Full Text Journal Articles by
Author Eric F Johnson

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Corrigendum to "Investigation of biaryl heterocycles as inhibitors of Wee1 kinase" [Bioorg. Med. Chem. Lett. 29 (2019) 1481-1486].

Anthony Mastracchio, Chunqiu Lai, Maricel Torrent, Kenneth Bromberg, Fritz G Buchanan, Debra Ferguson, Velitchka Bontcheva, Eric F Johnson, Loren Lasko, David Maag, Alexander R Shoemaker, Thomas D Penning,

Bioorg. Med. Chem. Lett. (Bioorganic & Medicinal Chemistry Letters)
[2020, 30(4):126895]

Cited: 0 times

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Investigation of biaryl heterocycles as inhibitors of Wee1 kinase.

Anthony Mastracchio, Chunqiu Lai, Maricel Torrent, Kenneth Bromberg, Fritz G Buchanan, Debra Ferguson, Velitchka Bontcheva, Eric F Johnson, Loren Lasko, David Maag, Alexander R Shoemaker, Thomas D Penning,

In continuation of our previous research towards the discovery of potent, selective and drug-like Wee1 inhibitors, 2 novel series of biaryl heterocycles were designed, synthesized and evaluated. The new biaryl cores were designed to enable structure-activity exploration of substituents at C-8 or N-8 which were used for tuning compound properties ... Read more >>

Bioorg. Med. Chem. Lett. (Bioorganic & medicinal chemistry letters)
[2019, 29(12):1481-1486]

Cited: 0 times

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Active-site differences between substrate-free and ritonavir-bound cytochrome P450 (CYP) 3A5 reveal plasticity differences between CYP3A5 and CYP3A4.

Mei-Hui Hsu, Eric F Johnson,

Cytochrome P450 (CYP) 3A4 is a major contributor to hepatic drug and xenobiotic metabolism in human adults. The related enzyme CYP3A5 is also expressed in adult liver and has broader age and tissue distributions. However, CYP3A5 expression is low in most Caucasians because of the prevalence of an allele that ... Read more >>

J. Biol. Chem. (The Journal of biological chemistry)
[2019, 294(20):8015-8022]

Cited: 0 times

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PARP1 Trapping by PARP Inhibitors Drives Cytotoxicity in Both Cancer Cells and Healthy Bone Marrow.

Todd A Hopkins, William B Ainsworth, Paul A Ellis, Cherrie K Donawho, Enrico L DiGiammarino, Sanjay C Panchal, Vivek C Abraham, Mikkel A Algire, Yan Shi, Amanda M Olson, Eric F Johnson, Julie L Wilsbacher, David Maag,

PARP inhibitors have recently been approved as monotherapies for the treatment of recurrent ovarian cancer and metastatic BRCA-associated breast cancer, and ongoing studies are exploring additional indications and combinations with other agents. PARP inhibitors trap PARP onto damaged chromatin when combined with temozolomide and methyl methanesulfonate, but the clinical relevance ... Read more >>

Mol. Cancer Res. (Molecular cancer research : MCR)
[2019, 17(2):409-419]

Cited: 13 times

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Noncovalent interactions dominate dynamic heme distortion in cytochrome P450 4B1.

Gareth K Jennings, Mei-Hui Hsu, Lisa S Shock, Eric F Johnson, John C Hackett,

Cytochrome P450 4B1 (4B1) functions in both xenobiotic and endobiotic metabolism. An ester linkage between Glu-310 in 4B1 and the 5-methyl group of heme facilitates preferential hydroxylation of terminal (ω) methyl groups of hydrocarbons (HCs) and fatty acids compared with ω-1 sites bearing weaker C-H bonds. This preference is retained ... Read more >>

J. Biol. Chem. (The Journal of biological chemistry)
[2018, 293(29):11433-11446]

Cited: 2 times

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The X-Ray Crystal Structure of the Human Mono-Oxygenase Cytochrome P450 3A5-Ritonavir Complex Reveals Active Site Differences between P450s 3A4 and 3A5.

