Mechanisms of action of flavopiridol

Critical Reviews in Oncology/Hematology

Volumn 38, Issue 2, 2001, Pages 139-170

  Sedlacek, H H ^a  

^a SANOFI AVENTIS DEUTSCHLAND GMBH   (Germany)

Author keywords

Antiangiogenic activity; Apoptosis; cdk; Cell cycle; Flavopiridol; Inhibitors; Mechanism of action; Multidrug resistance; Phospokinases

Indexed keywords

ANGIOGENESIS INHIBITOR; CYCLIN DEPENDENT KINASE; CYCLIN DEPENDENT KINASE 1; CYCLIN DEPENDENT KINASE 2; CYCLIN DEPENDENT KINASE 4; CYCLIN DEPENDENT KINASE 6; CYCLIN DEPENDENT KINASE 7; CYTOSTATIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR; FLAVOPIRIDOL; GLYCOPROTEIN P; MITOGEN ACTIVATED PROTEIN KINASE; MULTIDRUG RESISTANCE PROTEIN; PHOSPHOTRANSFERASE; PROTEIN BCL 2; PROTEIN KINASE; PROTEIN KINASE C; PROTEIN P53; PROTEIN TYROSINE KINASE; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; APOPTOSIS; CELL CYCLE; CYTOTOXICITY; DRUG MECHANISM; DRUG POTENTIATION; ENZYME INHIBITION; HUMAN; LEUKEMIA CELL; MULTIDRUG RESISTANCE; MUTATION; NONHUMAN; REVIEW; SIGNAL TRANSDUCTION;

ANTINEOPLASTIC AGENTS; APOPTOSIS; CYCLIN-DEPENDENT KINASES; DRUG SYNERGISM; FLAVONOIDS; HUMANS; PIPERIDINES; TUMOR CELLS, CULTURED;

EID: 0035055595     PISSN: 10408428     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1040-8428(00)00124-4     Document Type: Review

References (327)

1. The change in research for the therapy of tumors
2. Flavopiridol (L868 275; NSC649 890), a new kinase inhibitor for tumor therapy
3. Flavopiridol induces apoptosis of normal lymphoid cells, causes immunosuppression, and has potent antitumor activity in vivo against human leukemia and lymphoma xenografts
4. Antitumoral activity of flavone L86-8275
5. Flavopiridol (L86-2875): selective antitumor activity in vitro and activity in vivo for prostate carcinoma cells
6. Flavopiridol a novel cyclin dependent kinase inhibitor prevents the growth of head and neck squamous cell carcinomas by inducing apoptosis
7. Synchronization of HeLa cell cultures by inhibition of DNA polymerase-α with aphidicolin
8. Growth inhibition with reversible cell cycle arrest of carcinoma cells by flavone L86 8275
9. Transcriptional regulation during the mammalian cell cycle
10. Flavopiridol enhances the biological effects of paclitaxel a phase I trial in patients with advanced solid tumors
11. Phase I trial of continuous infusion Flavopiridol, a novel cyclin-dependent kinase inhibitor, in patients with refractory neoplasms
12. Flavopiridol: the first cyclin-dependent kinase inhibitor in human clinical trials. Invest
13. The cyclin-dependent kinase inhibitor Flavopiridol is an active and unexpectedly toxic agent in advanced gastric cancer
14. Flavopiridol, a novel cyclin-dependent kinase inhibitor, in metastatic renal cancer: a University of Chicago phase II consortium study
15. Kinase inhibitors in cancer therapy: a look ahead
16. Determination of flavopiridol (L86 8275; NSC 649 890) in human plasma by reversed-phase liquid chromatography with electrochemical detection
17. Phase I clinical and pharmacokinetic trial of flavopiridol
18. Signals and genes in the control of cell-cycle progression
19. Cell cycle control and cancer
20. Cell cycle checkpoints
21. Lineage-specific regulation of cell cycle gene expression in differentiating myeloid cells
22. Growth suppression by p18, a p16INK4/MTS1- and p14 INK4B/MTS2-related cdk6 inhibitor, correlates with wild-type pRb function
23. p15INK4B is a potential effector of TGFfl-induced cell cycle arrest
24. Cyclins and cancer. II: cyclin D and cdk inhibitors come of age
25. Cloning of senescent cell-derived inhibitors of DNA synthesis using an expression screen
26. Joining the complex: cyclin-dependent kinase inhibitory proteins and the cell cycle
27. Cyclins, cyclin-dependent kinases and cdk inhibitors: implications in cell cycle control and cancer
