• The plant source of colchicine, the autumn crocus (Colchicum autumnale), was described for treatment of rheumatism and swelling in the Ebers Papyrus (ca. 1500 B.C.), an Egyptian medical papyrus. (industrialtechnologies.in)
  • As of 2009, Colcrys is the only brand of colchicine approved by the FDA. (rxlist.com)
  • Our Colcrys (colchicine, USP) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication. (rxlist.com)
  • COLCRYS (colchicine, USP) tablets are supplied for oral administration as purple, filmcoated, capsule-shaped tablets (0.1575" x 0.3030"), debossed with "AR 374" on one side and scored on the other, containing 0.6 mg of the active ingredient colchicine USP. (rxlist.com)
  • COLCRYS (colchicine, USP) tablets are indicated for prophylaxis and the treatment of acute gout flares. (rxlist.com)
  • The novel tubulin-binding checkpoint activator BAL101553 inhibits EB1-dependent migration and invasion and promotes differentiation of glioblastoma stem-like cells. (swissbiotech.org)
  • ABSTRACT Colchicine, both in vitro and in vivo, inhibits secretion o f a l b u m i n and o t h e r p l a s m a proteins. (docksci.com)
  • Dabigatran reversibly binds to and inhibits the activity of thrombin, a serine protease that converts fibrinogen into fibrin. (blogspot.com)
  • Dabrafenib selectively binds to and inhibits the activity of B-raf, which may inhibit the proliferation of tumor cells which contain a mutated BRAF gene. (blogspot.com)
  • Dacetuzumab specifically binds to and inhibits the CD40 receptor, thereby inducing apoptosis and inhibiting cellular proliferation via antibody-dependent cellular cytotoxicity (ADCC) in cells that overexpress this receptor. (blogspot.com)
  • Apart from inhibiting mitosis (a process heavily dependent on cytoskeletal changes), colchicine also inhibits anti-inflammatory effect. (homecuresforgout.org)
  • Tubulin-binding drugs kill cancerous cells by inhibiting microtubule dynamics, which are required for DNA segregation and therefore cell division. (wikipedia.org)
  • After the dimer is incorporated into the microtubule, the molecule of GTP bound to the β-tubulin subunit eventually hydrolyzes into GDP through inter-dimer contacts along the microtubule protofilament. (wikipedia.org)
  • Whether the β-tubulin member of the tubulin dimer is bound to GTP or GDP influences the stability of the dimer in the microtubule. (wikipedia.org)
  • 1. A novel orally active microtubule destabilizing agent S-40 targets the colchicine-binding site and shows potent antitumor activity. (nih.gov)
  • 5. The novel microtubule-destabilizing drug BAL27862 binds to the colchicine site of tubulin with distinct effects on microtubule organization. (nih.gov)
  • 13. Discovery of potent microtubule-destabilizing agents targeting for colchicine site by virtual screening, biological evaluation, and molecular dynamics simulation. (nih.gov)
  • 17. Quinolin-6-Yloxyacetamides Are Microtubule Destabilizing Agents That Bind to the Colchicine Site of Tubulin. (nih.gov)
  • Although the mechanism by which they disrupt mitosis and cell replication is novel and unique to this class of compounds, there are small but important differences in the formation of the stable, nonfunctional microtubule bundles and in the affinity of the two compounds for binding sites. (nih.gov)
  • 4. The Design, Synthesis, and Biological Activities of Pyrrole-Based Carboxamides: The Novel Tubulin Inhibitors Targeting the Colchicine-Binding Site. (nih.gov)
  • 6. Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. (nih.gov)
  • 7. Targeting Tubulin-colchicine Site for Cancer Therapy: Inhibitors, Antibody- Drug Conjugates and Degradation Agents. (nih.gov)
  • Post molecular mechanics/generalized born surface area analysis of these potent inhibitors showed dG binding values -37.83 and -28.37 kcal/mol, respectively. (isfcppharmaspire.com)
  • 4. Khattab M, Al-Karmalawy A. Computational repurposing of benzimidazole anthelmintic drugs as potential colchicine binding site inhibitors. (isfcppharmaspire.com)
  • 6. Wu X, Wang Q, Li W. Recent advances in heterocyclic tubulin inhibitors targeting the colchicine binding site. (isfcppharmaspire.com)
  • Tubulin inhibitors binding to colchicine-site: a review from 2015 to 2019[J]. Curr Med Chem, 2020, 27(40):6787-6814. (magtechjournal.com)
  • The sensitivities of S. gordonii internalization to inhibitors cytochalasin D, colchicine and monensin indicated uptake through endocytosis, with requirement for actin accumulation. (elsevierpure.com)
  • What cytoskeletal component do colchicines affect, and why would drugs that target this component be effective at treating cancer? (bestnursingassignmenthelp.com)
  • In this study, polymorphisms in the colchicine-binding site of the TUBB1 gene, which encodes a tubulin isoform specific to leukocytes, were investigated in patients with colchicine-resistant disease. (nih.gov)
