Page last updated: 2024-12-11

concanamycin a

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

concanamycin A: from Streptomyces diastatochromogenes S-45; inhibits vacuolar H+ ATPase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

concanamycin A : A concanamycin in which the lactone ring contains 4 double bonds and is substituted by 4 methyl groups, 2 hydroxy groups, 2 methoxy groups and an ethyl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID6438151
CHEMBL ID1241239
CHEBI ID73167
MeSH IDM0112190

Synonyms (19)

Synonym
x 4357 b
antibiotic x 4357 b
oxacyclooctadeca-3,5,13,15-tetraen-2-one, 18-((1s,2r,3s)-3-((2r,4r,5s,6r)-4-((4-o-(aminocarbonyl)-2,6-dideoxy-beta-d-arbino-hexopyranosyl)oxy)tetrahydro-2-hydroxy-5-methyl-6-(1e)-1-propenyl-2h-pyran-2-yl)-2-hydroxy-1-methylbutyl)-9-ethyl-8,10-dihydroxy-3,
concanamycin a
80890-47-7
folimycin
[(2r,3s,4r,6r)-6-[(2r,4r,5s,6r)-2-[(2s,3r,4s)-4-[(2r,3s,4e,6e,9r,10s,11s,12r,13r,14e,16z)-11-ethyl-10,12-dihydroxy-3,17-dimethoxy-7,9,13,15-tetramethyl-18-oxo-1-oxacyclooctadeca-4,6,14,16-tetraen-2-yl]-3-hydroxypentan-2-yl]-2-hydroxy-5-methyl-6-[(e)-prop-
CHEMBL1241239
chebi:73167 ,
tan 1323 b
tan-1323 b
(5r)-3-o-(4-o-carbamoyl-2,6-dideoxy-beta-d-arabino-hexopyranosyl)-2,4-dideoxy-1-c-{(2s,3r,4s)-4-[(2r,3s,4e,6e,9r,10s,11s,12r,13r,14e,16z)-11-ethyl-10,12-dihydroxy-3,17-dimethoxy-7,9,13,15-tetramethyl-18-oxooxacyclooctadeca-4,6,14,16-tetraen-2-yl]-3-hydrox
AKOS024457223
(3z,5e,7r,8r,9s,10s,11r,13e,15e,17s,18r)-18-[(1s,2r,3s)-3-[(2r,4r,5s,6r)-4-[[4-o-(aminocarbonyl)-2,6-dideoxy-?-d-arabino-hexopyranosyl]oxy]tetrahydro-2-hydroxy-5-methyl-6-(1e)-1-propenyl-2h-pyran-2-yl]-2-hydroxy-1-methylbutyl]-9-ethyl-8,10-dihydroxy-3,17-
DJZCTUVALDDONK-HQMSUKCRSA-N
Q27140357
DB14062
HY-N1724
CS-0017399

Research Excerpts

Actions

ExcerptReferenceRelevance
"Concanamycin A caused an increase of the cytosolic Ca2+-concentration whereas W-7 did not."( A link of Ca2+ to cAMP oscillations in Dictyostelium: the calmodulin antagonist W-7 potentiates cAMP relay and transiently inhibits the acidic Ca2+-store.
Lusche, DF; Malchow, D; Schlatterer, C, 2004
)
1.04

Treatment

ExcerptReferenceRelevance
"The treatment of concanamycin A (ConcA), a specific inhibitor of V-ATPases, leads to obvious aggregation of the endosomal compartments labelled with PutVHA-c-GFP."( Conserved V-ATPase c subunit plays a role in plant growth by influencing V-ATPase-dependent endosomal trafficking.
Bu, Y; Liu, S; Takano, T; Zhang, X; Zhou, A, 2016
)
0.76

