Tubulin as a target for anticancer drugs

Current Opinion in Drug Discovery and Development

Volumn 3, Issue 5, 2000, Pages 575-584

  Von Angerer, E ^a  

^a UNIVERSITY OF REGENSBURG   (Germany)

Author keywords

Cancer chemotherapy; Drug resistance; Microtubules; Natural products; Tubulin polymerization

Indexed keywords

AC 7700; ANTINEOPLASTIC AGENT; CEMADOTIN; COMBRETASTATIN; CRYPTOPHYCIN 52; CRYPTOPHYCIN DERIVATIVE; CYTOSTATIC AGENT; DISCODERMOLIDE; DOLASTATIN 10; DOLASTATIN 15; ELEUTHEROBIN; EPOTHILONE A; EPOTHILONE B; IDN 5109; INDANOCINE; NATURAL PRODUCT; NAVELBINE; ONCOCIDIN A1; PHENYLAHISTIN; PIRONETIN; SARCODICTYIN; SPIROKETAL PYRAN; SPIXET P; SULFONAMIDE; T 138067; TAXANE DERIVATIVE; TAXOL; TAXOTERE; TUBULIN; UNCLASSIFIED DRUG; UNINDEXED DRUG; VINBLASTINE; VINCRISTINE; VINFLUNINE;

ANTINEOPLASTIC ACTIVITY; CANCER; CANCER CHEMOTHERAPY; CLINICAL TRIAL; DRUG ISOLATION; DRUG POTENCY; DRUG SYNTHESIS; DRUG TARGETING; HUMAN; MICROTUBULE ASSEMBLY; MULTIDRUG RESISTANCE; PHASE 2 CLINICAL TRIAL; REVIEW; SIDE EFFECT;

EID: 0033770554     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (61)

