Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(1R,3R,6aS,7R,8R,10bR,12aR)-1,6a,8,10a-tetramethyl-8-[(2R)-3-methylbutan-2-yl]-2-[[(2R)-1-methylpyrrolidin-2-yl]methoxy]-3-[5-(pyridin-4-yl)-1H-1,2,4-triazol-1-yl]-1,3,4,6,6a,7,8,9,10,10a,10b,11,12,12a-tetradecahydro-2H-1,4a-(methanooxymethano)chrysene-7-carboxylic acid
-
IC50: 19 ng/ml, pH and temperature not specified in the publication
(1R,3R,6aS,7R,8R,10bR,12aR)-1,6a,8,10a-tetramethyl-8-[(2R)-3-methylbutan-2-yl]-2-[[(2R)-2-methylpyrrolidin-2-yl]methoxy]-3-[5-(pyridin-4-yl)-1H-1,2,4-triazol-1-yl]-1,3,4,6,6a,7,8,9,10,10a,10b,11,12,12a-tetradecahydro-2H-1,4a-(methanooxymethano)chrysene-7-carboxylic acid
-
IC50: 4 ng/ml, pH and temperature not specified in the publication
(1R,3R,6aS,7R,8R,10bR,12aR)-1,6a,8,10a-tetramethyl-8-[(2R)-3-methylbutan-2-yl]-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]-3-[5-(pyridin-4-yl)-1H-1,2,4-triazol-1-yl]-1,3,4,6,6a,7,8,9,10,10a,10b,11,12,12a-tetradecahydro-2H-1,4a-(methanooxymethano)chrysene-7-carboxylic acid
-
IC50: 61 ng/ml, pH and temperature not specified in the publication
(1R,3R,6aS,7R,8R,10bR,12aR)-1,6a,8,10a-tetramethyl-8-[(2R)-3-methylbutan-2-yl]-3-[5-(pyridin-4-yl)-1H-1,2,4-triazol-1-yl]-2-[(2R)-pyrrolidin-2-ylmethoxy]-1,3,4,6,6a,7,8,9,10,10a,10b,11,12,12a-tetradecahydro-2H-1,4a-(methanooxymethano)chrysene-7-carboxylic acid
-
IC50: 22 ng/ml, pH and temperature not specified in the publication
(1R,3R,6aS,7R,8R,10bR,12aR)-1,6a,8,10a-tetramethyl-8-[(2R)-3-methylbutan-2-yl]-3-[5-(pyridin-4-yl)-1H-1,2,4-triazol-1-yl]-2-[(2S)-pyrrolidin-2-ylmethoxy]-1,3,4,6,6a,7,8,9,10,10a,10b,11,12,12a-tetradecahydro-2H-1,4a-(methanooxymethano)chrysene-7-carboxylic acid
-
IC50: 18 ng/ml, pH and temperature not specified in the publication
(1R,3R,6aS,7R,8R,10bR,12aR)-2-[[(2R)-1,2-dimethylpyrrolidin-2-yl]methoxy]-1,6a,8,10a-tetramethyl-8-[(2R)-3-methylbutan-2-yl]-3-[5-(pyridin-4-yl)-1H-1,2,4-triazol-1-yl]-1,3,4,6,6a,7,8,9,10,10a,10b,11,12,12a-tetradecahydro-2H-1,4a-(methanooxymethano)chrysene-7-carboxylic acid
-
IC50: 6.4 ng/ml, pH and temperature not specified in the publication
(1R,6aS,7R,8R,10bR,12aR)-1,6a,8,10a-tetramethyl-8-[(2R)-3-methylbutan-2-yl]-3-[5-(pyridin-4-yl)-1H-1,2,4-triazol-1-yl]-2-[[(2R)-2,3,3-trimethyl-2-(methylamino)butyl]oxy]-1,3,4,6,6a,7,8,9,10,10a,10b,11,12,12a-tetradecahydro-2H-1,4a-(methanooxymethano)chrysene-7-carboxylic acid
-
IC50: 2 ng/ml, pH and temperature not specified in the publication
(2,6-difluoro-phenyl)-carbamic acid 3-(4-benzothiazol-2-yl-piperazine-1-yl)-propyl ester
-
The piperazine propanol derivative GS1578 was identified as a potent inhibitor against 1,3-beta-D-glucan synthase, IC50: 0.16 microM.
