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Linning Yu

Explore the profile of Linning Yu including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 13
Citations 165
Followers 0
Related Specialties
Toxicology
Pharmacology
Biochemistry
Top 10 Co-Authors
Judy L Bolton
Abdul Mutlib
Richard B van Breemen
Rasmy Talaat
Joann Scatina
Robert Espina
Gregory R J Thatcher
Yan Li
Jiaqin Yao
Jianyao Wang
Published In
Chem Res Toxicol
Mol Pharm
Methods Enzymol
Chem Biol Drug Des
Mutat Res
Affiliations
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Recent Articles
1.
Characterization of HKI-272 covalent binding to human serum albumin
Wang J, Li-Chan X, Atherton J, Deng L, Espina R, Yu L, et al.
Drug Metab Dispos . 2010 Apr; 38(7):1083-93. PMID: 20400660
The study was initiated as an observation of incomplete extraction recovery of N-(4-(3-chloro-4-(2-pyridinylmethoxy)anilino)-3-cyano-7-ethoxy-6-quinolyl)-4-(dimethylamino)-2-butenamide (HKI-272) from human plasma. The objective of this study was to 1) identify the binding site(s) of...
2.
Bioactivation of lamotrigine in vivo in rat and in vitro in human liver microsomes, hepatocytes, and epidermal keratinocytes: characterization of thioether conjugates by liquid chromatography/mass spectrometry and high field nuclear magnetic...
Chen H, Grover S, Yu L, Walker G, Mutlib A
Chem Res Toxicol . 2009 Dec; 23(1):159-70. PMID: 19961160
Previous studies suggested that lamotrigene (LTG) underwent bioactivation to a reactive aryl epoxide intermediate in rats. Nevertheless, definitive structures of these thioether conjugates, which are often needed to substantiate the...
3.
Obtaining exposures of metabolites in preclinical species through plasma pooling and quantitative NMR: addressing metabolites in safety testing (MIST) guidance without using radiolabeled compounds and chemically synthesized metabolite standards
Vishwanathan K, Babalola K, Wang J, Espina R, Yu L, Adedoyin A, et al.
Chem Res Toxicol . 2008 Dec; 22(2):311-22. PMID: 19067650
The recent guidance on "Safety Testing of Drug Metabolites" issued by the U.S. Food and Drug Administration, Center for Drug Evaluation and Research (CDER) has highlighted the importance of identifying...
4.
Nuclear magnetic resonance spectroscopy as a quantitative tool to determine the concentrations of biologically produced metabolites: implications in metabolites in safety testing
Espina R, Yu L, Wang J, Tong Z, Vashishtha S, Talaat R, et al.
Chem Res Toxicol . 2008 Nov; 22(2):299-310. PMID: 18980340
Nuclear magnetic resonance (NMR) spectroscopy has traditionally been considered as an indispensable tool in elucidating structures of metabolites. With the advent of Fourier transform (FT) spectrometers, along with improvements in...
5.
Efficient use of the iron ortho-nitrophenylporphyrin chloride to mimic biological oxidations of dimethylaminoantipyrine
Bazin M, Shi H, Delaney J, Kline B, Zhu Z, Kuhn C, et al.
Chem Biol Drug Des . 2007 Oct; 70(4):354-9. PMID: 17937780
Major metabolites of dimethylaminoantipyrine have been synthesized using iron ortho-nitrophenylporphyrin chloride as biomimetic catalyst. Reactivity of iron tetrakis-ortho-nitrophenylporphyrin chloride [Fe(TNO2PP)Cl] has been compared with iron tetrakis-pentafluorophenylporphyrin chloride and iron tetrakis-2,6-dichlorophenylporphyrin...
6.
A rational chemical intervention strategy to circumvent bioactivation liabilities associated with a nonpeptidyl thrombopoietin receptor agonist containing a 2-amino-4-arylthiazole motif
Kalgutkar A, Driscoll J, Zhao S, Walker G, Shepard R, Soglia J, et al.
Chem Res Toxicol . 2007 Oct; 20(12):1954-65. PMID: 17935300
The current study examined the bioactivation potential of a nonpeptidyl thrombopoietin receptor agonist, 1-(3-chloro-5-((4-(4-fluoro-3-(trifluoromethyl)phenyl)thiazol-2-yl)carbamoyl)pyridine-2-yl)piperidine-4-carboxylic acid (1), containing a 2-carboxamido-4-arylthiazole moiety in the core structure. Toxicological risks arising from P450-catalyzed C4-C5...
7.
Breast cancer resistance protein (Bcrp/abcg2) is a major determinant of sulfasalazine absorption and elimination in the mouse
Zaher H, Khan A, Palandra J, Brayman T, Yu L, Ware J
Mol Pharm . 2006 May; 3(1):55-61. PMID: 16686369
Sulfasalazine is used in the treatment of ulcerative colitis, Crohn's disease, and rheumatoid arthritis. When administered orally, sulfasalazine is poorly absorbed with an estimated bioavailability of 3-12%. Recent studies using...
8.
Oxidation of raloxifene to quinoids: potential toxic pathways via a diquinone methide and o-quinones
Yu L, Liu H, Li W, Zhang F, Luckie C, van Breemen R, et al.
Chem Res Toxicol . 2004 Jul; 17(7):879-88. PMID: 15257612
Raloxifene was approved in 1997 by the FDA for the treatment of osteoporosis in postmenopausal women, and it is currently in clinical trials for the chemoprevention of breast cancer. Before...
9.
Equine estrogen metabolite 4-hydroxyequilenin induces anchorage-independent growth of human mammary epithelial MCF-10A cells: differential gene expression
Cuendet M, Liu X, Pisha E, Li Y, Yao J, Yu L, et al.
Mutat Res . 2004 May; 550(1-2):109-21. PMID: 15135645
Long-term exposure to synthetic and endogenous estrogens has been associated with the development of cancer in several tissues. One potential mechanism of estrogen carcinogenesis involves catechol formation and these catechols...
10.
Equine catechol estrogen 4-hydroxyequilenin is a more potent inhibitor of the variant form of catechol-O-methyltransferase
Li Y, Yao J, Chang M, Nikolic D, Yu L, Yager J, et al.
Chem Res Toxicol . 2004 Apr; 17(4):512-20. PMID: 15089093
Catechol-O-methyltransferase (COMT) plays an important role in the inactivation of biologically active and toxic catechols. It has been shown that COMT is genetically polymorphic with a wild-type and variant form...