K
Kelem Kassahun
Researcher at United States Military Academy
Publications - 16
Citations - 1362
Kelem Kassahun is an academic researcher from United States Military Academy. The author has contributed to research in topics: Integrase & Chemistry. The author has an hindex of 12, co-authored 13 publications receiving 1302 citations.
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Journal ArticleDOI
A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase.
Daria J. Hazuda,Neville J. Anthony,Robert P. Gomez,Samson M. Jolly,John S. Wai,Linghang Zhuang,Thorsten E. Fisher,Mark Embrey,James P. Guare,Melissa S. Egbertson,Joseph P. Vacca,Joel R. Huff,Peter J. Felock,Marc V. Witmer,Kara A. Stillmock,Robert M. Danovich,Jay A. Grobler,Michael D. Miller,Amy S. Espeseth,Lixia Jin,I.-W. Chen,Jiunn H. Lin,Kelem Kassahun,Joan D. Ellis,Bradley K. Wong,Wei Xu,Paul G. Pearson,William A. Schleif,Riccardo Cortese,Emilio A. Emini,Vincenzo Summa,M. Katharine Holloway,Steven D. Young +32 more
TL;DR: These studies provide a structural basis and rationale for developing integrase inhibitors with the potential for unique and nonoverlapping resistance profiles and propose a model of the two inhibitors that is consistent with this observation and suggests specific interactions with discrete binding sites for each ligand.
Journal ArticleDOI
Studies on the metabolism of troglitazone to reactive intermediates in vitro and in vivo. Evidence for novel biotransformation pathways involving quinone methide formation and thiazolidinedione ring scission.
Kelem Kassahun,Paul G. Pearson,Wei Tang,Ian McIntosh,Kwan Leung,Charles S. Elmore,Dennis C. Dean,Regina Wang,George Doss,Thomas A. Baillie +9 more
TL;DR: The finding that metabolism of the TZD ring of troglitazone was catalyzed selectively by P450 3A enzymes is significant in light of the recent report that trog litazone is an inducer of this isoform in human hepatocytes.
Journal ArticleDOI
Metabolism and disposition in humans of raltegravir (MK-0518), an anti-AIDS drug targeting the human immunodeficiency virus 1 integrase enzyme.
Kelem Kassahun,Ian McIntosh,Donghui Cui,David Hreniuk,Shelia A. Merschman,Kenneth C. Lasseter,Neal Azrolan,Marian Iwamoto,John A. Wagner,Larissa Wenning +9 more
TL;DR: The data indicate that the major mechanism of clearance of raltegravir in humans is UGT1A1-mediated glucuronidation, which is similar to that demonstrated in rats.
Journal ArticleDOI
In Vitro and in Vivo Evaluation of Dihydropyrimidinone C-5 Amides as Potent and Selective α1A Receptor Antagonists for the Treatment of Benign Prostatic Hyperplasia
James C. Barrow,Philippe G. Nantermet,Harold G. Selnick,Kristen L. Glass,Kenneth E. Rittle,Kevin F. Gilbert,Thomas G. Steele,Carl F. Homnick,Roger M. Freidinger,Rick W. Ransom,Paul J. Kling,Duane R. Reiss,Theodore P. Broten,Terry W. Schorn,Raymond S.L. Chang,Stacey O'Malley,Timothy V. Olah,Joan D. Ellis,A. Barrish,Kelem Kassahun,Paula Leppert,Dhanapalan Nagarathnam,Carlos Forray +22 more
TL;DR: While many of the compounds tested displayed poor pharmacokinetics, compound 48 was found to be more potent than terazosin in both a rat model of prostate tone and a dog model of intra-urethral pressure without significantly affecting blood pressure.
Journal Article
Disposition and Metabolism of Olanzapine in Mice, Dogs, and Rhesus Monkeys
Edward L. Mattiuz,Ronald B. Franklin,Todd A. Gillespie,Anthony T. Murphy,John R. Bernstein,Andre Chiu,Terry Hotten,Kelem Kassahun +7 more
TL;DR: The pharmacokinetics, excretion, and metabolism of OLZ were studied in CD-1 mice, beagle dogs, and rhesus monkeys after a single oral and/or intravenous dose of [14C]OLZ.