Aclarubicin: An anthracycline produced by Streptomyces galilaeus. It has potent antineoplastic activity.Topoisomerase II Inhibitors: Compounds that inhibit the activity of DNA TOPOISOMERASE II. Included in this category are a variety of ANTINEOPLASTIC AGENTS which target the eukaryotic form of topoisomerase II and ANTIBACTERIAL AGENTS which target the prokaryotic form of topoisomerase II.Amsacrine: An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.Drug Antagonism: Phenomena and pharmaceutics of compounds that inhibit the function of agonists (DRUG AGONISM) and inverse agonists (DRUG INVERSE AGONISM) for a specific receptor. On their own, antagonists produce no effect by themselves to a receptor, and are said to have neither intrinsic activity nor efficacy.Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.Antibiotics, Antineoplastic: Chemical substances, produced by microorganisms, inhibiting or preventing the proliferation of neoplasms.DNA Topoisomerases, Type II: DNA TOPOISOMERASES that catalyze ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. These enzymes bring about relaxation of the supercoiled DNA and resolution of a knotted circular DNA duplex.Carcinoma, Small Cell: An anaplastic, highly malignant, and usually bronchogenic carcinoma composed of small ovoid cells with scanty neoplasm. It is characterized by a dominant, deeply basophilic nucleus, and absent or indistinct nucleoli. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1286-7)Carcinoma, Ehrlich Tumor: A transplantable, poorly differentiated malignant tumor which appeared originally as a spontaneous breast carcinoma in a mouse. It grows in both solid and ascitic forms.
(1/93) Evidence of the role of protein kinase C during aclacinomycin induction of erythroid differentiation in K562 cells.

At subtoxic concentrations, aclacinomycin is effective in controlling erythroid differentiation of K562, a human erythroleukemic cell line. To better understand early events implicated in this process, we have used bisindolylmaleimide (GF109203X), an inhibitor with a high selectivity for protein kinase C (PKC). Our data show that GF109203X inhibits aclacinomycin effects on K562, evidenced by a strong reduction of hemoglobinized cells and a marked decrease of mRNA rates of erythroid genes. To establish firmly PKC involvement, we also verified that aclacinomycin stimulates its rapid translocation, from the cytosolic to the membrane compartment. By Western blot analysis, we also show that after short induction times, PKCalpha was the most implicated.  (+info)

(2/93) Modifications of aclacinomycin T by aclacinomycin methyl esterase (RdmC) and aclacinomycin-10-hydroxylase (RdmB) from Streptomyces purpurascens.

The genes rdmB and rdmC of Streptomyces purpurascens encoding aclacinomycin modifying enzymes RdmB and RdmC were expressed in Streptomyces lividans TK24. In contrast to the earlier suggestion that RdmC may be an esterase that causes the removal of the carbomethoxy group from the 10 position of aclacinomycins, RdmC functions as an aclacinomycin methyl esterase and catalyzes the removal of the methoxy group from the C-15 position of aclacinomycin T producing 15-demethoxyaclacinomycin T. RdmB acts upon C-10 of 15-demethoxyaclacinomycin T and is able to remove the carboxylic group from the C-10 position. It functions also as an aclacinomycin-10-hydroxylase being able to add a hydroxyl group at the same, C-10 position in vitro. Aclacinomycin methyl esterase was purified to apparent homogeneity from S. lividans carrying the rdmC and aclacinomycin-10-hydroxylase as a glutathione S-transferase fusion construct from Escherichia coli carrying the rdmB gene, respectively. Aclacinomycin methyl esterase functions as a monomer and aclacinomycin-10-hydroxylase as a tetramer. Aclacinomycin methyl esterase has an exceptionally high temperature stability and has an apparent K(m) for aclacinomycin T of 15.5 microM. The introduction of rdmC and rdmB in a Streptomyces galilaeus mutant HO38 produced the same modifications of aclacinomycin T in vivo as aclacinomycin methyl esterase and aclacinomycin-10-hydroxylase in vitro.  (+info)

(3/93) Molecular cloning and disruption of a novel gene encoding UDP-glucose: tetrahydrobiopterin alpha-glucosyltransferase in the cyanobacterium Synechococcus sp. PCC 7942.

