reblastatin profile

reblastatin: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	9807556
CHEMBL ID	267792
SCHEMBL ID	13009052
MeSH ID	M0370911

Synonym
reblastatin
CHEMBL267792
SCHEMBL13009052
bdbm50542414

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Heat shock protein HSP 90-alpha	Homo sapiens (human)	IC50 (µMol)	0.0050	0.0004	0.6950	10.0000	AID1659865
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
telomere maintenance via telomerase	Heat shock protein HSP 90-alpha	Homo sapiens (human)
neuron migration	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of protein phosphorylation	Heat shock protein HSP 90-alpha	Homo sapiens (human)
activation of innate immune response	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of defense response to virus by host	Heat shock protein HSP 90-alpha	Homo sapiens (human)
skeletal muscle contraction	Heat shock protein HSP 90-alpha	Homo sapiens (human)
mitochondrial transport	Heat shock protein HSP 90-alpha	Homo sapiens (human)
response to unfolded protein	Heat shock protein HSP 90-alpha	Homo sapiens (human)
response to heat	Heat shock protein HSP 90-alpha	Homo sapiens (human)
response to cold	Heat shock protein HSP 90-alpha	Homo sapiens (human)
response to xenobiotic stimulus	Heat shock protein HSP 90-alpha	Homo sapiens (human)
response to salt stress	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of lamellipodium assembly	Heat shock protein HSP 90-alpha	Homo sapiens (human)
cardiac muscle cell apoptotic process	Heat shock protein HSP 90-alpha	Homo sapiens (human)
regulation of protein ubiquitination	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of protein polymerization	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of interferon-beta production	Heat shock protein HSP 90-alpha	Homo sapiens (human)
regulation of protein localization	Heat shock protein HSP 90-alpha	Homo sapiens (human)
protein refolding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
response to cocaine	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of protein import into nucleus	Heat shock protein HSP 90-alpha	Homo sapiens (human)
regulation of apoptotic process	Heat shock protein HSP 90-alpha	Homo sapiens (human)
regulation of protein-containing complex assembly	Heat shock protein HSP 90-alpha	Homo sapiens (human)
protein unfolding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
response to estrogen	Heat shock protein HSP 90-alpha	Homo sapiens (human)
protein insertion into mitochondrial outer membrane	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of nitric oxide biosynthetic process	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of protein catabolic process	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of cell size	Heat shock protein HSP 90-alpha	Homo sapiens (human)
response to antibiotic	Heat shock protein HSP 90-alpha	Homo sapiens (human)
protein stabilization	Heat shock protein HSP 90-alpha	Homo sapiens (human)
chaperone-mediated protein complex assembly	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of cardiac muscle contraction	Heat shock protein HSP 90-alpha	Homo sapiens (human)
chaperone-mediated autophagy	Heat shock protein HSP 90-alpha	Homo sapiens (human)
cellular response to virus	Heat shock protein HSP 90-alpha	Homo sapiens (human)
regulation of postsynaptic membrane neurotransmitter receptor levels	Heat shock protein HSP 90-alpha	Homo sapiens (human)
positive regulation of tau-protein kinase activity	Heat shock protein HSP 90-alpha	Homo sapiens (human)
telomerase holoenzyme complex assembly	Heat shock protein HSP 90-alpha	Homo sapiens (human)
cellular response to heat	Heat shock protein HSP 90-alpha	Homo sapiens (human)
protein folding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
UTP binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
CTP binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
RNA binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
mRNA binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
protein binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
ATP binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
GTP binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
ATP hydrolysis activity	Heat shock protein HSP 90-alpha	Homo sapiens (human)
sulfonylurea receptor binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
protein phosphatase binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
MHC class II protein complex binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
nitric-oxide synthase regulator activity	Heat shock protein HSP 90-alpha	Homo sapiens (human)
TPR domain binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
ubiquitin protein ligase binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
