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| 1 | Recent progress and challenges in screening and characterization of UGT1A1 inhibitors显示文摘Uridine-diphosphate glucuronosyltransferase 1 A1(UGT1 A1) is an important conjugative enzyme in mammals that is responsible for the conjugation and detoxification of both endogenous and xenobiotic compounds. Strong inhibition of UGT1 A1 may trigger adverse drug/herb–drug interactions, or result in metabolic disorders of endobiotic metabolism. Therefore, both the US Food and Drug Administration(FDA)and the European Medicines Agency(EMA) have recommended assaying the inhibitory potential of drugs under development on the human UGT1 A1 prior to approval. This review focuses on the significance,progress and challenges in discovery and characterization of UGT1 A1 inhibitors. Recent advances in the development of UGT1 A1 probes and their application for screening UGT1 A1 inhibitors are summarized and discussed in this review for the first time. Furthermore, a long list of UGT1 A1 inhibitors, including information on their inhibition potency, inhibition mode, and affinity, has been prepared and analyzed. Challenges and future directions in this field are highlighted in the final section. The information and knowledge that are presented in this review provide guidance for rational use of drugs/herbs in order to avoid the occurrence of adverse effects via UGT1 A1 inhibition, as well as presenting methods for rapid screening and characterization of UGT1 A1 inhibitors and for facilitating investigations on UGT1 A1–ligand interactions. | Xia Lv Yangliu Xia Moshe Finel Jingjing Wu Guangbo Ge Ling Yang | 2019 | Acta Pharmaceutica Sinica B2019，9，2： | 14 |
| 2 | An ultra-sensitive and easy-to-use assay for sensing human UGT1A1 activities in biological systems显示文摘The human UDP-glucuronosyltransferase 1A1(UGT1A1),one of the most essential conjugative enzymes,is responsible for the metabolism and detoxification of bilirubin and other endogenous substances,as well as many different xenobiotic compounds.Deciphering UGT1A1 relevance to human diseases and characterizing the effects of small molecules on the activities of UGT1A1 requires reliable tools for probing the function of this key enzyme in complex biological matrices.Herein,an easy-to-use assay for highly-selective and sensitive monitoring of UGT1A1 activities in various biological matrices,using liquid chromatography with fluorescence detection(LC-FD),has been developed and validated.The newly developed LC-FD based assay has been confirmed in terms of sensitivity,specificity,precision,quantitative linear range and stability.One of its main advantages is lowering the limits of detection and quantification by about 100-fold in comparison to the previous assay that used the same probe substrate,enabling reliable quantification of lower amounts of active enzyme than any other method.The precision test demonstrated that both intra-and inter-day variations for this assay were less than 5.5%.Furthermore,the newly developed assay has also been successfully used to screen and characterize the regulatory effects of small molecules on the expression level of UGT1A1 in living cells.Ove rall,an easy-to-use LC-FD based assay has been developed for ultra-sensitive UGT1A1 activities measurements in various biological systems,providing an inexpensive and practical approach for exploring the role of UGT1A1 in human diseases,interactions with xenobiotics,and characterization modulatory effects of small molecules on this conjugative enzyme. | Ya-Di Zhu Hui-Lin Pang Qi-Hang Zhou Zi-Fei Qin Qiang Jin Moshe Finel Yi-Nan Wang Wei-Wei Qin Yin Lu Dan-Dan Wang Guang-Bo Ge | 2020 | Journal of Pharmaceutical Analysis2020，10，3： | 2 |