The gene encoding UDP-glucose:tetrahydrobiopterin alpha-glucosyltransferase (BGluT) was cloned from the genomic DNA of Synechococcus sp. PCC 7942. The encoded protein consisting of 359 amino acid residues was verified in vitro and in vivo to be responsible for the synthesis of tetrahydrobiopterin (BH4)-glucoside produced in the organism. The BGluT gene is the first cloned in pteridine glycosyltransferases and also a novel one cloned so far in UDP-glycosyltransferases. The mutant cells disrupted in the BGluT gene produced only aglycosidic BH4 at a level of 8.3% of the BH4-glucoside in wild type cells and exhibited half of the wild type growth in normal photoautotrophic conditions. These results suggest that the glucosylation of BH4 is required for the maintenance of the high cellular concentration of the compound, thereby supporting the normal growth of Synechococcus sp. PCC 7942.  (+info)

(4/93) Keratin attenuates tumor necrosis factor-induced cytotoxicity through association with TRADD.

Keratin 8 and 18 (K8/18) are the major components of intermediate filament (IF) proteins of simple or single-layered epithelia. Recent data show that normal and malignant epithelial cells deficient in K8/18 are nearly 100 times more sensitive to tumor necrosis factor (TNF)-induced cell death. We have now identified human TNF receptor type 1 (TNFR1)-associated death domain protein (TRADD) to be the K18-interacting protein. Among IF proteins tested in two-hybrid systems, TRADD specifically bound K18 and K14, type I (acidic) keratins. The COOH-terminal region of TRADD interacted with the coil Ia of the rod domain of K18. Endogenous TRADD coimmunoprecipitated with K18, and colocalized with K8/18 filaments in human mammary epithelial cells. Overexpression of the NH2 terminus (amino acids 1-270) of K18 containing the TRADD-binding domain as well as overexpression of K8/18 in SW13 cells, which are devoid of keratins, rendered the cells more resistant to killing by TNF. We also showed that overexpressed NH2 termini of K18 and K8/18 were associated with endogenous TRADD in SW13 cells, resulting in the inhibition of caspase-8 activation. These results indicate that K18 may sequester TRADD to attenuate interactions between TRADD and activated TNFR1 and moderate TNF-induced apoptosis in simple epithelial cells.  (+info)

(5/93) Aclarubicin treatment restores SMN levels to cells derived from type I spinal muscular atrophy patients.

Proximal spinal muscular atrophy (SMA) is a common motor neuron disorder caused by mutation of the telomeric survival of motor neuron gene SMN1. The centromeric survival of motor neuron SMN2 gene is retained in all SMA patients but does not produce sufficient SMN protein to prevent the development of clinical symptoms. The SMN1 and SMN2 genes differ functionally by a single nucleotide change. This change affects the efficiency with which exon 7 is incorporated into the mRNA transcript. Thus, SMN2 produces less full-length mRNA and protein than SMN1. We have screened a library of compounds in order to identify ones that can alter the splicing pattern of the SMN2 gene. Here, we report that the compound aclarubicin increases the retention of exon 7 into the SMN2 transcript. We show that aclarubicin effectively induces incorporation of exon 7 into SMN2 transcripts from the endogenous gene in type I SMA fibroblasts as well as into transcripts from a SMN2 minigene in the motor neuron cell line NSC34. In type I fibroblasts, treatment resulted in an increase in SMN protein and gems to normal levels. Our results suggest that alteration of splicing pattern represents a new approach to modification of gene expression in disease treatment and demonstrate the feasibility of high throughput screens to detect compounds that affect the splicing pattern of a gene.  (+info)

(6/93) Superior outcome of infant acute myeloid leukemia with intensive chemotherapy: results of the Japan Infant Leukemia Study Group.