Dosage Studied

ExcerptRelevanceReference
" Once confirmed by dose-response assays (EC(50)=26 microM), we verified V-ATPase inhibition by disulfiram in secondary assays that measured ATP hydrolysis in vacuolar membranes."( Identification of inhibitors of vacuolar proton-translocating ATPase pumps in yeast by high-throughput screening flow cytometry.
Allen, C; Johnson, RM; Melman, SD; Parra, KJ; Sklar, LA; Waller, A; Young, SM, 2010
)
0.36
" The optimized spiroindolone NITD609 shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model."( Spiroindolones, a potent compound class for the treatment of malaria.
Beck, HP; Brun, R; Cohen, SB; Dartois, V; Dharia, NV; Diagana, TT; Fidock, DA; Goh, A; González-Páez, GE; Jegla, T; Keller, TH; Lakshminarayana, SB; Lee, MC; McNamara, C; Nosten, F; Plouffe, DM; Renia, L; Rottmann, M; Russell, B; Schmitt, EK; Seitz, P; Spencer, KR; Suwanarusk, R; Tan, J; Winzeler, EA; Yeung, BK; Zou, B, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antifungal agentAn antimicrobial agent that destroys fungi by suppressing their ability to grow or reproduce.
metaboliteAny intermediate or product resulting from metabolism. The term 'metabolite' subsumes the classes commonly known as primary and secondary metabolites.
EC 3.6.3.14 (H(+)-transporting two-sector ATPase) inhibitorAn EC 3.6.3.* (acid anhydride hydrolase catalysing transmembrane movement of substances) inhibitor that interferes with the action of H(+)-transporting two-sector ATPase inhibitor (EC 3.6.3.14).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
concanamycinMacrolide antibiotics first isolated from Streptomyces species. They possess an 18-membered lactone ring and a 6-membered hemiketal ring in which the hydroxy group at position 23 is glycosylated by 2-deoxy-beta-D-rhamnose.
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID1700219Growth inhibition of Saccharomyces cerevisiae W303 at 0.5 uM after 2 to 3 days in ammonium iron(II) sulfate condition2020Journal of natural products, 11-25, Volume: 83, Issue:11
Callyspongiolide Is a Potent Inhibitor of the Vacuolar ATPase.
AID1700228Inhibition of V-ATpase in Saccharomyces cerevisiae BY4742 vacuolar membranes at 100 nM after 10 mins by spectrophotometric based coupled enzyme assay relative to control2020Journal of natural products, 11-25, Volume: 83, Issue:11
Callyspongiolide Is a Potent Inhibitor of the Vacuolar ATPase.
AID510929Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone3 bearing P-type ATPase4 D1247Y mutations after 72 hrs by SYBR green based fluorescence assay2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID1700215Growth inhibition of Saccharomyces cerevisiae W303 pdr5 deletion mutant at 0.5 uM after 2 to 3 days in glycerol condition relative to control2020Journal of natural products, 11-25, Volume: 83, Issue:11
Callyspongiolide Is a Potent Inhibitor of the Vacuolar ATPase.
AID510926Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green based fluorescence assay2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID1700230Inhibition of V-ATpase in Saccharomyces cerevisiae BY4742 vacuolar membranes after 10 mins by spectrophotometric based coupled enzyme assay2020Journal of natural products, 11-25, Volume: 83, Issue:11
Callyspongiolide Is a Potent Inhibitor of the Vacuolar ATPase.
AID510927Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone1 bearing P-type ATPase4 I398F and P990R mutations after 72 hrs by SYBR green based fluorescence assay2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID510928Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone2 bearing P-type ATPase4 T418N and P990R mutations after 72 hrs by SYBR green based fluorescence assay2010Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996
Spiroindolones, a potent compound class for the treatment of malaria.
AID1700225Inhibition of V-ATpase in Saccharomyces cerevisiae W303 pdr5 deletion mutant assessed as quinacrine accumulation in the cytosol at 0.5 uM after 4 hrs by fluorescence microscopic method2020Journal of natural products, 11-25, Volume: 83, Issue:11
Callyspongiolide Is a Potent Inhibitor of the Vacuolar ATPase.
AID1700214Growth inhibition of Saccharomyces cerevisiae W303 at 0.5 uM after 2 to 3 days in glycerol condition relative to control2020Journal of natural products, 11-25, Volume: 83, Issue:11
Callyspongiolide Is a Potent Inhibitor of the Vacuolar ATPase.
AID1700224Inhibition of V-ATpase in Saccharomyces cerevisiae W303 assessed as quinacrine accumulation in the cytosol at 0.5 uM after 4 hrs by fluorescence microscopic method2020Journal of natural products, 11-25, Volume: 83, Issue:11
Callyspongiolide Is a Potent Inhibitor of the Vacuolar ATPase.
AID1700211Antifungal activity against Saccharomyces cerevisiae W303 pdr5 deletion mutant assessed as reduction in microbial growth at 0.5 uM after 2 to 3 days2020Journal of natural products, 11-25, Volume: 83, Issue:11
Callyspongiolide Is a Potent Inhibitor of the Vacuolar ATPase.
AID1700218Growth inhibition of Saccharomyces cerevisiae W303 pdr5 deletion mutant at 0.5 uM after 2 to 3 days in ammonium iron(II) sulfate condition2020Journal of natural products, 11-25, Volume: 83, Issue:11
Callyspongiolide Is a Potent Inhibitor of the Vacuolar ATPase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (271)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (1.11)18.7374
1990's54 (19.93)18.2507
2000's133 (49.08)29.6817
2010's72 (26.57)24.3611
2020's9 (3.32)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.83

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index32.83 (24.57)
Research Supply Index5.62 (2.92)
Research Growth Index6.03 (4.65)
Search Engine Demand Index44.85 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (32.83)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (1.46%)6.00%
Case Studies1 (0.36%)4.05%
Observational0 (0.00%)0.25%
Other269 (98.18%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]