28. Crystal structure of cyclin-dependent kinase 2
29. Mutational analysis supports a structural model for the cell cycle kinase p34
30. Sequences within the conserved cyclin box of human cyclin A are sufficient for binding to and activation of cdc2 kinase
31. Cell cycle: will the real cdk-activating kinase please stand up
32. Effects of phosphorylation by CAK on cyclin binding by cdc2 and cdk2
33. cdc2 phosphorylation is required for its interaction with cyclin
34. Substrate specificity of cdc2 kinase from human HeLa cells as determined with synthetic peptides and molecular modelling
35. Cyclin C/cdk8 is a novel CTD kinase associated with RNA polymerase II
36. Cell cycle-related variation and tissue-restricted expression of human cyclin D1 protein
37. Regulation of cyclin D1 by calpain protease
38. How proteolysis drives the cell cycle
39. Components of a system that ligated cyclin to Ubiquitin and their regulation by the protein kinase cdc2
40. Mitosis in transition
41. Cyclin A-Cys41 does not undergo cell cycle-dependent degradation in Xenopus extracts
42. Anaphase is initiated by proteolysis rather than by the inactivation of maturation-promoting factor
43. Direct binding of cyclin D to the retinoblastoma gene product (pRb) and pRb phosphorylation by the cyclin D-dependent kinase cdk4
44. Cyclin D 1 protein expression and function in human breast cancer
45. Redundant cyclin overexpression and gene amplification in brest cancer cells
46. A novel cyclin encoded by a bcl1-linked candidate oncogene
47. Role of the cyclin-dependent kinase inhibitors in the development of cancer
48. Expression of cyclin A in soft tissue sarcomas correlates with tumor aggressiveness
49. Cyclin E, a potential prognostic marker for breast cancer
50. CDK4 amplification is an alternative mechanism to p16 gene homozygous deletion in glioma cell lines
51. A p16INK4a-insensitive CDK4 mutant targeted by cytolytic T lymphocytes in a human melanoma
52. Silencing of p16/CDKN2 expression in human gliomas by methylation and chromatin condensation
53. A cell cycle regulator potentially involved in genesis of many tumor types
54. Control and activity of type-1 serine/threonine protein phosphatase during the cell cycle
55. Functional inactivation of the retinoblastoma protein requires sequential modification by at least two distinct cyclin-cdk complexes
56. G1 cyclin/cdk-independent phosphorylation and accumulation of p130 during the transition from G1 to G0 lead to its association with E2F-4
57. The interactions of E2F with pRb and with p107 are regulated via the phosphorylation of pRb and 107 by a cyclin-dependent kinase
58. p107 uses a p21CIP1-related domain to bind cyclin/cdk2 and regulate interactions with E2F
59. Differential roles of two tandem E2F sites in repression of the human p107 promoter by retinoblastoma and p107 proteins
60. Cell cycle control and cancer
61. The retinoblastoma gene family: cousins with overlapping interests
62. The retinoblastoma protein and cell cycle control
63. Retinoblastoma protein expressed in human non-Hodgkin's lymphoma cells generates resistance against radiation-induced apoptosis
64. RB protein status and clinical correlation from 171 cell lines representing lung cancer, extrapulmonary small cell carcinoma, and mesothelioma
65. Regulation of the retinoblastoma protein-related p107 by G1 cyclin complexes
66. Cell cycle-dependent phosphorylation of the retinoblastoma-related protein p130
67. Regulation and expression of retinoblastoma proteins p107 and p130 during 3T3-L1 adipocyte differentiation
68. Differential regulation of the retinoblastoma family of proteins during cell proliferation and differentiation
69. Activation in vitro of NF-kB by phosphorylation of its inhibitor IkB
70. Expression and activity of the retinoblastoma protein (pRb)-family proteins, p107 and p130, during L6 myoblast differentiation