This study analyzed data on 35 infants with acute myeloid leukemia (AML) who were treated with intensive chemotherapy between 1995 and 1998 in Japan. The incidence of boys, younger age (< 6 months old), and hyperleukocytosis at onset was high in patients with the M4/M5 subtype (n = 23) in the French-American-British classification, compared with the non-M4/M5 subtype (n = 12). Thirteen (56%) and 16 (70%) patients with the M4/M5 subtype also showed 11q23 translocations and MLL gene rearrangements, respectively, whereas only one patient with the non-M4/M5 subtype had this rearrangement. All 35 patients were treated with the ANLL91 protocol consisting of etoposide, high-dose cytarabine, and anthracyclines. Overall survival and the event-free survival (EFS) rates at 3 years of all patients were 76% (95% confidence interval [CI], 61.3%-90.7%) and 72% (95% CI, 56.4%-87.9%), respectively. EFS showed no significant difference between 2 subgroups divided by age, gender, presence of the MLL gene rearrangements, and white blood cell count at onset; EFS in patients with the M4/M5 subtype tended to be better than those with the non-M4/M5 subtype. Although all 6 patients who underwent allogeneic stem cell transplantation (SCT) have been in complete remission, no benefit of SCT was confirmed. These findings suggest that the intensive chemotherapy with the ANLL91 protocol might have been responsible for the observed good outcome of infant AML, even without SCT. The presence of the MLL gene rearrangements or the age at onset had no impact on the outcome of infant AML.  (+info)

(7/93) Induction of p16INK4a transcription and of cellular senescence by aclacinomycin-derivatives and cardiac glycosides.

Stable transformants of Saos-2 cells that contain the luciferase reporter gene under the control of the human p16INK4a transcriptional regulatory region were established, and were used to identify growth-inhibiting substances from culture broths of actinomycetes and extracts of plants. Among the active substances so far identified were an aclacinomycin-derivative, cenerubin B, and a cardiac glycoside, periplocin. These substances inhibited growth of normal human fibroblasts, and induced senescent phenotypes including a flattened morphology and increased acidic beta-galactosidase activity, although the activities of their derivatives to induce p16CDKN2 and beta-galactosidase did not coincided with each other. These results suggest that the reporter system using the p16CDKN2 transcriptional regulatory region is a useful means for screening growth inhibiting substances that are potential anti-tumor agents.  (+info)

(8/93) Characterization of mutations in aclacinomycin A-non-producing Streptomyces galilaeus strains with altered glycosylation patterns.

In this study a set of Streptomyces galilaeus ATCC 31615 mutants was characterized, which are incapable of synthesizing some or all of the deoxyhexose sugars of aclacinomycin A. Complementation experiments with the the mutant strains H026, H038, H039, H054, H063, H065 and H075 were carried out with glycosylation genes previously derived from the wild-type S. galilaeus. Mutations in strains H038, H063 and H075 were complemented with single PCR-amplified genes. Furthermore, amplification and sequencing of the corresponding genes from the mutant strains revealed single point mutations in the sequences. First, in H038 a transition mutation in aknQ, encoding a putative dTDP-hexose 3-ketoreductase, causes an amino acid substitution from glycine to aspartate, suppressing the biosynthesis of both 2-deoxyfucose and rhodinose and thus leading to the accumulation of aclacinomycin T with rhodosamine as its only sugar. Second, in H063, which accumulates aklavinone without a sugar moiety, amino acid substitution occurs, with threonine being substituted by isoleucine in dTDP-glucose synthase, the first enzyme participating in deoxyhexose biosynthesis, encoded by aknY. Third, a nonsense mutation in aknP leads to truncated dTDP-hexose 3-dehydratase in H075, which is incapable of synthesizing rhodinose. In addition, mutants H054 and H065, which accumulate aclacinomycins without aminosugars, were complemented by a gene for an aminotransferase, aknZ. Characterization of the nature of the mutations adds to the usefulness and value of the mutants in the analysis of gene function and in the creation of novel compounds by combinatorial biosynthesis. Furthermore, these results strengthen the assignments of akn gene products and enlighten the biosynthetic pathway for deoxyhexoses.  (+info)