Mei-Hui Hsu, Uzen Savas, Eric F Johnson,

The contributions of cytochrome P450 3A5 to the metabolic clearance of marketed drugs is unclear, but its probable role is to augment the metabolism of several drugs that are largely cleared by P450 3A4. Selective metabolism by 3A4 is often a concern in drug development owing to potential drug-drug interactions ... Read more >>

Mol. Pharmacol. (Molecular pharmacology)
[2018, 93(1):14-24]

Cited: 4 times

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Determinants of the Inhibition of DprE1 and CYP2C9 by Antitubercular Thiophenes.

Renhe Liu, Xiaoxuan Lyu, Sarah M Batt, Mei-Hui Hsu, Michael B Harbut, Catherine Vilchèze, Bo Cheng, Kehinde Ajayi, Baiyuan Yang, Yun Yang, Hui Guo, Changyou Lin, Fei Gan, Chen Wang, Scott G Franzblau, William R Jacobs, Gurdyal S Besra, Eric F Johnson, Mike Petrassi, Arnab K Chatterjee, Klaus Fütterer, Feng Wang,

Mycobacterium tuberculosis (Mtb) DprE1, an essential isomerase for the biosynthesis of the mycobacterial cell wall, is a validated target for tuberculosis (TB) drug development. Here we report the X-ray crystal structures of DprE1 and the DprE1 resistant mutant (Y314C) in complexes with TCA1 derivatives to elucidate the molecular basis of ... Read more >>

Angew. Chem. Int. Ed. Engl. (Angewandte Chemie (International ed. in English))
[2017, 56(42):13011-13015]

Cited: 2 times

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Permanent Draft Genome Sequence of Desulfurococcus amylolyticus Strain Z-533T, a Peptide and Starch Degrader Isolated from Thermal Springs in the Kamchatka Peninsula and Kunashir Island, Russia.

Dwi Susanti, Eric F Johnson, Alla Lapidus, James Han, T B K Reddy, Supratim Mukherjee, Manoj Pillay, Anna A Perevalova, Natalia N Ivanova, Tanja Woyke, Nikos C Kyrpides, Biswarup Mukhopadhyay,

Desulfurococcus amylolyticus Z-533T, a hyperthermophilic crenarcheon, ferments peptide and starch, generating acetate, isobutyrate, isovalerate, CO2, and hydrogen. Unlike D. amylolyticus Z-1312, it cannot use cellulose and is inhibited by hydrogen. The reported draft genome sequence of D. amylolyticus Z-533T will help to understand the molecular basis for these differences. ... Read more >>

Genome Announc (Genome announcements)
[2017, 5(15):]

Cited: 1 time

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The Crystal Structure of Cytochrome P450 4B1 (CYP4B1) Monooxygenase Complexed with Octane Discloses Several Structural Adaptations for ω-Hydroxylation.

Mei-Hui Hsu, Brian R Baer, Allan E Rettie, Eric F Johnson,

P450 family 4 fatty acid ω-hydroxylases preferentially oxygenate primary C-H bonds over adjacent, energetically favored secondary C-H bonds, but the mechanism explaining this intriguing preference is unclear. To this end, the structure of rabbit P450 4B1 complexed with its substrate octane was determined by X-ray crystallography to define features of ... Read more >>

J. Biol. Chem. (The Journal of biological chemistry)
[2017, 292(13):5610-5621]

Cited: 9 times

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A dose-response study of separate and combined effects of the serotonin agonist 8-OH-DPAT and the dopamine agonist quinpirole on locomotor sensitization, cross-sensitization, and conditioned activity.

Eric F Johnson, Henry Szechtman,

Chronic treatment with the dopamine D2/D3 agonist, quinpirole, or the serotonin 1A agonist, 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT), induces behavioral sensitization. It is not known whether both drugs produce sensitization through a shared mechanism. Here, we examine whether quinpirole and 8-OH-DPAT show cross-sensitization and impact sensitization, as would be expected from shared mechanisms. ... Read more >>

Behav Pharmacol (Behavioural pharmacology)
[2016, 27(5):439-450]

Cited: 2 times

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A randomized Phase II study of veliparib with temozolomide or carboplatin/paclitaxel versus placebo with carboplatin/paclitaxel in BRCA1/2 metastatic breast cancer: design and rationale.

