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Page 1
Use of cloned and expressed human UDP-glucuronosyltransferases for the assessment of human drug conjugation and identification of potential drug interactions.
Ethell BT, Beaumont K, Rance DJ, Burchell B. Ethell BT, et al. Drug Metab Dispos. 2001 Jan;29(1):48-53. Drug Metab Dispos. 2001. PMID: 11124229
The meta and para phenols, UK-156,037 and UK-157,147, were found to be substrates for UGT1A1 with K(m) values of 256 and 105 microM, respectively. The ortho phenol UK-157,261 was glucuronidated predominantly by UGT1A9 with a K(m) of 45 microM. The latter K(m) …
The meta and para phenols, UK-156,037 and UK-157,147, were found to be substrates for UGT1A1 with K(m) values of 256 and 105 microM, …
Determining the incidence of interstitial pneumonitis and chronic kidney disease following full intensity haemopoetic stem cell transplant conditioned using a forward-planned intensity modulated total body irradiation technique.
Durie E, Nicholson E, Anthias C, Dunne EM, Potter M, Ethell M, Messiou C, Brennan J, Eagle S, Talbot J, Smyth G, Ingram W, Saran F, Mandeville HC. Durie E, et al. Among authors: ethell m. Radiother Oncol. 2021 May;158:97-103. doi: 10.1016/j.radonc.2021.02.020. Epub 2021 Feb 23. Radiother Oncol. 2021. PMID: 33636231

Toxicities were defined as per CTCAE v4.0: IP as multilobar infiltrates on CT with symptoms of dyspnoea, and renal dysfunction as an Estimated Glomerular Filtration rate (eGFR) < 60 ml/min/1.73 m(2) for > 3 months. Secondary endpoints were overall survival (OS), prog

…
Toxicities were defined as per CTCAE v4.0: IP as multilobar infiltrates on CT with symptoms of dyspnoea, and renal dysfunction as an Estimat …
The effect of valproic acid on drug and steroid glucuronidation by expressed human UDP-glucuronosyltransferases.
Ethell BT, Anderson GD, Burchell B. Ethell BT, et al. Biochem Pharmacol. 2003 May 1;65(9):1441-9. doi: 10.1016/s0006-2952(03)00076-5. Biochem Pharmacol. 2003. PMID: 12732356
Valproic acid glucuronidation kinetics were carried our with three human UGT isoforms: UGT1A6, UGT1A9, and UGT2B7 as well as human liver and kidney microsomes. The glucuronidation of valproic acid was typified by high K(m) values with microsomes and expressed UGTs (2.3-5.2 …
Valproic acid glucuronidation kinetics were carried our with three human UGT isoforms: UGT1A6, UGT1A9, and UGT2B7 as well as human liver and …
Glucuronidation of dihydroartemisinin in vivo and by human liver microsomes and expressed UDP-glucuronosyltransferases.
Ilett KF, Ethell BT, Maggs JL, Davis TM, Batty KT, Burchell B, Binh TQ, Thu le TA, Hung NC, Pirmohamed M, Park BK, Edwards G. Ilett KF, et al. Among authors: ethell bt. Drug Metab Dispos. 2002 Sep;30(9):1005-12. doi: 10.1124/dmd.30.9.1005. Drug Metab Dispos. 2002. PMID: 12167566
In human liver microsomal incubations, DHA-G (diastereomer unspecified) was the only metabolite found (V(max) 177 +/- 47 pmol min(-1) mg(-1), K(m) 90 +/- 16 microM). Alpha-DHA-G was formed in incubations of DHA with expressed UGT1A9 (K(m) 32 microM, V(max) 8.9 pmol …
In human liver microsomal incubations, DHA-G (diastereomer unspecified) was the only metabolite found (V(max) 177 +/- 47 pmol min(-1) mg(-1) …
The specificity of glucuronidation of entacapone and tolcapone by recombinant human UDP-glucuronosyltransferases.
