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A non-toxic Hsp90 inhibitor protects neurons from Abeta-induced toxicity.
The molecular chaperones have been implicated in numerous neurodegenerative disorders in which the defining pathology is misfolded proteins and the accumulation of protein aggregates. In Alzheimer'sExpand
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TCP-FA4: a derivative of tranylcypromine showing improved blood-brain permeability.
A variety of approaches have been taken to improve the brain penetration of pharmaceutical agents. The amphipathic character of a compound can improve its interaction with the lipid bilayer withinExpand
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Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis
  • X. Wang, B. Liu, +14 authors P. Kym
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • 5 January 2018
Cystic fibrosis (CF) is a multiorgan disease of the lungs, sinuses, pancreas, and gastrointestinal tract that is caused by a dysfunction or deficiency of the cystic fibrosis transmembrane conductanceExpand
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Improving blood brain barrier permeation of small molecules exhibiting chemotherapeutic and neuroprotective effects
The molecular chaperones have been implicated in numerous neurodegenerative disorders in which a defining pathology is misfolded proteins and the accumulation of protein aggregates. In Alzheimer’sExpand
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Placental ABC Transporters: Biological Impact and Pharmaceutical Significance
The human placenta fulfills a variety of essential functions during prenatal life. Several ABC transporters are expressed in the human placenta, where they play a role in the transport of endogenousExpand
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In silico, in vitro and in situ models to assess interplay between CYP3A and P-gp.
The bioavailability, fraction of dose that reaches systemic circulation, of orally administered drugs is often limited by both physical barriers of the intestine (e.g., unstirred-water and mucosalExpand
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In Silico Absorption, Distribution, Metabolism, Excretion, and Pharmacokinetics (ADME-PK): Utility and Best Practices. An Industry Perspective from the International Consortium for Innovation through
In silico tools to investigate absorption, distribution, metabolism, excretion, and pharmacokinetics (ADME-PK) properties of new chemical entities are an integral part of the current industrial drugExpand
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Paclitaxel succinate analogs: Anionic and amide introduction as a strategy to impart blood-brain barrier permeability.
A focused library of TX-67 (C10 hemi-succinate) analogs has been prepared, including C7 regioisomers, esters, amides, and one-carbon homologs. These were prepared to investigate whether the lack ofExpand
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Preclinical absorption, distribution, metabolism and excretion (ADME) characterization of ICAM1988, an LFA-1/ICAM antagonist, and its prodrug
Intercellular adhesion molecule (ICAM)-1988 is a small molecule lymphocyte function-associated antigen-1 (LFA-1) antagonist being considered for its anti-inflammatory properties. FollowingExpand
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Single-site chemical modification at C10 of the baccatin III core of paclitaxel and Taxol C reduces P-glycoprotein interactions in bovine brain microvessel endothelial cells.
A single-site modification of paclitaxel analogs at the C10 position on the baccatin III core that reduces interaction with P-glycoprotein in bovine brain microvessel endothelial cells is described.Expand
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