1. Structure of the α/β tubulin dimer by electron crystallography
2. High-resolution model of the microtubule
3. Vinorelbine (Navelbine): A third-generation vinca alkaloid
4. Preclinical in vivo antitumor activity of vinflunine, a novel fluorinated vinca alkaloid
5. Antimitotic and tubulin-interacting properties of vinflunine, a novel fluorinated vinca alkaloid
6. Superior in vivo experimental antitumour activity of vinflunine, relative to vinorelbine, in a panel of human tumour xenografts
7. New inhibitors of tubulin polymerisation
8. Evaluation of antivascular and antimitotic effects of tubulin binding agents in solid tumor therapy
9. A novel combretastatin A-4 derivative, AC-7700, shows marked antitumor activity against advanced solid tumors and orthotopically transplanted tumors
10. Combretastatin A-4 phosphate as a tumor vascular-targeting agent: Early effects in tumors and normal tissues
11. Antitumor effects due to irreversible stoppage of tumor tissue blood flow: Evaluation of a novel combretastatin A-4 derivative, AC7700
12. Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization
13. Structure-activity requirements for flavone cytotoxicity and binding to tubulin
14. Recent progress in the development of tubulin inhibitors as antimitotic antitumor agents
15. Antitumor agents. 196 Substituted 2-thienyl-1,8-naphthyridin-4-ones: Their synthesis, cytotoxicity, and inhibition of tubulin polymerization
16. Synthesis end biological evaluation of dihydrobenzofuran lignans and related compounds as potential antitumor agents that inhibit tubulin polymerization
17. Indanocine, a microtubule-binding indanone and a selective inducer of apoptosis in multidrug-resistant cancer cells
18. Selective, covalent modification of β-tubulin residue Cys-239 by T138067, an antitumor agent with in vivo efficacy against multidrug-resistant tumors
19. Oncocldin A1: A novel tubulin-binding drug with antitumor activity against human breast and ovarian carcinoma xenografts in nude mice
20. Structure-based design of e novel synthetic spiroketal pyran as a pharmacophore for the marine natural product spongistatin 1
21. The dolastatins, a family of promising antineoplastic agents
22. Activity of dolastatin 10 against small-cell lung cancer In vitro and in vivo: Induction of apoptosis and Bcl-2 modification
23. Phase II study of dolastatin-10 in patients with advanced non-small-cell lung cancer
24. Novel marine-derived anti-cancer agents: A phase I clinical, pharmacological, and pharmacodynamic study of dolastatin 10 (NSC 376128) in patients with advanced solid tumors
25. Symplostatin 1: A dolastatin 10 analog from the marine cyanobacterium Symploca hydnoides
26. Suppression of microtubule dynamics by binding of cemadotin to tubulin: Possible mechanism for its antitumor action
27. A new tubulin polymerization inhibitor, auristatin PE, induces tumor regression in a human Waldenstrom's macroglobulinemia xenograft model
28. Synthesis and cytostatic properties of structure-simplified analogs of dolastatin 15
29. In vitro pharmacology of cryptophycin 52 (LY355703) in human tumor cell lines
30. Halohydrin analogs of cryptophycin 1: Synthesis and biological activity
31. Novel cryptophycin antitumor agents: Synthesis and cytotoxicity of fragment 'B' analogs
32. Antiproliferative mechanism of action of cryptophycin-52: Kinetic stabilization of microtubule dynamics by high-affinity binding to microtubule ends
33. Cytotoxic peptides hemiasterlin, hemiasterlin A and hemiasterlin B induce mitotic arrest and abnormal spindle formation
34. Interactions of the sponge-derived antimitotic tripeptide hemiasterlin with tubulin: Comparison with dolastatin 10 and cryptophycin 1
35. (-)-Phenylahistin arrests cells in mitosis by inhibiting tubulin polymerization
36. Antitumor activity of phenylahistin in vitro and in vivo
37. Apoptosis induction via microtubule disassembly by an antitumor compound, pironetin
38. Taxanes and other microtubule stabilising agents
39. Synthesis and structure-activity relationships of new second-generation taxoids
40. IDN5109, a taxane with oral bioavailability and potent antitumor activity
41. A novel taxane with improved tolerability and therapeutic activity in a panel of human tumor xenografts
42. Antibiotics from gliding bacteria. 77. Epothilone A and B - Novel 16-membered macrolides with cytotoxic activity: Isolation, crystal structure, and conformation in solution
43. Epothilone B stabilizes microtubuli of macrophages like taxol without showing taxol-like endotoxin activity
44. Activities of the microtubule-stabilizing agents epothilones A and B with purified tubulin and in cells resistant to paclitaxel (Taxol®)
45. Tubulin from paclitaxel-resistant cells as a probe for novel antimicrotubule agents
46. Desoxyepothilone B: An efficacious microtubule-targeted antitumor agent with a promising in vivo profile relative to epothilone B
47. Eleutherobin, a novel cytotoxic agent that induces tubulin polymerization, is similar to paclitaxel (Taxol)
48. The coral-derived natural products eleutherobin and sarcodictyins A and B: Effects on the assembly of purified tubulin with and without microtubule-associated proteins and binding at the polymer taxoid site
49. Total synthesis and chemical biology of the sarcodictyins
50. Structure-activity profiles of eleutherobin analogs and their cross-resistance in Taxol-resistant cell lines
51. Discodermolide, a cytotoxic marine agent that stabilizes microtubules more potently than taxol
52. The potent microtubule-stabilizing agent (+)-discodermolide induces apoptosis in human breast carcinoma cells - Preliminary comparisons to paclitaxel
53. Total synthesis of the antimicrotubule agent (+)-discodermolide using boron-mediated aldol reactions of chiral ketones
54. A common pharmacophore for cytotoxic natural products that stabilize microtubules
55. A common pharmacophore for epothilone and taxanes: Molecular basis for drug resistance conferred by tubulin mutations in human cancer cells
56. A common pharmacophore for Taxol and the epothilones based on the biological activity of a taxane molecule lacking a C-13 side chain
57. Biochemical, cellular, and pharmacological aspects of the multidrug transporter
58. Antisense oligonucleotides to class III β-tubulin sensitize drug-resistant cells to Taxol
59. Paclitaxel-resistant human ovarian cancer cells have mutant β-tubulins that exhibit impaired paclitaxel-driven polymerization
60. Markedly decreased binding of vincristine to tubulin in vinca alkaloid-resistant Chinese hamster cells is associated with selective overexpression of α and β tubulin isoforms
61. Molecular effects of paclitaxel: Myths and reality