Selective Inhibitors of Candida albicans Dihydrofolate Reductase: Activity and Selectivity of 5-(Arylthio)-2,4-diaminoquinazolines

1995 ◽  
Vol 38 (18) ◽  
pp. 3608-3616 ◽  
Author(s):  
Joseph H. Chan ◽  
Jean S. Hong ◽  
Lee F. Kuyper ◽  
David P. Baccanari ◽  
Suzanne S. Joyner ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Dihydrofolate Reductase ◽  
Reductase Activity ◽  
Selective Inhibitors

ChemInform Abstract: Selective Inhibitors of Candida albicans Dihydrofolate Reductase: Activity and Selectivity of 5-(Arylthio)-2,4-diaminoquinazolines.

ChemInform ◽  
2010 ◽  
Vol 26 (52) ◽  
pp. no-no
Author(s):  
J. H. CHAN ◽  
J. S. HONG ◽  
L. F. KUYPER ◽  
D. P. BACCANARI ◽  
S. S. JOYNER ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Dihydrofolate Reductase ◽  
Reductase Activity ◽  
Selective Inhibitors

scholarly journals Characterization of Candida albicans Dihydrofolate Reductase

1989 ◽  
Vol 264 (2) ◽  
pp. 1100-1107
Author(s):  
D P Baccanari ◽  
R L Tansik ◽  
S S Joyner ◽  
M E Fling ◽  
P L Smith ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Dihydrofolate Reductase

scholarly journals Short-chain aurachin D derivatives are selective inhibitors of E. coli cytochrome bd-I and bd-II oxidases

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Melanie Radloff ◽  
Isam Elamri ◽  
Tamara N. Grund ◽  
Luca F. Witte ◽  
Katharina F. Hohmann ◽  
...  
Keyword(s):  
Pathogenic Bacteria ◽  
Reductase Activity ◽  
Mitochondrial Respiratory Chain ◽  
Short Chain ◽  
Inhibitory Effects ◽  
Selective Inhibitors ◽  
E Coli ◽  
Terminal Oxidases ◽  
Cytochrome Bd ◽  
Oxygen Reductase

AbstractCytochrome bd-type oxidases play a crucial role for survival of pathogenic bacteria during infection and proliferation. This role and the fact that there are no homologues in the mitochondrial respiratory chain qualify cytochrome bd as a potential antimicrobial target. However, few bd oxidase selective inhibitors have been described so far. In this report, inhibitory effects of Aurachin C (AurC-type) and new Aurachin D (AurD-type) derivatives on oxygen reductase activity of isolated terminal bd-I, bd-II and bo3 oxidases from Escherichia coli were potentiometrically measured using a Clark-type electrode. We synthesized long- (C10, decyl or longer) and short-chain (C4, butyl to C8, octyl) AurD-type compounds and tested this set of molecules towards their selectivity and potency. We confirmed strong inhibition of all three terminal oxidases for AurC-type compounds, whereas the 4(1H)-quinolone scaffold of AurD-type compounds mainly inhibits bd-type oxidases. We assessed a direct effect of chain length on inhibition activity with highest potency and selectivity observed for heptyl AurD-type derivatives. While Aurachin C and Aurachin D are widely considered as selective inhibitors for terminal oxidases, their structure–activity relationship is incompletely understood. This work fills this gap and illustrates how structural differences of Aurachin derivatives determine inhibitory potency and selectivity for bd-type oxidases of E. coli.

Direct demonstration of genetic alterations at the dihydrofolate reductase locus after gamma irradiation

1982 ◽  
Vol 2 (1) ◽  
pp. 93-96
Author(s):  
L H Graf ◽  
L A Chasin
Keyword(s):  
Dihydrofolate Reductase ◽  
Gamma Ray ◽  
Reductase Activity ◽  
Chinese Hamster Ovary Cells ◽  
Cdna Probe ◽  
Chinese Hamster ◽  
Genetic Alterations ◽  
Ovary Cells ◽  
Direct Demonstration ◽  
Dna Deletions

Gamma ray-induced mutants of Chinese hamster ovary cells lacking dihydrofolate reductase activity were screened for DNA sequence changes at the locus specifying this activity by using a cloned cDNA probe. Two of nine mutants screened displayed an altered restriction fragment pattern suggesting the occurrence of DNA deletions or rearrangements.

Light‐Wavelength‐Based Quantitative Control of Dihydrofolate Reductase Activity by Using a Photochromic Isostere of an Inhibitor

ChemBioChem ◽  
2019 ◽  
Vol 20 (11) ◽  
pp. 1382-1386
Author(s):  
Takato Mashita ◽  
Toshiyuki Kowada ◽  
Hiroto Takahashi ◽  
Toshitaka Matsui ◽  
Shin Mizukami
Keyword(s):  
Dihydrofolate Reductase ◽  
Reductase Activity ◽  
Light Wavelength

Synthesis of potent and selective inhibitors of Candida albicans N-myristoyltransferase based on the benzothiazole structure

2005 ◽  
Vol 13 (7) ◽  
pp. 2509-2522 ◽  
Author(s):  
Kazuo Yamazaki ◽  
Yasushi Kaneko ◽  
Kie Suwa ◽  
Shinji Ebara ◽  
Kyoko Nakazawa ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Selective Inhibitors
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