*  Aclarubicin
... (INN) or aclacinomycin A is an anthracycline drug that is used in the treatment of cancer. Soil bacteria ... October 1991). "Antagonistic effect of aclarubicin on daunorubicin-induced cytotoxicity in human small cell lung cancer cells: ... Streptomyces galilaeus can produce aclarubicin. It can induce histone eviction from chromatin upon intercalation. CID 451415 ...
*  Drug discovery
Anthracyclines (Aclarubicin · Daunorubicin · Doxorubicin · Epirubicin · Idarubicin · Amrubicin · Pirarubicin · Valrubicin · ...
*  Streptomyces galilaeus
"A gene cluster from Streptomyces galilaeus involved in glycosylation of aclarubicin". Molecular & general genetics : MGG. 264 ( ...
*  Chemotherapy
This group includes novobiocin, merbarone, and aclarubicin, which also have other significant mechanisms of action. The ... Other clinically used drugs in the anthracyline group are pirarubicin, aclarubicin, and mitoxantrone. The mechanisms of ...
*  Spinal muscular atrophy
"Aclarubicin treatment restores SMN levels to cells derived from type I spinal muscular atrophy patients". Human Molecular ... like sodium orthovanadate and aclarubicin. Morpholino-type antisense oligonucleotides, with the same cellular target as ...
*  Streptomyces isolates
... aclarubicin, tomaymycin, sibiromycin, and mazethramycin. Derivatives of Streptomycetes isolate migrastatin, including ...
*  Schedule H
2006 Abacavir Abciximab Acebutolol Hydrochloride Aclarubicin Inj Actilyse Adrenocorticotrophic hormone (ACTH) Alclometasone ...
*  List of MeSH codes (D09)
... aclarubicin MeSH D09.408.051.059.200 --- daunorubicin MeSH D09.408.051.059.200.150 --- carubicin MeSH D09.408.051.059.200.175 ...
*  ATC code L01
L01DA01 Dactinomycin L01DB01 Doxorubicin L01DB02 Daunorubicin L01DB03 Epirubicin L01DB04 Aclarubicin L01DB05 Zorubicin L01DB06 ...
*  List of drugs: Ac
... aclarubicin (INN) aclatonium napadisilate (INN) aclidinium bromide (USAN, INN) Aclovate acolbifene (USAN) acodazole (INN) ...
*  List of MeSH codes (D04)
... aclarubicin MeSH D04.615.562.050.200 --- daunorubicin MeSH D04.615.562.050.200.150 --- carubicin MeSH D04.615.562.050.200.175 ...
Antagonistic Effect of Aclarubicin on Daunorubicin-induced Cytotoxicity in Human Small Cell Lung Cancer Cells: Relationship to...  Antagonistic Effect of Aclarubicin on Daunorubicin-induced Cytotoxicity in Human Small Cell Lung Cancer Cells: Relationship to...
Aclarubicin had no influence on the accumulation of daunorubicin in these cells. In contrast, the accumulation of daunorubicin ... Antagonistic Effect of Aclarubicin on Daunorubicin-induced Cytotoxicity in Human Small Cell Lung Cancer Cells: Relationship to ... Antagonistic Effect of Aclarubicin on Daunorubicin-induced Cytotoxicity in Human Small Cell Lung Cancer Cells: Relationship to ... Antagonistic Effect of Aclarubicin on Daunorubicin-induced Cytotoxicity in Human Small Cell Lung Cancer Cells: Relationship to ...
more infohttp://cancerres.aacrjournals.org/content/51/19/5093
Aclarubicin - Wikipedia  Aclarubicin - Wikipedia
Aclarubicin (INN) or aclacinomycin A is an anthracycline drug that is used in the treatment of cancer. Soil bacteria ... October 1991). "Antagonistic effect of aclarubicin on daunorubicin-induced cytotoxicity in human small cell lung cancer cells: ... Streptomyces galilaeus can produce aclarubicin. It can induce histone eviction from chromatin upon intercalation. CID 451415 ...
more infohttps://en.wikipedia.org/wiki/Aclarubicin
Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) | Proteasome Inhibitor | MedChemExpress  Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) | Proteasome Inhibitor | MedChemExpress
Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity ... Aclacinomycin A hydrochloride (Synonyms: Aclarubicin hydrochloride). Cat. No.: HY-N2306A Purity: 98.08% Data Sheet SDS Handling ... Aclarubicin, an anthracycline anti-cancer drug, fluorescently contrasts mitochondria and reduces the oxygen consumption rate in ... Aclarubicin, an anthracycline anti-cancer drug, fluorescently contrasts mitochondria and reduces the oxygen consumption rate in ...
more infohttps://www.medchemexpress.com/Aclacinomycin_A_hydrochloride.html
Drug Information  Drug Information
Aclarubicin Aclarubicin or aclacinomycin A is used to treat acute non lymphocytic leukemia, a cancer of the blood and bone ...
more infohttps://www.medindia.net/doctors/drug_information/home.asp
Khandelwal Laboratories Pvt. Ltd. Product Information | Medindia  Khandelwal Laboratories Pvt. Ltd. Product Information | Medindia
Aclarubicin Aclarubicin or aclacinomycin A is used to treat acute non lymphocytic leukemia, a cancer of the blood and bone ...
more infohttps://www.medindia.net/drugs/manufacturers/khandelwal-laboratories-pvt-ltd.htm
Schedule H - Wikipedia  Schedule H - Wikipedia
Schedule H is a class of prescription drugs in India appearing as an appendix to the Drugs and Cosmetics Rules, 1945 introduced in 1945. These are drugs which cannot be purchased over the counter without the prescription of a qualified doctor.The manufacture and sale of all drugs are covered under the Drugs and Cosmetics Act and Rules. It is revised at times based on the advice of the Drugs Technical Advisory Board, part of the Central Drugs Standard Control Organization[1] in the Ministry of Health and Family Welfare. The most recent schedule H (2006) lists 536 drugs from abacavir to zuclopenthixol.[2] However, enforcement of Schedule H laws in India is lax, compared to the more restrictive Schedule X, for which a mandatory documentation trail must be maintained.[3] ...
more infohttps://en.wikipedia.org/wiki/Schedule_H
Patente WO2011099007A1 - Pharmaceutical compositions and methods for the treatment and prevention of ... - Google Patentes  Patente WO2011099007A1 - Pharmaceutical compositions and methods for the treatment and prevention of ... - Google Patentes
... aclarubicin; acodazole hydrochloride; acronine; adozelesin; aldesleukin; altretamine; ambomycin; ametantrone acetate; amsacrine ...
more infohttp://www.google.es/patents/WO2011099007A1?cl=en
Patente US8102176 - NMR device for detection of analytes - Google Patentes  Patente US8102176 - NMR device for detection of analytes - Google Patentes
Examples of anti-cancer agents include acivicin; aclarubicin; acodazole hydrochloride; acronine; adriamycin; adozelesin; ...
more infohttp://www.google.es/patents/US8102176
Search of: leukodystrophy - List Results - ClinicalTrials.gov  Search of: leukodystrophy - List Results - ClinicalTrials.gov
Aclarubicin for the Treatment of Retinal Vasculopathy With Cerebral Leukodystrophy. *Vasculopathy, Retinal, With Cerebral ...
more infohttps://clinicaltrials.gov/ct2/results?cond=leukodystrophy&term=&cntry=&state=&city=&dist=
Aceclofenac - DrugBank  Aceclofenac - DrugBank
Aclarubicin. Aceclofenac may decrease the excretion rate of Aclarubicin which could result in a higher serum level.. ...
more infohttps://www.drugbank.ca/drugs/DB06736
Tiludronic acid - DrugBank  Tiludronic acid - DrugBank
Aclarubicin. Aclarubicin may increase the hypocalcemic activities of Tiludronic acid.. Investigational. Adapalene. The risk or ...
more infohttps://www.drugbank.ca/drugs/DB01133
BH-AC-AMP protocol
     Summary Report | CureHunter  BH-AC-AMP protocol Summary Report | CureHunter
chemotherapy protocol consisting of N(4)-behenoyl-1-beta-arabinofuranosylcytosine, aclarubicin, 6-mercaptopurine & prednisolone ...