dATP binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
identical protein binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
protein homodimerization activity	Heat shock protein HSP 90-alpha	Homo sapiens (human)
histone deacetylase binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
transmembrane transporter binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
tau protein binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
GTPase binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
Rho GDP-dissociation inhibitor binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
DNA polymerase binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
scaffold protein binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
disordered domain specific binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
ATP-dependent protein folding chaperone	Heat shock protein HSP 90-alpha	Homo sapiens (human)
protein tyrosine kinase binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
unfolded protein binding	Heat shock protein HSP 90-alpha	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular region	Heat shock protein HSP 90-alpha	Homo sapiens (human)
nucleus	Heat shock protein HSP 90-alpha	Homo sapiens (human)
nucleoplasm	Heat shock protein HSP 90-alpha	Homo sapiens (human)
cytoplasm	Heat shock protein HSP 90-alpha	Homo sapiens (human)
mitochondrion	Heat shock protein HSP 90-alpha	Homo sapiens (human)
cytosol	Heat shock protein HSP 90-alpha	Homo sapiens (human)
plasma membrane	Heat shock protein HSP 90-alpha	Homo sapiens (human)
cell surface	Heat shock protein HSP 90-alpha	Homo sapiens (human)
membrane	Heat shock protein HSP 90-alpha	Homo sapiens (human)
basolateral plasma membrane	Heat shock protein HSP 90-alpha	Homo sapiens (human)
apical plasma membrane	Heat shock protein HSP 90-alpha	Homo sapiens (human)
brush border membrane	Heat shock protein HSP 90-alpha	Homo sapiens (human)
secretory granule lumen	Heat shock protein HSP 90-alpha	Homo sapiens (human)
melanosome	Heat shock protein HSP 90-alpha	Homo sapiens (human)
neuronal cell body	Heat shock protein HSP 90-alpha	Homo sapiens (human)
lysosomal lumen	Heat shock protein HSP 90-alpha	Homo sapiens (human)
dendritic growth cone	Heat shock protein HSP 90-alpha	Homo sapiens (human)
axonal growth cone	Heat shock protein HSP 90-alpha	Homo sapiens (human)
perinuclear region of cytoplasm	Heat shock protein HSP 90-alpha	Homo sapiens (human)
collagen-containing extracellular matrix	Heat shock protein HSP 90-alpha	Homo sapiens (human)
extracellular exosome	Heat shock protein HSP 90-alpha	Homo sapiens (human)
endocytic vesicle lumen	Heat shock protein HSP 90-alpha	Homo sapiens (human)
sperm mitochondrial sheath	Heat shock protein HSP 90-alpha	Homo sapiens (human)
sperm plasma membrane	Heat shock protein HSP 90-alpha	Homo sapiens (human)
ficolin-1-rich granule lumen	Heat shock protein HSP 90-alpha	Homo sapiens (human)
protein-containing complex	Heat shock protein HSP 90-alpha	Homo sapiens (human)
plasma membrane	Heat shock protein HSP 90-alpha	Homo sapiens (human)
neuronal cell body	Heat shock protein HSP 90-alpha	Homo sapiens (human)
perinuclear region of cytoplasm	Heat shock protein HSP 90-alpha	Homo sapiens (human)
myelin sheath	Heat shock protein HSP 90-alpha	Homo sapiens (human)
cytosol	Heat shock protein HSP 90-alpha	Homo sapiens (human)
nucleus	Heat shock protein HSP 90-alpha	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay ID	Title	Year	Journal	Article
AID1740803	Selectivity index, ratio of IC50 for cytotoxicity against human HDF cells to IC50 for cytotoxicity against human SK-OV-3 cells	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges.
AID1659863	Antibacterial activity against Staphylococcus aureus	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID314503	Growth inhibition of human HCT116 cells	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.
AID1659865	Inhibition of HSP90alpha (unknown origin)	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID314501	Inhibition of Hsp90 in human KPL4 cells assessed as depletion of Raf-1 level after 40 hrs	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.
AID1659857	Antibiofilm activity against Shewanella oneidensis MR-1	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID1659858	Antibiofilm activity against Bacillus amyloliquefaciens	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID314499	Binding affinity at purified Hsp90 by DELFIA assay	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.
AID314505	Growth inhibition of human A549 cells	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.