  • In addition, several anti-worm drugs preferentially target the colchicine site of β-Tubulin in worm rather than in higher eukaryotes. (wikipedia.org)
  • 2. Colchicine Binding Site Agent DJ95 Overcomes Drug Resistance and Exhibits Antitumor Efficacy. (nih.gov)
  • 8. The discovery of novel indazole derivatives as tubulin colchicine site binding agents that displayed potent antitumor activity both in vitro and in vivo. (nih.gov)
  • 9. The compound millepachine and its derivatives inhibit tubulin polymerization by irreversibly binding to the colchicine-binding site in β-tubulin. (nih.gov)
  • 16. Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site. (nih.gov)
  • Novel Cytocidal Substituted Phenyl 4-(2-Oxoimidazolidin-1-yl) Benzenesulfonates and Benzenesulfonamides with Affinity to the Colchicine-Binding Site: Is the Phenyl 2-Imidazolidinone Moiety a New Haptophore for the Design of New Antimitotics? (scirp.org)
  • These chemicals work by binding to colchicine sensitive site of beta tubulin of intestinal cells of worms. (umabrothers.net)
  • LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2/M arrest. (usuhs.edu)
  • Compound 90b possessed a mean GI 50 value of 22 nM in the NCI60 cell line screen, displayed minimal cytotoxicity and was shown to interact at the colchicine-binding site on β-tubulin. (tudublin.ie)
  • It binds to CD20 antigen, inducing complement- or antibody-mediated cytolysis. (medscape.com)
  • Upon antibody/antigen binding and internalization, the cytotoxic agent induces tumor cell apoptosis, through an as of yet not publicly known mechanism. (nih.gov)
  • Upon administration, tarlatamab binds to both the CD3 antigen on cytotoxic T-lymphocytes (CTLs) and the DLL3 antigen found on DLL3-expressing tumor cells. (nih.gov)
  • While mebendazole still retains some binding affinity to human and Drosophila β-tubulin, albendazole almost exclusively binds to the β-tubulin of worms and other lower eukaryotes. (wikipedia.org)
  • Solution studies revealed that TTL binds at the polymerization, we investigated whether binding of edge of the tubulin dimer, making contacts mostly full-length stathmin and TTL to tubulin are mutually with -tubulin and possibly the protomer junction exclusive and whether TTL can form a triple complex where it can interfere with both longitudinal and with tubulin:stathmin and tyrosinate it efficiently. (nih.gov)
  • However, the therapeutic value of colchicine against cancer is (as is typical with chemotherapy agents) limited by its toxicity against normal cells. (homecuresforgout.org)
  • Colchicine toxicity can be potentiated by the concomitant use of cholesterol-lowering drugs (statins, fibrates). (homecuresforgout.org)
  • Colchicine inhibition of plasma protein release from rat hepatocytes. (docksci.com)
  • IL-1 inhibition is a treatment option for most (especially children) colchicine resistant FMF patients. (biomedcentral.com)
  • Upon administration of anti-HER2 ADC RC48, the antibody moiety targets and binds to HER2 on tumor cells. (nih.gov)
  • After binding to the EGF receptor, the agent is internalized by the cell, where the diphtheria toxin moiety exerts its cytotoxic effect, inhibiting protein synthesis through ADP-ribosylation of elongation factor 2. (blogspot.com)
  • This paper reports the results of a detailed study of the action of colchicine and other functionally related agents in inhibiting, in vitro and in vivo, the secretion of albumin and other plasma proteins by rat liver. (docksci.com)
  • Colchicine resistance was defined as ongoing disease activity (≥ 1 attack/month over 3 months or persistently elevated CRP) while taking the maximum tolerated dose of colchicine. (nih.gov)
  • Ten to 20% of a colchicine dose is excreted unchanged by the kidneys. (homecuresforgout.org)
  • Colchicine does not inhibit protein synthesis at these concentrations. (docksci.com)
  • Internalization levels of S. gordonii were enhanced by expression of S. aureus fibronectin-binding protein A (FnBPA) on the S. gordonii cell surface. (elsevierpure.com)
  • These results suggest either that TTL and stathmin have a partially overlapping footprint on the tubulin dimer or that stathmin induces a tubulin conformation incompatible with stable TTL binding. (nih.gov)
  • None of the colchicine metabolites in concentrations ranging from 10(-6) to 10(-4) M was able to protect phospholipids against peroxidation induced by either azo-initiators of peroxyl radicals or via myeloperoxidase (MPO)-catalyzed reactions in the presence of hydrogen peroxide. (cdc.gov)
  • While both of the C-terminal NDE1-GFP fusions accumulated at the IS, only NDE1-mEGFP showed the ability to bind dynein. (utexas.edu)
  • KA alone had little effect on lambda binding, whereas COL alone caused large decreases. (nih.gov)
  • KA plus COL caused even larger decreases in lambda binding, to as much as 85% below control. (nih.gov)
  • To determine if rilonacept, a fusion protein that binds and neutralizes IL-1, decreases the number of FMF attacks compared to placebo. (biomedcentral.com)
