Výsledky vyhledávání - "Jennifer Piraino"

Crystallographic analysis reveals a novel second binding site for trimethoprim in active site double mutants of human dihydrofolate reductase

Autor: Jennifer Piraino, Jim Pace, Sherry F. Queener, Vivian Cody

Publikováno v: Journal of Structural Biology. 176:52-59

In order to produce a more potent replacement for trimethoprim (TMP) used as a therapy for Pneumocystis pneumonia and targets dihydrofolate reductase from Pneumocystis jirovecii (pjDHFR), it is necessary to understand the determinants of potency and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13fd253b1772af038bb770108e0d8078
https://doi.org/10.1016/j.jsb.2011.06.001

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Preferential selection of isomer binding from chiral mixtures: alternate binding modes observed for theEandZisomers of a series of 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines as ternary complexes with NADPH and human dihydrofolate reductase

Autor: Jennifer Piraino, Jim Pace, Aleem Gangjee, Vivian Cody, Wei Li

Publikováno v: Acta Crystallographica Section D Biological Crystallography. 66:1271-1277

The crystal structures of six human dihydrofolate reductase (hDHFR) ternary complexes with NADPH and a series of mixed E/Z isomers of 5-substituted 5-[2-(2-methoxyphenyl)-prop-1-en-1-yl]furo[2,3-d]pyrimidine-2,4-diamines substituted at the C9 positio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d4312969b05002a7100307a08b580f6
https://doi.org/10.1107/s0907444910035808

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Design, Synthesis, and X-ray Crystal Structure of Classical and Nonclassical 2-Amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as Dual Thymidylate Synthase and Dihydrofolate Reductase Inhibitors and as Potential Antitumor Agents

Autor: Aleem Gangjee, Vivian Cody, Jim Pace, J. Makin, Roy L. Kisliuk, Wei Li, Jennifer Piraino

Publikováno v: Journal of Medicinal Chemistry. 52:4892-4902

N-{4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl}-L-glutamic acid 2 and thirteen nonclassical analogues 2a–2m were synthesized as potential dual thymidylate synthase (TS) and dihydrofolate reductase (DHFR) inhibitors

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::849b459819eeae05ad8f676627780c9e
https://doi.org/10.1021/jm900490a

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Design, synthesis, biological evaluation and X-ray crystal structure of novel classical 6,5,6-tricyclic benzo[4,5]thieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors

Autor: Roy L. Kisliuk, Xin Zhang, Vivian Cody, Xilin Zhou, Aleem Gangjee, Jennifer Piraino

Classical antifolates (4–7) with a tricyclic benzo[4,5]thieno[2,3-d]pyrimidine scaffold and a flexible and rigid benzoylglutamate were synthesized as dual thymidylate synthase (TS) and dihydrofolate reductase (DHFR) inhibitors. Oxidative aromatizat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::966f1e83bd342ae4fe964993a58dc985
https://europepmc.org/articles/PMC3138190/

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Correlations of inhibitor kinetics for Pneumocystis jirovecii and human dihydrofolate reductase with structural data for human active site mutant enzyme complexes

Autor: Vivian Cody, Andre Rosowsky, Jennifer Piraino, Sherry F. Queener, J. Pace, J. Makin

Publikováno v: Biochemistry. 48(8)

To understand the role of specific active site residues in conferring selective dihydrofolate reductase (DHFR) inhibition from pathogenic organisms such as Pneumocystis carinii (pc) or Pneumocystis jirovecii (pj), the causative agent in AIDS pneumoni

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ac839e421e888f26d34c36a276a6778
https://pubmed.ncbi.nlm.nih.gov/19196009

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