71. The accumulation of an E2F-p130 transcriptional repressor distinguishes a G0 cell state from a G1 cell state
72. Distinct mechanisms control the accumulation of the Rb-related p107 and p130 proteins during cell growth
73. pRb and P107/p130 are required for the regulated expression of different sets of E2F responsive genes
74. Role of the retinoblastoma protein family, pRb, p107 and p130 in the negative control of cell growth
75. Physical interaction of the retinoblastoma protein with human D cyclins
76. Functional interactions of the retinoblastoma protein with mammalian D-type cyclins
77. Cyclin D1/cdk4 regulates retinoblastoma protein-mediated cell cycle arrest by site-specific phosphorylation
78. Cell cycle arrest and apoptosis in NSCLC cell lines by cyclin-dependent kinase inhibitor
79. Potent inhibition of cdc2 kinase activity by the flavonoid L86-8275
80. Inhibition of cdk2 by Flavopiridol and structural analoga
81. cdc2 kinase by the flavone L86-8275 in breast carcinoma cells
82. A family of human cdc2-related protein kinases
83. Production of large numbers of mitotic mammalian cells by use of the reversible microtubuline inhibitor nocodazole. Nocodazole accumulated mitotic cells
84. Flavopiridol induces G1 arrest with inhibition of cyclin-dependent kinase (cdk) 2 and cdk4 in human breast carcinoma cells
85. Inhibition of cdk2, cdk4 and cdk7 by Flavopiridol and structural analogs
86. Cyclin D1 and Cdk6 are the targets for Flavopiridol-mediated G1 block in MCF10A breast epithelial cell line
87. PITALRE, a nuclear CDC2-related protein kinase that phosphorylates the retinoblastoma protein in vitro
88. Targeting of cdk8 to a promoter-proximal RNA element demonstrates catalysis-dependent activation of gene expression
89. Down-regulation of cyclin D1 by transcriptional repression in MCF-7 human breast carcinoma cells induced by Flavopiridol
90. Structural basis for specificity and potency of a flavonoid inhibitor of human cdk2, a cell cycle kinase
91. Mechanism of cdk activation revealed by the structure of a cyclin A-cdk2 complex
92. Identification of cytosolic aldehyde dehydrogenase 1 from non-small cell lung carcinomas as a flavopiridol-binding protein
93. Flavopiridol, a protein kinase inhibitor, down-regulates hypoxic induction of vascular endothelial growth factor expression in human monocytes
94. The expanding role of cell regulators
95. Myc and ras collaborate in inducing accumulation of active cyclin E/Cdk2 and E2F
96. Participation of cyclin A in Myc-induced apoptosis
97. Unrestricted cell cyclin and cancer
98. Cancer cell cycles
99. Induction of differentiation accompanies inhibition of cdk2 in a non-small cell lung cancer cell lines
100. Antisense cyclin D1 induces apoptosis and tumor shrinkage in human squamous carcinoma
101. Adenovirally transferred p16INK4/CDKN2 and p53 genes cooperate to induce apoptotic tumor cell death
102. Chemotherapy-induced apoptosis
103. Enhanced sensitivity to 1-β-D-arabinofuranosylcytosine and topoisomerase II inhibitors in tumor cell lines harboring activated ras oncogenes
104. The ras oncogene-mediated sensitization of human cells to topoisomerase II inhibitor-induced apoptosis
105. Negative regulation of the growth-promoting transcription factor E2F-1 by a stably bound cyclin A-dependent protein kinase
106. Flavopiridol, a novel cyclin-dependent kinase inhibitor, suppresses the growth of head and neck squamous cell carcinomas by inducing apoptosis
107. Flavopiridol induces apoptosis in chronic lymphocytic leukemia cells via activation of caspase-3 without evidence of bcl-2 modulation or dependence on functional p53
108. Cell cycle-independent induction of apoptosis by the anti-tumor drug Flavopiridol in endothelial cells
109. Involvement of cell cycle elements, cyclin-dependent kinases, pRb and E2F DP, in B-amyloid-induced neuronal death