Steven J Isakoff, Shannon Puhalla, Susan M Domchek, Michael Friedlander, Bella Kaufman, Mark Robson, Melinda L Telli, Véronique Diéras, Hyo Sook Han, Judy E Garber, Eric F Johnson, David Maag, Qin Qin, Vincent L Giranda, Stacie P Shepherd,

Veliparib is an orally administered poly(ADP-ribose) polymerase inhibitor that is being studied in Phase I-III clinical trials, including Phase III studies in non-small-cell lung cancer, ovarian cancer and breast cancer. Tumor cells with deleterious BRCA1 or BRCA2 mutations are deficient in homologous recombination DNA repair and are intrinsically sensitive to ... Read more >>

Future Oncol (Future oncology (London, England))
[2017, 13(4):307-320]

Cited: 14 times

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20-Hydroxyeicosatetraenoic Acid (HETE)-dependent Hypertension in Human Cytochrome P450 (CYP) 4A11 Transgenic Mice: NORMALIZATION OF BLOOD PRESSURE BY SODIUM RESTRICTION, HYDROCHLOROTHIAZIDE, OR BLOCKADE OF THE TYPE 1 ANGIOTENSIN II RECEPTOR.

Üzen Savas, Shouzou Wei, Mei-Hui Hsu, John R Falck, F Peter Guengerich, Jorge H Capdevila, Eric F Johnson,

Male and female homozygous 129/Sv mice carrying four copies of the human cytochrome P450 4A11 gene (CYP4A11) under control of its native promoter (B-129/Sv-4A11(+/+)) develop hypertension (142 ± 8 versus 113 ± 7 mm Hg systolic blood pressure (BP)), and exhibit increased 20-hydroxyeicosatetraenoic acid (20-HETE) in kidney and urine. The ... Read more >>

J. Biol. Chem. (The Journal of biological chemistry)
[2016, 291(32):16904-16919]

Cited: 17 times

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Permanent draft genome sequence of Desulfurococcus mobilis type strain DSM 2161, a thermoacidophilic sulfur-reducing crenarchaeon isolated from acidic hot springs of Hveravellir, Iceland.

Dwi Susanti, Eric F Johnson, Alla Lapidus, James Han, T B K Reddy, Manoj Pilay, Natalia N Ivanova, Victor M Markowitz, Tanja Woyke, Nikos C Kyrpides, Biswarup Mukhopadhyay,

This report presents the permanent draft genome sequence of Desulfurococcus mobilis type strain DSM 2161, an obligate anaerobic hyperthermophilic crenarchaeon that was isolated from acidic hot springs in Hveravellir, Iceland. D. mobilis utilizes peptides as carbon and energy sources and reduces elemental sulfur to H2S. A metabolic construction derived from ... Read more >>

Stand Genomic Sci (Standards in genomic sciences)
[2016, 11:3]

Cited: 1 time

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Mechanistic Dissection of PARP1 Trapping and the Impact on In Vivo Tolerability and Efficacy of PARP Inhibitors.

Todd A Hopkins, Yan Shi, Luis E Rodriguez, Larry R Solomon, Cherrie K Donawho, Enrico L DiGiammarino, Sanjay C Panchal, Julie L Wilsbacher, Wenqing Gao, Amanda M Olson, DeAnne F Stolarik, Donald J Osterling, Eric F Johnson, David Maag,

Poly(ADP-ribose) polymerases (PARP1, -2, and -3) play important roles in DNA damage repair. As such, a number of PARP inhibitors are undergoing clinical development as anticancer therapies, particularly in tumors with DNA repair deficits and in combination with DNA-damaging agents. Preclinical evidence indicates that PARP inhibitors potentiate the cytotoxicity of ... Read more >>

Mol. Cancer Res. (Molecular cancer research : MCR)
[2015, 13(11):1465-1477]

Cited: 69 times

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Contributions of ionic interactions and protein dynamics to cytochrome P450 2D6 (CYP2D6) substrate and inhibitor binding.