| 3 | Allelic Deter- minants of Vitamin D Insufficiency, Bone Mineral Density, and Bor Fractures显示文摘 | Trummer O Schwetz V Walter - Finell D | 2012 | J Clin Endocrinol Metab2012，97，7： | 1 |
| 4 | Arsenic Removal by Native and Chemically Modified Lacti- cacid Bateria 显示文摘 | TEEMU HALTTUNEN MATTIAS FINELL SEPPO SALMINEN | 2007 | International Journal of Food Microbiology2007，120，2007： | 1 |
| 5 | Coupling phase field and viscoplasticity to study rafting in Ni-base superalloys显示文摘 | Gauberta A Bouar Y L Finel A | 2010 | Philosophical Magazine2010，90，： | 1 |
| 6 | A simple method to determine nanogram levels of 4-hydroxyproline in biological tissue显示文摘 | Jamall IS Finell VN Que Hee SS | 1981 | Anal Biochem1981，112，1： | 1 |
| 7 | Investigation of coherency loss by prismatic punching with a nonlinear elastic model显示文摘 | Geslin P A Appolaire B Finel A | 2014 | Acta Materialia2014，71，： | 1 |
| 8 | Synthesis, structure characterization, and enzyme screening of clenbuterol glucuronides显示文摘 | Anna Alonen Minna Gartman Olli Aitio Moshe Finel Jari Yli-Kauhaluoma Risto Kostiainen | 2009 | European Journal of Pharmaceutical Sciences2009，，5： | 1 |
| 9 | Arsenic removal by native and chemically modified lactic acid bacteria显示文摘 | TEEMU HALTTUNEN MATHAS FINELL SEPPO SALMINEN | 2007 | international Journal of Food Microbiology2007，120，： | 1 |
| 10 | The human UDP-glucuronosyltransferase UGT1A3 is highly selective towards N2 in the tetrazole ring of losartan,candesartan,and zolarsartan显示文摘 | Alonen A Finel M Kostiaiene R | | 0，，06： | 1 |
| 11 | Non-steroidal antiinflammatory drugs interact with testosterone glucuronidation显示文摘 | Sten T Finel M Ask B | 2009 | Steroids2009，74，12： | 1 |
| 12 | N-glucuronidation of drugs and other xenobiotics by human and animal UDP-glucuronosyltransferases显示文摘 | Kaivosaari S Finel M Koskinen M | | 0，，08： | 1 |
| 13 | N-glucuronidation of drugs and other xenobiotics by human and animal UDP-glucuronosyltrans- ferases 显示文摘 | Kaivosaari S Finel M Koskinen M | 2011 | Xenobiotica2011，41，8： | 1 |
| 14 | High-throughput screening technologies for drug glucuronidation profiling显示文摘 | TRUBETSKOY O FINEL hi TRUBETSKOY V | 2008 | J Pharm Pharmaco12008，60，8： | 1 |
| 15 | Coupling Phase Field and Vis- coplasticity to Study Rafting in Ni-Based Superalloys 显示文摘 | Gaubert A Le Bouar Y Finel A | 2010 | Philo- sophicalMagazine2010，90，14： | 1 |
| 16 | Effects of extractives on the physical characteristics of Scots pine sawdust fuel pellets显示文摘 | BERGSTR?M D FINELL M GREF R | 2010 | Forest Products Journal2010，60，7： | 1 |
| 17 | 显示文摘 | Jacquot J M Pelissier J Finels H Strubel D | 1999 | Presse médicale(Paris France:1983)1999，28，33： | 1 |
| 18 | In situ diffuse scatterings of neutrons on binary alloys显示文摘 | Caudron R Barrachin M Finel Y | 1992 | Phsica B:Condensed Matter1992，180，6： | 1 |
| 19 | Imagingapproaches for evaluating peripheral joint abnormalities injuvenile idiopathic arthritis显示文摘 | Breton S Jousse-Joulin S Finel E | 2012 | Semin Arthritis Rheum2012，41，5： | 1 |
| 20 | Autologous Hematopoietic Stem Cell Transplantation for Plasmablastic Lymphoma: The European Society for Blood and Marrow Transplantation Experience 显示文摘 | Cattaneo C Finel H McQuaker G | 2015 | Biol Blood Marrow Transplant2015，21，： | 1 |
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