110. Selective sensitization of transformed cells to flavopiridol-induced apoptosis during S phase
111. Cytotoxic synergy between Flavopiridol (NSC 649 890, L86-2875) and various antineoplastic agents: the importance of sequence of administration
112. Synergistic interaction between Flavopiridol (FLAVO) and Taxol (TAX) in a p53-null non-small cell lung carcinoma (NSCLC) cell line
113. Inappropriate cell cycle progression enhances the induction of apoptosis by Flavopiridol (Flavo) in Taxol treated gastric cancer cells
114. The cyclin-dependent kinase (CDK) inhibitor Flavopiridol (Flavo) inhibits polyploidy in paclitaxel(P) treated p53-/- breast cancer cells
115. Sequential dependent enhancement of caspase activation and apoptosis by Flavopiridol on Paclitaxel-treated human gastric and breast cancer cells
116. Protein kinase C activity and multidrug resistance on MOLT-3 human lymphoblastic leukemia cells resistant to trimethotrexate
117. The protein kinase C (PKC) inhibitors UCN-01 and Flavopiridol (FLAVO) significantly enhance the cytotoxic effect of chemotherapy by promoting apoptosis in gastric and breast cancer cells
118. Sensitivity of tumor cells to the cyclin dependent kinase (CDK) inhibitor Flavopiridol (FLAVO) correlates to loss of bcl-2 expression
119. Potentiation of apoptosis by flavopiridol in mitomycin-C-treated gastric and breast cancer cells
120. Mitochondria in chemotherapy-induced apoptosis: a prospective novel target of cancer therapy (review)
121. The induction of apoptosis by chemotherapeutic agents occurs in all phases of the cell cycle
122. Sequential dependent enhancement of caspase activation and apoptosis by flavopiridol on paclitaxel-treated human gastric and breast cancer cells
123. Flavopiridol binds to duplex DNA
124. Flavopiridol, a cyclin-dependent kinase inhibitor, prevents spindle inhibitor-induced endoreduplication in human cancer cells
125. Caspase-dependent and -independent death of camptothecin-treated embryonic cortical neurons
126. Inhibitors of cyclin-dependent kinases promote survival of post-mitotic neuronally differentiated cells and sympathetic neurons
127. Multiple pathways of neuronal death induced by DNA-damaging agents, NGF deprivation, and oxidative stress
128. The mechanism of Ara-C-induced apoptosis of differentiating cerebellar granule neurons
129. G1/S cell cycle blockers and inhibitors of cyclin-dependent kinases suppress camptothecin-induced apoptosis
130. Cyclin-dependent kinases participate in death of neurons evokes by DNA-damaging agents
131. Flavopiridol: a cytotoxic flavone that induces cell death in noncyclin A549 human lung carcinoma cells
132. Potentiation of Flavopiridol-mediated apoptosis in non-small cell lung cancer cell lines following recruitment of cells to S phase
133. Flavopiridol mediates cell cycle arrest and apoptosis in esophageal cancer cells
134. In vitro evaluation of flavopiridol, a novel cell cycle inhibitor, in bladder cancer
135. Flavopiridol-induced apoptosis is associated with a decrease in cyclin D1 in mantle lymphoma cell lines
136. Flavopiridol enhances doxorubicin-induced apoptosis in human sarcoma cells lacking Rb protein
137. Retinoblastoma protein inhibits IFN-γ induced apoptosis
138. Retinoblastoma protein expressed in human non-Hodgkin's lymphoma cells generates resistance against radiation-induced apoptosis
139. RB protein status and clinical correlation from 171 cell lines representing lung cancer, extrapulmonary small cell carcinoma, and mesothelioma
140. Retinoblastoma protein inhibits IFN-γ induced apoptosis
141. Cyclin D1 expression is regulated by the retinoblastoma protein
142. Cyclin D1 is dispensable for G1 control in retinoblastoma gene-deficient cells independently of cdk4 activity
143. Absence of p16ink4 protein is restricted to the subset of lung cancer lines that retains wildtype Rb
