Small molecule inhibitors
Small molecule inhibitors of protein-protein interactions
... . Small molecule inhibitors targeting six different PPIs have been developed in recent years to the point of entering clinical trials 14 ...(Bcl-2) small molecule inhibitor, ...
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Small Molecule Inhibitors of Protein-Protein Interactions
... design small molecule inhibitors using fast and efficient MCR ...active inhibitors of MDM2 and p53 interactions, with crystal structures confirming the benefits of targeting the known ...
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Identification and characterization of small-molecule inhibitors of hepsin.
... Abstract Hepsin is a type-II transmembrane serine protease overexpressed in the majority of human prostate cancers. We recently demonstrated that hepsin promotes prostate cancer progression and metastasis and thus ...
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Small Molecule Inhibitors of toxT Expression in Vibrio cholerae
... Small-Molecule Inhibitors of toxT Expression in Vibrio cholerae Rebecca Anthouard, Victor ...tify inhibitors of the virulence ...that small-molecule inhibitors of ...
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Tumor suppression by small molecule inhibitors of translation initiation
... #1181 are suitable probes for testing the hypothesis that small molecule inhibitors of translation initiation are mechanism specific anti-cancer agents. Here we report the anti-cancer efficacy, mode ...
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Novel Small-Molecule Inhibitors of RNA Polymerase III
... of small molecule inhibitors of RNA polymerase (Pol) III from Saccharomyces ...broad-spectrum inhibitors, displaying activity against RNA Pol III transcription systems derived from Candida ...
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Small molecule inhibitors of steroid receptors for breast and prostate cancer
... new small molecule inhibitors of androgen and estrogen receptor ...These inhibitors could then serve as starting points for the development of therapeutically relevant drugs and additionally ...
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The first small-molecule inhibitors of members of the ribonuclease E family
... Potent small molecule inhibitors that bind the active site of essential enzymes are proving to be a source of potential drug leads and tools to dissect function through chemical ...obtain ...
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Molecular basis of USP7 inhibition by selective small molecule inhibitors
... 25 Extended Data Figure 2. Compounds undergo selective USP7 target engagement in vitro and in cells. a, Schematic representation of DUB activity-based profiling of small molecule inhibitors. ...
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Molecular basis of USP7 inhibition by selective small molecule inhibitors
... 41 Extended Data Figure 2. USP7 target engagement and specificity in MCF7 cells. a, Schematic representation of DUB activity-based profiling of small molecule inhibitors. Compounds were incubated ...
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Interactions between arenavirus proteins and small molecule inhibitors of infection
... and Small Molecule Inhibitors of Infection Chairperson: Jack Nunberg Arenaviruses are globally distributed, negative-sense, single-stranded RNA viruses which persist in specific rodent host ...
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DISCOVERY, CHARACTERIZATION, AND DEVELOPMENT OF SMALL MOLECULE INHIBITORS OF GLYCOGEN SYNTHASE
... Only a few studies have identified molecules that target glycogen accumulation, including the widely-used glucose lowering T2D drug metformin 108,111 , the mTORC1 inhibitor, rapamycin, that indirectly suppress GS ...
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Small Molecule Inhibitors of CXCR4
... A series of dipyrimidine amines in which two heteroaromatic systems are connected by a p-xylyl-enediamine linker was already reported. These derivatives were identified through rational design and analyses of structural ...
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Small Molecule Inhibitors of PTP1B and TCPTP
... 0.1-10mM.The small sized fragments make the subsequent optimization is relatively easier to build the molecule by exploring the chemical space in the binding ...of small molecule compounds ...
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Small molecule inhibitors of Aβ-aggregation and neurotoxicity
... hybrid inhibitors from the study could prevent Ab aggregation; rather, they increased aggregate size and changed aggregate ...hybrid inhibitors might work via a mechanism that does not rely on a 1:1 complex ...
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Synthesis and Evaluation of Small Molecule Inhibitors of Pyruvate Carboxylase
... Docking of enol tautomers of 9a and 18 (Figure 4.3) with PC in the closed conformation reveals coordination of the carboxyl moiety with the metal ion in the active site, contrasted to pyruvate’s carboxyl moiety forming a ...
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Discovery of Small Molecule Inhibitors of Protein-Protein Interactions
... p53-Mdm2 inhibitors* *Adapted with permission from John Wiley and Sons: 2761080319960 The unmatched properties of the element fluorine are reflected in organofluorine ...of small molecules to its target, ...
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New Small-Molecule Inhibitors Effectively Blocking Picornavirus Replication
... IMPORTANCE Diverse picornaviruses can trigger multiple human maladies, yet currently, only hepatitis A virus and poliovirus can be con- trolled with vaccination. The development of antipicornavirus therapeutics is also ...
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Molecular basis of USP7 inhibition by selective small-molecule inhibitors
... for small molecules that could not have been predicted from available ...selective inhibitors for other family members will unveil the full therapeutic potential of DUB ...
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Targeting Tau Degradation by Small Molecule Inhibitors for Treatment of Tauopathies
... 17 Inhibitors of another chaperone, Hsp90, also have anti-tau ...Hsp70 inhibitors, these also facilitate tau degradation via the ...Hsp90 inhibitors for other diseases, in particular cancer, but the ...
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