1,2-Bis(O-aminophenoxy)ethane-N,N,N',N'-tetraacetate
-
-
Acylcarnitine
-
inhibition in presence of digitonin, stimulation in absence of digitonin within a certain concentration range
anidulafungin
-
an antifungal echinocandin drug, inhibition profile of wild-type and mutant enzymes
Congo red
-
non competitive
D-glucono-1,5-lactone
-
-
dihydrosphingosine
-
non-competitive inhibition
enfumafungin
-
IC50: 40 microgram/ml, pH 7.5, temperature not specified
Glycylglycine buffer
-
0.75 M
lysophosphatidylcholine
-
inhibition in presence of digitonin, stimulation in absence of digitonin within a certain concentration range
Mg2+
-
1,3-beta-glucan synthase 1
micafungin
-
an antifungal echinocandin drug, inhibition profile of wild-type and mutant enzymes
monomeric single-chain variable fragment (scFv)
-
Natural inhibitor in green Euglena cells
-
-
-
orizabin IX
-
IC50: 0.181 mg/ml
orizabin V
-
IC50: 0.155 mg/ml
orizabin X
-
IC50: 0.070 mg/ml
orizabin XI
-
IC50: 0.072 mg/ml
orizabin XIV
-
IC50: 0.074 mg/ml
orizabin XIX
-
IC50: 0.062 mg/ml
orizabin XV
-
IC50: 0.149 mg/ml
orizabin XVII
-
IC50: 0.078 mg/ml
orizabin XX
-
IC50: 0.065 mg/ml
p-chloromercuribenzoate
-
-
p-hydroxymercuribenzoate
-
-
papulacandin
-
IC50: 0.02 microgram/ml, pH 7.5, temperature not specified
Phospholipase A2
-
fatty acids and lysophospholipids are the inhibitory moieties
-
Phospholipase C
-
fatty acids and lysophospholipids are the inhibitory moieties
-
phytosphingosine
-
non-competitive inhibition
platelet-activating factor
-
inhibition in presence of digitonin, stimulation in absence of digitonin within a certain concentration range
pneumocandin
-
IC50: 120 microgram/ml, pH 7.5, temperature not specified
Sirofluor
-
fluorochrome from aniline blue
-
tricolorin A
-
IC50: 0.085 mg/ml
tricolorin B
-
IC50: 0.132 mg/ml
tricolorin C
-
IC50: 0.135 mg/ml
tricolorin D
-
IC50: 0.087 mg/ml
tricolorin E
-
IC50: 0.099 mg/ml
tricolorin F
-
IC50: more than 0.250 mg/ml
tricolorin I
-
IC50: 0.106 mg/ml
unsaturated fatty acids
-
trienoic acids most effective
-
ATP
-
-
ATP
-
both 1,3-beta-glucan synthases
Ca2+
-
at high concentration, stimulation at low concentration
Ca2+
-
1,3-beta-glucan synthase 1
caspofungin
-
-
caspofungin
-
50% inhibition at 0.00013 mg/ml
caspofungin
treatment with caspofungin at either the growth-inhibitory concentration (0.5 microg/ml) or paradoxical growth-inducing concentration (4 microg/ml) for 24 h causes similar abnormalities, including wider, hyperbranched hyphae, increased septation, and repeated hyphal tip lysis, followed by regenerative intrahyphal growth. At both concentrations, Fks1 initially mislocalizes from the hyphal tips to vacuoles. Only continuous exposure to 4 microg/ml of caspofungin for 48 h leads to recovery of the normal hyphal morphology with renewed localization of Fks1 to hyphal tips. Farnesol blocks paradoxical growth and relocalizes Fks1 and regulatory subunit Rho1 to vacuoles
caspofungin
-
very high caspofungin concentrations exert an additional antifungal activity besides inhibition of the beta-1,3-glucan synthase. Exposure to inhibitory caspofungin concentrations causes initial growth deprivation independently of the capability of the drug concentration to induce the paradoxical effect, i.e. the resumption of growth of otherwise susceptible strains at higher drug concentrations. Paradoxically growing hyphae emerge from microcolonies essentially devoid of beta-1,3-glucan. These hyphae expose beta-1,3-glucan again, suggesting that beta-1,3-glucan synthesis is restored. Expression of the beta-1,3-glucan synthase Fks1 is an essential requirement for the paradoxical effect. Overexpression of Fks1 renders Emericella nidulans more susceptible, whereas reduced expression leads to hyphae that are more resistant to the growth-inhibitory and limited fungicidal activity of caspofungin