144. Alterations of the cyclin D1/p16-pRB pathway in mantle cell lymphoma
145. Increased expression of the cyclin D1 gene in Barrett's esophagus
146. Mutations of cell cycle regulators. Biological and clinical implications for human neoplasia
147. The targeting of the cyclin D1 oncogene by an Epstein-Barr virus promoter in transgenic mice causes dysplasia in the tongue, esophagus and forestomach
148. Antisense to cyclin D1 inhibits growth and reverses the transformed phenotype of human esophageal cancer cells
149. Inhibition of esophageal cancer proliferation by adenoviral-mediated delivery of p16INK4
150. Roles for p53 in growth arrest and apoptosis: putting on the brakes after genotoxic stress
151. p53 mutations in human cancers
152. The p53 tumour suppressor gene
153. p53 and its 14 kDa C-terminal domain recognize primary DNA damage in the form of insertion/deletion mismatches
154. The C-terminal domain of p53 recognizes DNA damaged by ionizing radiation
155. Multisite phosphorylation and the integration of stress signals at p53
156. Complex regulation of the DNA-binding activity of p53 by phoshphorylation: differential effects of individual phosphorylation sites on the interaction with different binding motifs
157. Bcl-2 targets the protein kinase Raf-1 to mitochondria
158. Cytotoxicity of Flavopiridol in ovarian cancer cells, alone and in combination with CDDP
159. Breast cancer resistance protein (BCRP) associated drug export and p53 inactivation impact Flavopiridol (FLA) antitumor activity
160. The E1B 19K protein block apoptosis by interaction with and inhibiting the p53-inducibble and death-promoting Bax protein
161. The proto-oncogene Bcl-2 and its role in regulating apoptosis
162. Identification of a novel regulatory domain in Bcl-X(L) and Bcl-2
163. Double identity for proteins of the Bcl-2 family
164. The AML1/ETO fusion protein activates transcription of BCL-2
165. A dominant interfering Myb mutant causes apoptosis in T cells
166. A novel Bcl-2 related gene, Bfl-1, is overexpressed in stomach cancer and preferentially expressed in bone marrow
167. bcl-2 proto-oncogene expression in normal and neoplastic human myeolid cells
168. bcl-2 expression is reciprocal to p53 and c-myc expression in metastatic human colorectal cancer
169. L, an antiapoptotic member of the Bcl-2 family, in esophageal squamous cell carcinoma
170. Hematopoietic malignancies demonstrate loss-of-function mutations of BAX
171. The BAX gene, the promoter of apoptosis, is mutated in genetically unstable cancers of the colorectum, stomach, and endometrium
172. Somatic frameshift mutations in the BAX gene in colon cancers of the microsatellite mutator phenotype
173. Frameshift somatic mutations in gastrointestinal cancer of the microsatellite mutator phenotype
174. A matter of life and cell death
175. Tumor suppressor p53 is a direct transcriptional activator of the human bax gene
176. The Bcl-2 protein family: arbiters of cell survival
177. Akt phosphorylation of BAD couples survival signals to the cell intrinsic death machinery
178. Mitochondria and apoptosis
179. bcl-Xs-induced cell death in 3T3 cells does not require or induce caspase activation
180. Interleukin-3-induced phosphorylation of BAD through the protein kinase AKT
181. Expression of T-antigen in pleural mesothelioma delays Flavopiridol mediated cell cycle arrest and apoptosis
182. Phosphorylation of Bcl-2 is a marker of M phase events and not a determinant of apoptosis
183. Early induction of apoptosis in hematopoietic cell lines after exposure to Flavopiridol
184. Protein kinase C inhibitor 7OH-staurosporine (UCN-01) and CDK-family kinase inhibitor flavopiridol down regulation expression of survival genes and induce apoptosis in B-CLL chronic lymphocyte leukemia (B-CLL)
