Defining the cellular response to pharmacological agents is critical for understanding the mechanism of action of small molecule perturbagens. Here, we developed a 96-well-plate-based high-throughput screening infrastructure for quantitative proteomics and profiled 875 compounds in a human cancer cell ...
Mechanism of action describes the process by which a molecule, such as a drug, functions to produce a pharmacological effect. A drug’s mechanism of action may refer to its effects on a biological readout such as cell growth, or its interaction and modulation of its direct biomolecular target...
After 50 years of use, has the molecular mode of action finally been identified for pyrazinamide? Recently, inhibition of trans-translation in Mycobacterium tuberculosis was suggested as a novel mode of action for this important TB drug. The results of the study by Zhang et al., reported in ...
The low-grade inflammation is pivotal in obesity and its comorbidities; however, the inflammatory proteins are out of target for traditional drug therapy. Omega-3 (ω3) fatty acids can modulate the downstream signaling of Toll-like receptor (TLR) and tumor necrosis factor-α receptor (TNFα) ...
resistant (MDR) HIV-1, FTR is well tolerated and virologically active. According to recent investigations, drug combination therapy can positively affect MDR-HIV. The mechanism of action, resistance, interaction, pharmacokinetics, pharmacodynamics, and safety of FTR has been highlighted in this review...
View PDFView articleView in ScopusGoogle Scholar [3] A.M. Khot, H.V. Anuradha, V.S. Prakash, M.C. Shivamurathy Antianginal efficacy and tolerability of ranolazine as an add-on drug to concomitant medications primarily metoprolol in chronic stable angina patients: a prospective, open-label...
2A), String database and Cytoscape3.2.1 software were used to draw the protein interaction network, and Systems Dock Web Site was used to perform molecular docking verification of components and targets (Fig. 2B). In order to gain a deeper understanding of the relationships between the drug, ...
In vitro and in vivo studies have found that kp acts as an analgesic in a preclinical mouse model of pathological pain and that its cellular mechanism of action in neurons is based on its GSK-3β inhibitory function, which enhances Kcc2/KCC2 gene expression. In turn, Kcc2 upregulation is...
The inflammasomes are innate immune system receptors and sensors that regulate the activation of caspase-1 and induce inflammation in response to infectious microbes and molecules derived from host proteins. They have been implicated in a host of inflamm
Cellular target engagement technologies enable quantification of intracellular drug binding, but the simultaneous assessment of drug-associated phenotypes is challenging. Here, the authors develop CeTEAM (cellular target engagement by accumulation of mutant), a platform that can simultaneously evaluate drug-...