An Wang, C David Stout, Qinghai Zhang, Eric F Johnson,

P450 2D6 contributes significantly to the metabolism of >15% of the 200 most marketed drugs. Open and closed crystal structures of P450 2D6 thioridazine complexes were obtained using different crystallization conditions. The protonated piperidine moiety of thioridazine forms a charge-stabilized hydrogen bond with Asp-301 in the active sites of both ... Read more >>

J. Biol. Chem. (The Journal of biological chemistry)
[2015, 290(8):5092-5104]

Cited: 24 times

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Pyrimidine-based tricyclic molecules as potent and orally efficacious inhibitors of wee1 kinase.

Yunsong Tong, Maricel Torrent, Alan S Florjancic, Kenneth D Bromberg, Fritz G Buchanan, Debra C Ferguson, Eric F Johnson, Loren M Lasko, David Maag, Philip J Merta, Amanda M Olson, Donald J Osterling, Nirupama Soni, Alexander R Shoemaker, Thomas D Penning,

Aided by molecular modeling, compounds with a pyrimidine-based tricyclic scaffold were designed and confirmed to inhibit Wee1 kinase. Structure-activity studies identified key pharmacophores at the aminoaryl and halo-benzene regions responsible for binding affinity with sub-nM K i values. The potent inhibitors demonstrated sub-μM activities in both functional and mechanism-based cellular ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2015, 6(1):58-62]

Cited: 3 times

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Correlating structure and function of drug-metabolizing enzymes: progress and ongoing challenges.

Eric F Johnson, J Patrick Connick, James R Reed, Wayne L Backes, Manoj C Desai, Lianhong Xu, D Fernando Estrada, Jennifer S Laurence, Emily E Scott,

This report summarizes a symposium sponsored by the American Society for Pharmacology and Experimental Therapeutics at Experimental Biology held April 20-24 in Boston, MA. Presentations discussed the status of cytochrome P450 (P450) knowledge, emphasizing advances and challenges in relating structure with function and in applying this information to drug design. ... Read more >>

Drug Metab. Dispos. (Drug metabolism and disposition: the biological fate of chemicals)
[2014, 42(1):9-22]

Cited: 11 times

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Structural diversity of eukaryotic membrane cytochrome p450s.

Eric F Johnson, C David Stout,

X-ray crystal structures are available for 29 eukaryotic microsomal, chloroplast, or mitochondrial cytochrome P450s, including two non-monooxygenase P450s. These structures provide a basis for understanding structure-function relations that underlie their distinct catalytic activities. Moreover, structural plasticity has been characterized for individual P450s that aids in understanding substrate binding in P450s ... Read more >>

J. Biol. Chem. (The Journal of biological chemistry)
[2013, 288(24):17082-17090]

Cited: 47 times

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Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195.

Yunsong Tong, Kent D Stewart, Alan S Florjancic, John E Harlan, Philip J Merta, Magdalena Przytulinska, Nirupama Soni, Kerren K Swinger, Haizhong Zhu, Eric F Johnson, Alexander R Shoemaker, Thomas D Penning,

To investigate the role played by the unique pre-DFG residue Val 195 of Cdc7 kinase on the potency of azaindole-chloropyridines (1), a series of novel analogues with various chloro replacements were synthesized and evaluated for their inhibitory activity against Cdc7. X-ray cocrystallization using a surrogate protein, GSK3β, and modeling studies ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2013, 4(2):211-215]

Cited: 7 times

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Structural characterization of human cytochrome P450 2C19: active site differences between P450s 2C8, 2C9, and 2C19.

R Leila Reynald, Stefaan Sansen, C David Stout, Eric F Johnson,

To identify the structural features underlying the distinct substrate and inhibitor profiles of P450 2C19 relative to the closely related human enzymes, P450s 2C8 and 2C9, the atomic structure (Protein Data Bank code 4GQS) of cytochrome P450 2C19 complexed with the inhibitor (2-methyl-1-benzofuran-3-yl)-(4-hydroxy-3,5-dimethylphenyl)methanone (Protein Data Bank chemical component 0XV) was ... Read more >>

J. Biol. Chem. (The Journal of biological chemistry)
[2012, 287(53):44581-44591]

Cited: 37 times

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Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families.