185. Flavopiridol: finally a chemotherapeutic that is Bcl-2 independent
186. Caspase-2 (Nedd-2) processing and death of trophic factor-deprived PC12 cells and sympathetic neurons occur independently of caspase-3 (CPP32)-like activity
187. Metabolism and the effects of epidermal growth factor and related growth factors in mammals
188. Protein tyrosine kinases and cancer
189. Epidermal growth factor dependent transformation by a human EGF receptor proto-oncogene
190. Growth factors in breast cancer
191. Transcripts for transforming growth factors in human breast cancer: clinical correlates
192. Epidermal growth factor: receptor and ligand expression in human breast cancer
193. The prognostic significance of transforming growth factors in human breast cancer
194. A new acquaintance for erbB3 and erbB4: a role for receptor heterodimerization in growth signalling
195. Heterodimerization of the erbB-1 and erbB-2 receptors in human breast carcinoma cells: a mechanism for receptor transregulation
196. p185c-neu and epidermal growth factor receptor associate into a structure composed of activated kinases
197. ErbB3 is involved in activating phosphatidylinositol 3-kinase by epidermal growth factor
198. Multiple independent activation of the neu oncogene by point mutations altering the transmembrane domain of p185
199. Epidermal growth factor-related peptides and their receptors in human malignancies
200. Overexpression of ErbB-2 or EGF receptor proteins present in early stage mammary carcinoma is detected simultaneously in matched primary tumors and regional metastases
201. c-ErbB-2/neu overexpression enhances metastatic potential of human lung cancer cells by induction of metastasis-associated properties
202. The phosphorylation connection to cancer (review)
203. A native 170 000 epidermal growth factor receptor-kinase complex from shed plasma membrane vesicles
204. Transcriptional repression of the D-type cyclin-dependent kinase inhibitor p167 by the retinoblastoma susceptibility gene product pRb
205. Grb2 mediated the EGF-dependent activation of guanine nucleotide exchange on Ras
206. ras
207. Phosphorylation of GAP and GAP-associated proteins by transforming and mitogenic tyrosine kinases
208. Receptors for epidermal growth factor and other polypeptide mitogens
209. Mechanism of epidermal growth factor receptor at threonine 669
210. Sensitization of tumor cells to ribotoxic stress-induced apoptotic cell death: A new therapeutic strategy
211. Induction of apoptosis and inhibition of c-erbB-2 in breast cancer cells by flavopiridol
212. The when and how of Src regulation
213. Involvement of pp60c-src with two major singlaing pathways in human breast cancer
214. Potentiation of epidermal growth factor receptor-mediated oncogenesis by c-Src: implications for the etiology of multiple human cancers
215. pp60c-src tyrosine kinase, myristylation, and modulatory domaons are required for enhanced mitogenic responsiveness to epdidermal growth factor seen in cells overexpressing c-src
216. Nonreceptor tyrosine protein kinases
217. Increased levels of β21ras-GTP and enhanced DNA synthesis accompany elevated tyrosyl phosphorylation of GAP-associated proteins, p190 and p62, in c-src overexpressors
218. Identification and characterization of a cytoskeleton-associated, epidermal growth factor sensitive pp60c-src substrate
219. Differential expression of ros oncogene in primary huan astrocytomas and astrocytoma cell lines
220. LAT: the ZAP-70 tyrosine kinase substrate that links T cell receptor to cellular activation
221. Inhibition of Src kinase by a selective tyrosine kinase inhibitor cases mitotic arrest
222. Protein kinase C inhibitors
223. Cell genetic evidence of correlation of intracellular translocation of protein kinase C (PKC) and PKC-mediated phosphorylation of 80-kDa protein with mitogenic action of tumor promoters