caspofungin
-
exposure of strain RG101 to caspofungin during growth yields a modified enzyme that is drug insensitive (4 log orders) in kinetic inhibition assays, and this insensitivity is also observed for enzymes isolated from clinical isolates. The lipid microenvironment of the enzyme with resistance induced by caspofungin reveals a prominent increase in the abundances of dihydrosphingosine and phytosphingosine. Exogenous addition of dihydrosphingosine and phytosphingosine to the sensitive enzyme recapitulates the drug insensitivity of the caspofungin-derived enzyme. Caspofungin induces mitochondrion-derived reactive oxygen species, and dampening reactive oxygen species formation by antimycin A or thiourea eliminates drug-induced resistance
caspofungin
-
50% inhibition at 0.016 mg/ml
caspofungin
-
50% inhibition at 0.004 mg/ml
caspofungin
-
50% inhibition at 0.00013 mg/ml
caspofungin
-
IC50: 0.3 microgram/ml, pH 7.5, temperature not specified
caspofungin
-
an antifungal echinocandin drug, inhibition profile of wild-type and mutant enzymes
Caspofungin acetate
-
IC50: 30nM
cilofungin
-
maximal inhibition at 1.25 mM is 80%; non-competitive inhibition
cilofungin
-
non-competitive inhibition
cilofungin
-
50% inhibition at 0.064 mg/ml
Echinocandin B
-
-
Echinocandin B
-
inhibition in presence of digitonin, stimulation in absence of digitonin within a certain concentration range
EDTA
-
fully reversible by addition of Ca2+
EGTA
-
fully reversible by addition of Ca2+
ethanol
-
-
GTP
-
-
GTP
-
both 1,3-beta-glucan synthases
HM-1
-
HM-1 inhibits the growth of yeast cells by forming a pore at the growing tip of the daughter cell, resulting in the formation of a protruding structure and eventual cell death.
-
HM-1
-
HM-1 inhibits the growth of yeast cells by forming a pore at the growing tip of the daughter cell, resulting in the formation of a protruding structure and eventual cell death.
-
HM-1
-
HM-1 inhibits the growth of yeast cells by forming a pore at the growing tip of the daughter cell, resulting in the formation of a protruding structure and eventual cell death.
-
HM-1
-
HM-1 inhibits the growth of yeast cells by forming a pore at the growing tip of the daughter cell, resulting in the formation of a protruding structure and eventual cell death.
-
HM-1
-
HM-1 inhibits the growth of yeast cells by forming a pore at the growing tip of the daughter cell, resulting in the formation of a protruding structure and eventual cell death.
-
MK 991
-
-
Mn2+
-
at high concentration, stimulation at low concentration
Mn2+
-
1,3-beta-glucan synthase 1
monomeric single-chain variable fragment (scFv)
-
All four scFvs (scFv-A1, scFv-A2, scFv-A3, scFv-A4) inhibit beta-1,3-glucan-synthase. Most cultured cells treated with scFvs (3h) have a pearlike structure with protruding materials, characteristic of pore formation and similar to the morphology change after treatment with HM-1. These clearly indicate that the scFvs appear to have the same effect as HM-1 on sensitive yeast cells.