  • Since one of the defining characteristics of cancer cells is a significantly increased rate of mitosis, this means that cancer cells are significantly more vulnerable to colchicine poisoning than are normal cells. (homecuresforgout.org)
  • Colchicine elicits various effects on neutrophil migration, degranulation, and activation that may diminish inflammation. (medscape.com)
  • Anti-/pro-oxidant effects of phenolic compounds in cells: are colchicine metabolites chain-breaking antioxidants? (cdc.gov)
  • Using our fluorescence-HPLC assay with metabolically incorporated oxidation-sensitive cis-parinaric acid (PnA) we studied the effects of colchicine metabolites on peroxidation of different classes of membrane phospholipids in HL-60 cells. (cdc.gov)
  • Quantitative in vitro autoradiography was used to assess the effects of kainic acid (KA) and colchicine (COL) on mu and lambda opiate binding in the rat hippocampus. (nih.gov)
  • The GTP molecule bound to the α-tubulin subunit is not hydrolyzed during the whole process. (wikipedia.org)
  • Here we explore the mutual relationship between these proteins in vitro and demonstrate that full-length stathmin and TTL compete for binding to tubulin and fail to make a stable tubulin:stathmin:TTL triple complex in solution. (nih.gov)
  • Colchicine has no effect on t r a n s p o r t o f secretory proteins in the rough or s m o o t h e n d o p l a s m i c reticulum but it causes these proteins to a c c u m u l a t e in G o l g i - d e r i v e d secretory vesicles. (docksci.com)
  • Here, using Jurkat cells as a model T cell system, we showed that the dynein-binding proteins NDE1 and p150 [superscript Glued] form mutually exclusive complexes with dynein and exhibit non-overlapping distributions in target-stimulated Jurkat cells. (utexas.edu)
  • The typical treatment for the disease is colchicine. (nih.gov)
  • Levels of mu binding were markedly increased in all regions 48 h after treatment with KA. (nih.gov)
  • There is no current treatment alternative for patients with FMF whose disease is resistant to, or do not tolerate colchicine. (biomedcentral.com)
  • The British drug development company Angiogene is developing a prodrug of a colchicine congener, ZD6126 [15] (also known as ANG453) as a treatment for cancer . (homecuresforgout.org)
  • Tubulin-binding properties aside, colchicine metabolites remain largely untested for other possible biological activities, including antioxidant activity. (cdc.gov)
  • Human α-tubulin subtypes include:[citation needed] TUBA1A TUBA1B TUBA1C TUBA3C TUBA3D TUBA3E TUBA4A TUBA8 All drugs that are known to bind to human tubulin bind to β-tubulin. (wikipedia.org)
  • Colchicine is an alkaloid chemically described as (S)N- (5,6,7,9-tetrahydro- 1,2,3, 10-tetramethoxy-9-oxobenzo [alpha] heptalen-7-yl) acetamide with a molecular formula of C 22 H 25 NO 6 and a molecular weight of 399.4. (rxlist.com)
  • Electron spin resonance (ESR) experiments demonstrated that in a catalytic system containing horseradish peroxidase (HRP)/H(2)O(2), colchicine metabolites undergo one-electron oxidation to form phenoxyl radicals that, in turn, cause ESR-detectable ascorbate radicals by oxidation of ascorbate. (cdc.gov)
  • It cant occur any sooner either McHale, The University of BirminghamDr Jonathan entire second act preparing for that statistically most signicant prediction by in vitro binding experiments. (season2seasonconstruction.com)
  • Colchicine, a d m i n i s t e r e d intravenously, acts within 2 min and its inhibitory effect lasts for at least 3 h. (docksci.com)
  • Phenoxyl radicals of colchicine metabolites formed through MPO-catalyzed H(2)O(2)-dependent reactions in HL-60 cells and via HRP/H(2)O(2) in model systems can also oxidize GSH. (cdc.gov)
  • Administration of kainic acid and colchicine alters mu and lambda opiate binding in rat hippocampus. (nih.gov)
  • Upon administration of mipasetamab uzoptirine, mipasetamab binds to AXL, which is expressed on the surfaces of a variety of cancer cell types. (nih.gov)
  • However, a subset of patients are not responsive to colchicine. (nih.gov)
  • A total of 62 Turkish FMF patients (42 colchicine-responsive and 20 colchicine-resistant) and a control group of healthy children were included in the study. (nih.gov)
  • Subjects were FMF patients ≥4 years of age recruited at 6 U.S. sites, who had at least 1 FMF attack per month despite receiving adequate doses of, or who were intolerant of colchicine. (biomedcentral.com)
  • Long-term (prophylactic) regimens of oral colchicine are absolutely contraindicated in patients with advanced renal failure (including those on dialysis). (homecuresforgout.org)
  • In addition, the low protein level of MyoD-Y156F was recovered over that of crazy type by an Somatostatin additional mutation at Leu-164, a critical binding residue of MAFbx/AT-1, a Skp, Cullin, F-box (SCF) E3-ubiquitin Somatostatin ligase. (immune-source.com)