof-of-concept study using γ-secretase inhibitors as a model has shown that sulfonimidamides act as bioisosteres for sulfonamides. Detailed in vitro and in vivo profiling reveal that the sulfonimidamide motif imparts desirable properties such as decreased lipophilicity and plasma protein binding, accompanied by increased solubility. Our data support a wider use of this unique functional group in the design of new pharmacologically active agents.
Medicinal Chemistry, iScience, CNSP iMed, AstraZeneca R&D Södertälje, Västra Mälarehamnen 9, 151 85 Södertälje (Sweden).
This article was published in the following journal.
Abstract Owing to our limited understanding of the relationship between sequence and function and the interaction between intracellular pathways and regulatory systems, the rational design of enzyme-c...
T7 RNA polymerase is the foundation of synthetic biological circuitry both in vivo and in vitro due to its robust and specific control of transcription from its cognate promoter. Here we present the d...
We have taken a rational approach to redesigning the amino acid binding and aminoacyl-tRNA pairing specificities of bacterial glutaminyl-tRNA synthetase. The four-stage engineering incorporates genera...
The application of the twelve principles of green chemistry in nanoparticle synthesis is a relatively new emerging issue concerning the sustainability. This field has received great attention in recen...
We present a simulation study of an actomyosin in vitro motility assay. In vitro motility assays have served as an essential element facilitating the application of actomyosin in nanotechnology; such ...
Subjects are healthy adult volunteers either at high risk for HIV infection or already known to be seropositive, who will donate blood for in vitro tests of T-cell function and in vitro re...
To compare the safety and efficacy of aerosolized pentamidine and dapsone in the prevention of Pneumocystis carinii pneumonia (PCP) in high-risk HIV-infected patients who are intolerant to...
Oxytocin is normally administered following delivery in pregnant patients to reduce postpartum bleeding by increasing uterine tone. It is unclear whether the use of intravenous oxytocin al...
Continuous albuterol has become the standard of care for patients in status asthmaticus. We have previously performed an in-vitro study comparing 4 different brands of continuous nebulizer...
Susceptibility testing is commonly employed in patients with bacterial infections in order to guide rational use of antibiotics; however, the use of antifungal susceptibility testing is li...
Biologically functional sequences of DNA chemically synthesized in vitro.
Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.
Synthetic transcripts of a specific DNA molecule or fragment, made by an in vitro transcription system. This cRNA can be labeled with radioactive uracil and then used as a probe. (King & Stansfield, A Dictionary of Genetics, 4th ed)
Studies determining the effectiveness or value of processes, personnel, and equipment, or the material on conducting such studies. For drugs and devices, CLINICAL TRIALS AS TOPIC; DRUG EVALUATION; and DRUG EVALUATION, PRECLINICAL are available.
Studies designed to assess the efficacy of programs. They may include the evaluation of cost-effectiveness, the extent to which objectives are met, or impact.
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Blood is a specialized bodily fluid that delivers necessary substances to the body's cells (in animals) – such as nutrients and oxygen – and transports waste products away from those same cells. In vertebrates, it is composed of blo...