-
monomeric single-chain variable fragment (scFv)
-
All four scFvs (scFv-A1, scFv-A2, scFv-A3, scFv-A4) inhibit beta-1,3-glucan-synthase. Most cultured cells treated with scFvs (3h) have a pearlike structure with protruding materials, characteristic of pore formation and similar to the morphology change after treatment with HM-1. These clearly indicate that the scFvs appear to have the same effect as HM-1 on sensitive yeast cells.
-
monomeric single-chain variable fragment (scFv)
-
All four scFvs (scFv-A1, scFv-A2, scFv-A3, scFv-A4) inhibit beta-1,3-glucan-synthase. Most cultured cells treated with scFvs (3h) have a pearlike structure with protruding materials, characteristic of pore formation and similar to the morphology change after treatment with HM-1. These clearly indicate that the scFvs appear to have the same effect as HM-1 on sensitive yeast cells.
-
monomeric single-chain variable fragment (scFv)
-
All four scFvs (scFv-A1, scFv-A2, scFv-A3, scFv-A4) inhibit beta-1,3-glucan-synthase. Most cultured cells treated with scFvs (3h) have a pearlike structure with protruding materials, characteristic of pore formation and similar to the morphology change after treatment with HM-1. These clearly indicate that the scFvs appear to have the same effect as HM-1 on sensitive yeast cells.
-
monomeric single-chain variable fragment (scFv)
-
All four scFvs (scFv-A1, scFv-A2, scFv-A3, scFv-A4) inhibit beta-1,3-glucan-synthase. Most cultured cells treated with scFvs (3h) have a pearlike structure with protruding materials, characteristic of pore formation and similar to the morphology change after treatment with HM-1. These clearly indicate that the scFvs appear to have the same effect as HM-1 on sensitive yeast cells.
-
N-ethylmaleimide
-
0.16 mM, partial inhibition
N-ethylmaleimide
-
0.16 mM, partial inhibition
N-ethylmaleimide
-
0.16 mM, partial inhibition
N-ethylmaleimide
-
0.16 mM, partial inhibition
N-ethylmaleimide
-
0.16 mM, partial inhibition
N-ethylmaleimide
-
0.16 mM, partial inhibition
oryzalin
-
-
papulacandin B
-
-
papulacandin B
-
IC50: 0.1 mg/ml
Showdomycin
-
0.1 mM, partial inhibition
Showdomycin
-
0.1 mM, partial inhibition
Showdomycin
-
0.1 mM, partial inhibition
Showdomycin
-
0.1 mM, partial inhibition
Showdomycin
-
0.1 mM, partial inhibition
Showdomycin
-
0.1 mM, partial inhibition
Triton X-100
-
-
UDP
-
-
UMP
-
-
UTP
-
-
additional information
-
Preincubation with nMAb-KT eliminate the inhibition of Candida growth by scFv antibodies, suggestig that the observed cytocidal effect of scFv antibodies is due to their structural resemblance to HM-1.
-
additional information
-
enzyme activity is inhibited by ethanol extract of Salvia miltiorrhiza
-
additional information
-
Preincubation with nMAb-KT eliminate the inhibition of Candida growth by scFv antibodies, suggestig that the observed cytocidal effect of scFv antibodies is due to their structural resemblance to HM-1.
-
additional information
-
Preincubation with nMAb-KT eliminate the inhibition of Candida growth by scFv antibodies, suggestig that the observed cytocidal effect of scFv antibodies is due to their structural resemblance to HM-1.
-
additional information
-
not inhibited by caspofungin acetate (CFA)
-
additional information
-
the somatic isozyme is inactivated by trypsin, in contrast to the pollen isozyme
-
additional information
-
Preincubation with nMAb-KT eliminate the inhibition of Candida growth by scFv antibodies, suggestig that the observed cytocidal effect of scFv antibodies is due to their structural resemblance to HM-1.
-
additional information
-
Preincubation with nMAb-KT eliminate the inhibition of Candida growth by scFv antibodies, suggestig that the observed cytocidal effect of scFv antibodies is due to their structural resemblance to HM-1.
-