224. Lamin B phosphorylation by protein kinase calpha and proteolysis during apoptosis in human leukemia HL60 cells
225. The molecular heterogeneity of protein kinase C and its implications for cellular regulation
226. The protein kinase C family: heterogeneity and its implications
227. Protein kinase C - a family affair
228. Protein kinase C
229. Expression, purification, and characterization of protein kinase C-ε
230. Purification and characterisation of bovine brain protein kinase C isotypes α, β and γ
231. Elevated activities of protein kinase C and tyrosine kinase correlate to leukemic cell aggressiveness
232. Protein kinase C-α: a novel target for the therapy of androgen-independent prostate cancer?
233. Expression of the invasive phenotype by MCF7 human breast cancer cells transfected to overexpress protein kinase C-α or the erbB2 proto-oncogene
234. 12(S)-HETE enhancement of prostate tumor cell invasion: selective role of PKC-α
235. MCF7 breast cancer cells transfected with protein kinase C-α exhibit altered expression of other protein kinase C isoforms and display a more aggressive neoplastic phenotype
236. Constitutive presence of a catalytic fragment of protein kinase Cε in a small cell lung carcinoma cell line
237. 2+-dependent protein kinases in human colon carcinomas
238. Altered protein kinase C activity in biopsies of human colonic adenomas and carcinomas
239. Protein kinase C activity as marker for colorectal cancer
240. Alterations in protein kinase C isozymes α and β2 in activated Ha-ras containing papillomas in the absence of an increase in diacylglycerol
241. Inhibition of PCK inhibits growth an induces apoptosis in colorectal tumor cells
242. Telomerase is controlled by protein kinase Cα in human breast cancer cells
243. Protein kinase C (vertebrates)
244. Cells that overproduce protein kinase C are more susceptible to transformation by an activated H-ras oncogene
245. Synthesis of diacylglycerol de novo is responsible for permanent activation and down-regulation of protein kinase C in transformed cells
246. Evidence for a role of phosphatidylcholine-hydrolysing phospholipase C in the regulation of protein kinase C by ras and src oncogenes
247. Enhancement of inositol phospholipid metabolism and activation of protein kinase C in ras-transformed rat fibroblasts
248. Quantitative measurement of sn-1,2-diacylglycerols present in platelets, hepatocytes and ras- and sis-transformed normal rat kidney cells
249. Stimulation of phosphatidylcholine hydrolysis, diacylglycerol release and arachidonic acid production by oncogenic ras is a consequence of protein kinase C activation
250. Elevated levels of diacylglycerol and decreased phorbol ester sensitivity in ras-transformed fibroblasts
251. Transformation by a ras oncogene causes increased expression of protein kinase C-α and decreased expression of protein kinase C-ε
252. Expression of four protein kinase C isoforms in rat fibroblasts: distinct subcellular distribution and regulation by calcium and phorbol esters
253. Expression of four protein kinase C isoforms in rat fibroblasts: differential alterations in ras-, src- and fos-transformed cells
254. Purified transcription factor AP-1 interacts with TPA-inducible enhancer elements
255. Affinity-purified c-jun amino-terminal protein kinase requires serine/threonine phosphorylation for activity
256. Activation of protein kinase C decreases phosphorylation of c-jun at sites that negatively regulate its DNA-binding activity
257. C-fos promoter insensitivity to phorbol ester and possible role of protein kinase C in androgen-independent cancer cells
258. A cytokine-responsive IkappaB kinase that activates the transcription factor NF-kappaB
259. Inhibitors of both nuclear factor-kappaB and activator protein-1 activation block the neoplastic transformation response
260. Induction of apoptosis of cytokine-producing bladder cancer cells by adenovirus-mediated IκBα overexpression
261. Induction of apoptosis with I-κB, the inhibitor of NF-κB
262. Mechanism of telomerase induction during T cell activation
263. Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture
264. Telomerasaes
265. Activation of telomerase in a human tumor
266. Telomeres and telomerase: a simple picture becomes complex
267. Specific association of human telomerase activity with immortal cells and cancer
268. Selective phosphorylation of human DNA methyltransferase by protein kinase C
269. Inhibition of protein kinase C (PKC) arrests cell growth, induced apoptosis, and alters the effect of basic fibroblast growth factor (bFGF) on bcl-2 expression in chronic lymphoid malignancies
270. The potential of protein kinase C as a target for anticancer treatment
271. Regulation of cell death by protein kinase C
272. Development of multidrug resistance protein inhibitors