more infohttp://www.curehunter.com/public/keywordSummaryC045192-BH-AC-AMP-protocol.do
Application # 2012/0035268. SPHINGO-GUANIDINES AND THEIR USE AS INHIBITORS OF SPHINGOSINE KINASE - Patents.com  Application # 2012/0035268. SPHINGO-GUANIDINES AND THEIR USE AS INHIBITORS OF SPHINGOSINE KINASE - Patents.com
... aclarubicin; acylfulvene; adecypenol; adozelesin; aldesleukin; ALL-TK antagonists; altretamine; ambamustine; amidox; amifostine ... aclarubicin; acodazole hydrochloride; acronine; adozelesin; aldesleukin; altretamine; ambomycin; ametantrone acetate; ...
more infohttp://patents.com/us-20120035268.html
US Patent # 9,987,258. Histone deacetylase as a modulator of PDL1 expression and activity - Patents.com  US Patent # 9,987,258. Histone deacetylase as a modulator of PDL1 expression and activity - Patents.com
Aclarubicin; Acodazole Hydrochloride; AcrQnine; Adozelesin; Aldesleukin; Altretamine; Ambomycin; Ametantrone Acetate; ...
more infohttp://patents.com/us-9987258.html
METHODS AND COMPOSITIONS FOR TREATING CANCER - GLOBAVIR BIOSCIENCES, INC.  METHODS AND COMPOSITIONS FOR TREATING CANCER - GLOBAVIR BIOSCIENCES, INC.
... aclarubicin; acodazole hydrochloride; acronine; adozelesin; aldesleukin; alemtuzumab; allopurinol; alitretinoin; altretamine; ...
more infohttp://www.sumobrain.com/patents/wipo/Methods-compositions-treating-cancer/WO2016201354A1.html
Dosage Forms
      - Dosage Form
     Summary Report | CureHunter  Dosage Forms - Dosage Form Summary Report | CureHunter
06/01/1992 - "Enhancement of therapeutic efficacy of aclarubicin against lymph node metastases using a new dosage form: ... aclarubicin adsorbed on activated carbon particles.". 07/01/1985 - "As systemic cancer chemotherapy was not so effective, ...
more infohttp://www.curehunter.com/public/keywordSummaryD004304-Dosage-Forms-Dosage-Form.do
WO2007028171A1 - Methods of using (+)-1,4-dihydro-7-[(3s,4s)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1...  WO2007028171A1 - Methods of using (+)-1,4-dihydro-7-[(3s,4s)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1...
... aclarubicin; acylfulvene; adecypenol; adozelesin; aldesleukin; ALL-TK antagonists; altretamine; ambamustine; amidox; amifostine ...
more infohttps://patents.google.com/patent/WO2007028171A1/en
Patent US20110152683 - Abrading Balloon Catheter for Extravasated Drug Delivery - Google Patents  Patent US20110152683 - Abrading Balloon Catheter for Extravasated Drug Delivery - Google Patents
... aclarubicin, and bleomycin; plant alkaloids and terpenoids, such as noscapine, vincristine, vinblastine, vinorelbine, vindesine ...
more infohttp://www.google.co.uk/patents/US20110152683
KAKEN - Research Projects | Analysis of origin and spreading of Ca^|2+| transients by digital imaging system in isolated...  KAKEN - Research Projects | Analysis of origin and spreading of Ca^|2+| transients by digital imaging system in isolated...
Publications] Kyosuke Temma: 'Comparison of cardiac actions of doxorubicin,pirarubicin and aclarubicin in isolated guinea-pig ... Publications] Kyosuke Temma: 'Comparisn of cardiac actions of doxorubicin, pirarubicin and aclarubicin in isolated guinea-pig ... Publications] Kyosuke Temma: 'Comparison of cardiac actions of doxorubicin,pirarubicin and aclarubicin in isolated guines-pig ...
more infohttps://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-04660330/
  • The effect of combinations of the anthracyclines aclarubicin and daunorubicin was investigated in a clonogenic assay using the human small cell lung cancer cell line OC-NYH and a multidrug-resistant (MDR) murine subline of Ehrlich ascites tumor (EHR2/DNR+). (aacrjournals.org)