Keith B Glaser, Junling Li, Patrick A Marcotte, Terrance J Magoc, Jun Guo, David R Reuter, Paul Tapang, Ru-Qi Wei, Lori J Pease, Mai H Bui, Zehan Chen, Robin R Frey, Eric F Johnson, Donald J Osterling, Amanda M Olson, Jennifer J Bouska, Yanping Luo, Michael L Curtin, Cherrie K Donawho, Michael R Michaelides, Chris Tse, Steven K Davidsen, Daniel H Albert,

ABT-348 [1-(4-(4-amino-7-(1-(2-hydroxyethyl)-1H-pyrazol-4-yl)thieno[3,2-c]pyridin-3-yl)phenyl)-3-(3-fluorophenyl)urea] is a novel ATP-competitive multitargeted kinase inhibitor with nanomolar potency (IC(50)) for inhibiting binding and cellular autophosphorylation of Aurora B (7 and 13 nM), C (1 and 13 nM), and A (120 and 189 nM). Cellular activity against Aurora B is reflected by inhibition of phosphorylation of histone ... Read more >>

J. Pharmacol. Exp. Ther. (The Journal of pharmacology and experimental therapeutics)
[2012, 343(3):617-627]

Cited: 7 times

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Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

Qingwei Zhang, Zhiren Xia, Michael J Mitten, Loren M Lasko, Vered Klinghofer, Jennifer Bouska, Eric F Johnson, Thomas D Penning, Yan Luo, Vincent L Giranda, Alexander R Shoemaker, Kent D Stewart, Stevan W Djuric, Anil Vasudevan,

A high throughput screening (HTS) hit, 1 (Plk1 K(i)=2.2 μM) was optimized and evaluated for the enzymatic inhibition of Plk-1 kinase. Molecular modeling suggested the importance of adding a hydrophobic aromatic amine side chain in order to improve the potency by a classic kinase H-donor-acceptor binding mode. Extensive SAR studies ... Read more >>

Bioorg. Med. Chem. Lett. (Bioorganic & Medicinal Chemistry Letters)
[2012, 22(24):7615-7622]

Cited: 2 times

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Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.

Gui-Dong Zhu, Jianchun Gong, Viraj B Gandhi, Xuesong Liu, Yan Shi, Eric F Johnson, Cherrie K Donawho, Paul A Ellis, Jennifer J Bouska, Donald J Osterling, Amanda M Olson, Chang Park, Yan Luo, Alexander Shoemaker, Vincent L Giranda, Thomas D Penning,

PARP-1, the most abundant member of the PARP superfamily of nuclear enzymes, has emerged as a promising molecular target in the past decade particularly for the treatment of cancer. A number of PARP-1 inhibitors, including veliparab discovered at Abbott, have advanced into different stages of clinical trials. Herein we describe ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2012, 20(15):4635-4645]

Cited: 4 times

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Crystal structure of human cytochrome P450 2D6 with prinomastat bound.

An Wang, Uzen Savas, Mei-Hui Hsu, C David Stout, Eric F Johnson,

Human cytochrome P450 2D6 contributes to the metabolism of >15% of drugs used in clinical practice. This study determined the structure of P450 2D6 complexed with a substrate and potent inhibitor, prinomastat, to 2.85 Å resolution by x-ray crystallography. Prinomastat binding is well defined by electron density maps with its ... Read more >>

J. Biol. Chem. (The Journal of biological chemistry)
[2012, 287(14):10834-10843]

Cited: 39 times

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Aminopyrimidinone cdc7 kinase inhibitors.

Keith W Woods, Chunqiu Lai, Julie M Miyashiro, Yunsong Tong, Alan S Florjancic, Edward K Han, Niru Soni, Yan Shi, Loren Lasko, Joel D Leverson, Eric F Johnson, Alexander R Shoemaker, Thomas D Penning,

We have investigated the SAR of a series of pyrimidinone-containing Cdc7 kinase inhibitors. A wide range of amine substitutions give potent compounds with activities (K(i)) less than 1nM. Kinase selectivity is reasonable and cytotoxicity corresponds to inhibition of MCM2 phosphorylation. ... Read more >>

Bioorg. Med. Chem. Lett. (Bioorganic & Medicinal Chemistry Letters)
[2012, 22(5):1940-1943]

Cited: 6 times

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