273. Biochemistry of multidrug resistance mediated by the multidrug transporter
274. Multidrug resistance mediated by the ATP-binding cassette transporter protein MRP
275. Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line
276. The MRP gene associated with a non-P-glycoprotein multidrug resistance encodes a 190-kDa membrane bound glycoprotein
277. Apoptosis induced by anticancer drugs
278. p53-dependent apoptosis modulates the cytoxicity of anticancer agents
279. Novel mechanisms of resistance to cancer chemotherapy
280. Multidrug resistance is more than MDR1 activity
281. The multidrug resistance P-glycoprotein
282. Overexpression of the gene encoding the multidrug resistance-associated protein results in increased ATP-dependent glutatione S-conjugate transport
283. ABC transporters: from micro-organisms to man
284. ATP-dependent transport of glutathione S-conjugates by the multidrug resistance-associated protein
285. Multidrug resistance proteins and other drug transport-related resistance to natural product agents
286. Modulation of activity of the promoter of the human MDR1 gene by Ras and p53
287. Cisplatin resistance in human cancers
288. Influence of myc overexpression on the phenotypic properties of Chinese hamster lung cells resistant to antitumor agents
289. Presence of the Raf-1 responsive element in human MDR1 promoter
290. Identification of specific sites in human P-glycoprotein phosphorylated by protein kinase C
291. Regulation of phorbol ester and protein kinase C inhibitors of P-glycoprotein phosphorylation and relationship of drug accumulation in multidrug-resistant human KB cells
292. Human multidrug resistant KB cells overexpress protein kinase C: involvement in drug resistance
293. Distinct patterns of phorbol ester-induced downregulation of protein kinase C activity in adriamycin-selected multidrug resistant and parental murine fibrosarcoma cells
294. Selective regulation of expression of protein kinase C (PKC) isoenzymes in multidrug resistant MCF-7 cells
295. Phorbol esters induce multidrug resistance in human breast cancer cells
296. Partial reversal of multidrug resistance in human breast cancer cells by an N-myristoylated protein kinase C-α pseudosubstrate peptide
297. Staurosporin, a potent inhibitor of C-kinase, enhances drug accumulation in multidrug resistant cells
298. Tissue-specific expression of three distinct types of rabbit protein kinase C
299. Transfection with protein kinase Cα confers increased multidrug resistance to MCF-7 cells expressing P-glycoprotein
300. Phosphorylation of the M 170 000 to 180 000 glycoprotein specific to multidrug-resistant tumor cells: effects of verapamil, trifluoperazine and phorbol esters
301. Drug resistance to the cyclin-dependent kinase (cdk) inhibitor, flavopiridol
302. Characterization of an ovarian carcinoma cell line resistant to cisplatin and flavopiridol
303. Potent interaction of flavopiridol with MRP1
304. Modulation by (iso)flavonoids of the ATPase activity of the multidrug resistance protein
305. Induction of apoptosis on tumor or normal cells: comparison between Flavopiridol and camptothecin
306. c-fos-induced growth factor/vascular endothelial growth factor D induces angiogenesis in vivo and in vitro
307. Wild-type p53 and v-Src exert opposing influences on human vascular endothelial growth factor gene expression
308. Flavopiridol inhibits angiogenesis
309. Integrins, proteases in angiogenesis
310. Angiogenesis modulates the tumour immune response
311. Angiogenesis inhibitors overcome tumor induced endothelial cell anergy
312. During angiogenesis, vascular endothelial growth factor and basic fibroblast growth factor regulate natural killer cell adhesion to tumor endothelium
313. Endothelial vascular cell adhesion molecule 1 expression is suppressed by melanoma and carcinoma
314. Thio-flavopiridol, a selective inhibitor of Cdk1
315. Flavopiridol produces growth arrest and apoptosis in NSCLC cell lines
316. Flavopiridol-mediated cdk inhibition results in p53-independent apoptosis in non-small cell lung cancer cell lines
317. Flavopiridol induces cell cycle arrest and p53-independent apoptosis in non-small cell lung cancer cell lines
318. The enhancement of chemotherapy-induced apoptosis by flavopiridol (FLAVO) in gastric cancer cells is sequence-dependent (meeting abstract)
319. Flavopiridol (F) potentiates gemcitabine (G) induced apoptosis in association with downregulation of ribonucleotide reductase (RR)
320. The novel cyclin-dependent kinase inhibitor Flavopiridol downregulates Bcl-2 and induces growth arrest and apoptosis in chronic B-cell leukemia lines
321. Differences between human wild-type and UCN-01 resistant A549 lung carcinoma cells in susceptibility towards apoptosis induction and changes in G1 checkpoint function by UCN-01