Niemann-Pick C1 Like 1 (NPC1L1) Is the Intestinal Phytosterol and Cholesterol Transporter and a Key Modulator of Whole-body Cholesterol Homeostasis*
- H. Davis, Li‐ji Zhu, S. Altmann
- BiologyJournal of Biological Chemistry
- 6 August 2004
NPC1L1 is required for intestinal uptake of both cholesterol and phytosterols and plays a major role in cholesterol homeostasis and may be a useful drug target for the treatment of hypercholesterolemia and sitosterolemia.
Tumor Cells Chronically Treated with a Trastuzumab–Maytansinoid Antibody–Drug Conjugate Develop Varied Resistance Mechanisms but Respond to Alternate Treatments
- F. Loganzo, X. Tan, H. Gerber
- BiologyMolecular Cancer Therapeutics
- 2 February 2015
Antibody–drug conjugates (ADC) are emerging as clinically effective therapy. We hypothesized that cancers treated with ADCs would acquire resistance mechanisms unique to immunoconjugate therapy and…
Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications.
- A. Maderna, M. Doroski, C. J. O’Donnell
- Chemistry, BiologyJournal of Medicinal Chemistry
- 2014
The design and synthesis of several new auristatins with N-terminal modifications that include amino acids with α,α-disubstituted carbon atoms are described, including the discovery of the lead auristatin, PF-06380101.
A Potent Synthetic LXR Agonist Is More Effective than Cholesterol Loading at Inducing ABCA1 mRNA and Stimulating Cholesterol Efflux*
- C. Sparrow, J. Baffic, J. Menke
- Biology, ChemistryJournal of Biological Chemistry
- 22 March 2002
Data show that APD is a more effective LXR agonist than endogenous oxysterols, and may therefore be useful for the prevention and treatment of atherosclerosis, especially in the context of low HDL levels.
A fluorescent cholesterol analog traces cholesterol absorption in hamsters and is esterified in vivo and in vitro.
- C. Sparrow, S. Patel, P. Detmers
- Biology, ChemistryJournal of Lipid Research
- 1 October 1999
Fluoresterol apparently interacts with the proteins required for cholesterol uptake, trafficking, and processing in the small intestine.
Different roles of liver X receptor alpha and beta in lipid metabolism: effects of an alpha-selective and a dual agonist in mice deficient in each subtype.
- E. Lund, L. Peterson, C. Sparrow
- BiologyBiochemical Pharmacology
- 2006
The data lend further experimental support to the hypothesis that LXRbeta-selective agonists may raise HDL-cholesterol and stimulate macrophage cholesterol efflux without causing liver triglyceride accumulation.
A novel liver X receptor agonist establishes species differences in the regulation of cholesterol 7alpha-hydroxylase (CYP7a).
- J. Menke, K. Macnaul, C. Sparrow
- Biology, ChemistryEndocrinology
- 2002
A synthetic molecule named F(3)MethylAA [3-chloro-4-(3-(7-propyl-3-trifluoromethyl-6-(4,5)-isoxazolyl)propylthio)-phenyl acetic acid] that is more potent than 22(R)-hydroxycholesterol in LXR in vitro assays is described.
Characterization of a platelet-activating factor receptor antagonist isolated from haifenteng (Piper futokadsura): specific inhibition of in vitro and in vivo platelet-activating factor-induced…
- T. Shen, S. Hwang, R. Li
- Biology, MedicineProceedings of the National Academy of Sciences…
- 1 February 1985
A novel antagonist of PAF is identified in the methylene chloride extract of a Chinese herbal plant, haifenteng, which inhibits PAF-induced increases of hematocrit and circulating N-acetylglucosaminidase in the rat at greater than 10 mg/kg i.p. in a dose-dependent manner.
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