Lautala P, Ethell BT, Taskinen J, Burchell B. Lautala P, et al. Among authors: ethell bt. Drug Metab Dispos. 2000 Nov;28(11):1385-9. Drug Metab Dispos. 2000. PMID: 11038168
The kinetic data illustrates that UGT1A9 exhibited a much greater rate of glucuronidation and a far lower K(m) value for both entacapone and tolcapone than UGT2B15 and UGT2B7 whose contribution is minor by comparison. Entacapone showed a 3 to 4 times higher V(max) value an …
The kinetic data illustrates that UGT1A9 exhibited a much greater rate of glucuronidation and a far lower K(m) value for both entacap …
Cloning and characterisation of the first drug-metabolising canine UDP-glucuronosyltransferase of the 2B subfamily.
Soars MG, Fettes M, O'Sullivan AC, Riley RJ, Ethell BT, Burchell B. Soars MG, et al. Among authors: ethell bt. Biochem Pharmacol. 2003 Apr 15;65(8):1251-9. doi: 10.1016/s0006-2952(03)00064-9. Biochem Pharmacol. 2003. PMID: 12694866
The following results were obtained: (i) sequence alignments between UGT2B31 and UGT2B15 gave the greatest degree of identity (76%); however, human UGT2B4, human UGT2B7, monkey UGT2B9 (all 75%), and rat UGT2B1 (73%) also gave a high degree of identity; (ii) phylogenetic analysis …
The following results were obtained: (i) sequence alignments between UGT2B31 and UGT2B15 gave the greatest degree of identity (76%); however …
Quantitative structure activity relationships for the glucuronidation of simple phenols by expressed human UGT1A6 and UGT1A9.
Ethell BT, Ekins S, Wang J, Burchell B. Ethell BT, et al. Drug Metab Dispos. 2002 Jun;30(6):734-8. doi: 10.1124/dmd.30.6.734. Drug Metab Dispos. 2002. PMID: 12019203
However, the affinity of UGT1A6 for these compounds exhibited higher K(m) values than UGT1A9, although rates of turnover were similar. ...The K(m) values for UGT1A9 showed a similar relationship to UGT1A6 but with much lower K(m) values and greater variabilit …
However, the affinity of UGT1A6 for these compounds exhibited higher K(m) values than UGT1A9, although rates of turnover were similar …
Rituximab, Gemcitabine, Cisplatin and Methylprednisolone (R-GEM-P) is an effective regimen in relapsed diffuse large B-cell lymphoma.
Barton S, Hawkes EA, Cunningham D, Peckitt C, Chua S, Wotherspoon A, Attygalle A, Horwich A, Potter M, Ethell M, Dearden C, Gleeson M, Chau I. Barton S, et al. Among authors: ethell m. Eur J Haematol. 2015 Mar;94(3):219-26. doi: 10.1111/ejh.12416. Epub 2014 Aug 18. Eur J Haematol. 2015. PMID: 25039915
METHODS: We assessed the efficacy and safety of GEM-P+/-R in a retrospective single-centre analysis including patients meeting criteria of 18 yr of age, histologically proven DLBCL, treated between 2001 and 2011 in second-line with gemcitabine 1000 mg/m(2) day 1, 8 and 15, …
METHODS: We assessed the efficacy and safety of GEM-P+/-R in a retrospective single-centre analysis including patients meeting criteria of 1 …
The role of maintenance chemotherapy after autotransplantation for acute lymphoblastic leukemia in first remission: single-center experience of 100 patients.
Sirohi B, Powles R, Treleaven J, Kulkarni S, Saso R, Potter M, Ethell M, Morgan G, Singhal S, Mehta J. Sirohi B, et al. Among authors: ethell m. Bone Marrow Transplant. 2008 Jul;42(2):105-12. doi: 10.1038/bmt.2008.95. Epub 2008 Apr 14. Bone Marrow Transplant. 2008. PMID: 18408773
A total of 100 adults with ALL in first CR received melphalan (110 mg/m(2)) with TBI followed by autologous marrow (n=35) or single-agent melphalan (200 mg/m(2)) followed by autologous blood stem cells (n=65). ...
A total of 100 adults with ALL in first CR received melphalan (110 mg/m(2)) with TBI followed by autologous marrow (n=35) or single-a …