AID314502	Induction of human K562 cells differentiation	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.
AID1740802	Selectivity index, ratio of IC50 for cytotoxicity against human HDF cells to IC50 for cytotoxicity against human SK-BR-3 cells	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges.
AID1659868	Cytotoxicity against human HL60 cells assessed as reduction in cell viability	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID1659861	Antibacterial activity against Bacillus amyloliquefaciens	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID1659860	Antibacterial activity against Shewanella oneidensis MR-1	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID314506	Growth inhibition of human KPL4 cells	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.
AID1659859	Antibiofilm activity against Staphylococcus aureus	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID1740796	Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges.
AID1740798	Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges.
AID1740797	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges.
AID314504	Growth inhibition of human DLD1 cells	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.
AID314500	Inhibition of Hsp90 in human KPL4 cells assessed as depletion of ErbB2 level after 40 hrs	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.
AID1659867	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID1659866	Cytotoxicity against human A549 cells assessed as reduction in cell viability	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID1659869	Cytotoxicity against human K562 cells assessed as reduction in cell viability	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.
AID1740804	Selectivity index, ratio of IC50 for cytotoxicity against human HDF cells to IC50 for cytotoxicity against human PC-3 cells	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	4 (36.36)	29.6817
2010's	5 (45.45)	24.3611
2020's	2 (18.18)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	11 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
quinone benzoquinone : The simplest members of the class of benzoquinones, consisting of cyclohexadiene which is substituted by two oxo groups.. 1,4-benzoquinone : The simplest member of the class of 1,4-benzoquinones, obtained by the formal oxidation of hydroquinone to the corresponding diketone. It is a metabolite of benzene.. quinone : Compounds having a fully conjugated cyclic dione structure, such as that of benzoquinones, derived from aromatic compounds by conversion of an even number of -CH= groups into -C(=O)- groups with any necessary rearrangement of double bonds (polycyclic and heterocyclic analogues are included).	7.05	1	1,4-benzoquinones	cofactor; human xenobiotic metabolite; mouse metabolite
cytarabine [no description available]	2.25	1	beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside	antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	2.25	1	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
geldanamycin [no description available]	2.82	3	1,4-benzoquinones; ansamycin; carbamate ester; organic heterobicyclic compound	antimicrobial agent; antineoplastic agent; antiviral agent; cysteine protease inhibitor; Hsp90 inhibitor
geldanamycin [no description available]	2.74	3
monorden monorden: inhibits HSP90 Heat-Shock Proteins, DNA topoisomerase VI and human Topoisomerase II	2.04	1	cyclic ketone; enone; epoxide; macrolide antibiotic; monochlorobenzenes; phenols	antifungal agent; metabolite; tyrosine kinase inhibitor
elaiophylin [no description available]	7.15	1	lactol; macrodiolide; monosaccharide derivative	antifungal agent; autophagy inhibitor; bacterial metabolite
tanespimycin CP 127374: analog of herbimycin A	2.5	2	1,4-benzoquinones; ansamycin; carbamate ester; organic heterobicyclic compound; secondary amino compound	antineoplastic agent; apoptosis inducer; Hsp90 inhibitor

Condition	Relationship Strength	Studies
Breast Cancer [description not available]	2.13	1
Breast Neoplasms Tumors or cancer of the human BREAST.	2.13	1
Cancer of Lung [description not available]	2	1
Lung Neoplasms Tumors or cancer of the LUNG.	2	1

reblastatin

Description

Cross-References

Synonyms (4)

Protein Targets (1)

Inhibition Measurements

Biological Processes (40)

Molecular Functions (28)

Ceullar Components (27)

Bioassays (25)

Research

Studies (11)

Market Indicators

Research Demand Index: 12.32

Study Types

reblastatin

Description

Cross-References

Synonyms (4)

Protein Targets (1)

Inhibition Measurements

Biological Processes (40)

Molecular Functions (28)

Ceullar Components (27)

Bioassays (25)

Research

Studies (11)

Market Indicators

Research Demand Index: 12.32

Study Types

Related Drugs (8)

Related Conditions (4)