Serine-threonine protein phosphatase inhibitors: Development of potential therapeutic strategies

Journal of Medicinal Chemistry

Volumn 45, Issue 6, 2002, Pages 1151-1175

  McCluskey, Adam ^a   Sim, Alistair T R ^a   Sakoff, Jennette A ^b  

^a UNIVERSITY OF NEWCASTLE   (Australia)

^b NEWCASTLE MATER HOSPITAL   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

CALCINEURIN; CALYCULIN A; CANTHARIDIC ACID; CANTHARIDIN; CYANOGINOSIN LR; CYCLOLINOPEPTIDE A; CYCLOSPORIN A; DISCORHABDIN P; DRAGMACIDIN D; DRAGMACIDIN E; FOSTRIECIN; ISOPALINURIN; NODULARIN; OKADAIC ACID; OKADAMYCIN; PALASONIN; PHENYL PHOSPHATE; PHOSPHOPROTEIN DARPP 32; PHOSPHOPROTEIN PHOSPHATASE; PHOSPHOPROTEIN PHOSPHATASE 1; PHOSPHOPROTEIN PHOSPHATASE 2A; PHOSPHOPROTEIN PHOSPHATASE 2C; PHOSPHOPROTEIN PHOSPHATASE 3; PHOSPHOPROTEIN PHOSPHATASE INHIBITOR; SERINE THREONINE PROTEIN PHOSPHATASE INHIBITOR; TACROLIMUS; TAUTOMYCETIN; TAUTOMYCIN; THYRISIFERYL 23 ACETATE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

AMINO ACID SEQUENCE; APOPTOSIS; CANCER; CELL CYCLE; CYSTIC FIBROSIS; DIABETES MELLITUS; DRUG ACTIVITY; DRUG MECHANISM; DRUG TARGETING; ENZYME ACTIVITY; ENZYME ANALYSIS; ENZYME BINDING; ENZYME INHIBITION; ENZYME REGULATION; ENZYME STRUCTURE; HUMAN; IMMUNOPATHOLOGY; METABOLIC DISORDER; MITOSIS; MOLECULAR MODEL; NERVE INJURY; NEUROLOGIC DISEASE; NONHUMAN; PARKINSON DISEASE; PROTEIN DEPHOSPHORYLATION; PROTEIN PHOSPHORYLATION; RESPIRATORY TRACT DISEASE; REVIEW; SEQUENCE HOMOLOGY; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION;

ALKENES; ANTIBIOTICS, ANTIFUNGAL; ANTIBIOTICS, ANTINEOPLASTIC; CANTHARIDIN; CRYSTALLOGRAPHY, X-RAY; CYCLOSPORINE; ENZYME INHIBITORS; HUMANS; MICROCYSTINS; MODELS, MOLECULAR; OKADAIC ACID; PEPTIDES, CYCLIC; PHOSPHOPROTEIN PHOSPHATASE; PYRANS; PYRONES; SPIRO COMPOUNDS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0037075845     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010066k     Document Type: Review

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170. Total synthesis of Calyculin C
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172. Isolation of dephosphonocalyculin A from the marine sponge Discodermia calyx
173. 37 fragment and model Wittig couplings
174. 25 fragment
175. Synthesis of trans-4-alkenyl oxazoles
176. Stereoselective methylations of bicyclic lactams derived from pyroglutamic acid
177. Total synthesis of (+)-calyculin A
178. The synthesis of naturally occurring (-)-Calyculin A
179. 37 fragment
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183. 37 γ-amino acid fragments
184. 25 spiroketal fragment
185. Reversal of aldehyde diastereofacial selectivity in a methyl ketenealdol reaction. Application to the synthesis of the calyculin spiroketal
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187. Triple asymmetric synthesis of fragment assembly. Validity of approximate multiplicity of the three diastereofacial selectivities
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189. Synthesis of γ-lactone derivatives as key intermediates for the spiroketal fragment in Calyculin A
190. An efficient synthesis of C20-C25 building blocks for Calyculin A
191. Synthesis of the tetraene fragment of Calycilins having natural configurations
192. A synthesis of the oxazole part of calyculins. Part 1
193. A synthesis of the oxazole part of calyculins. Part 2
194. Synthesis of 2,4-disubstituted oxazoles
195. Synthesis of the C26-C37 fragment of calyculin A having natural configuration
196. Synthesis of the tetraene fragment of calyculins having natural configurations
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198. Synthesis of the C13-C19 unit in the spiroketal fragment of calyculins
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200. New methods and reagents in organic synthesis. 94. Stereoselective synthesis of the C13-C19 fragment of the cytotoxic marine products, calyculins. Part 2
201. Calyculin synthetic studies. 4. Remarkable reversal of diastereoselectivity in Payne epoxidation of vinyl spiroketal intermediates
202. Calyculin synthetic studies. 3. Enantiomeric purity determination for the C26-C32 oxazole segment via the Silks-edom Se77 NMR method
203. Calyculin synthetic studies. 2. Stereocontrolled assembly of the C(9)-C(13) dithiane and C(26)-C(37) oxazole intermediates
204. Calyculin synthetic studies. Stereoselective construction of the C(14)-C(25) spiroketal subunit
205. Stereocontrolled synthesis of calyculin A: Construction of the C(26)-C(37) amide-oxazole unit
206. Stereocontrolled synthesis of calyculin A: Construction of the C(1)-C(14) tetraene nitrile unit
207. Stereocontrolled synthesis of calyculin A: Construction of the C(15)-C(25) spiro ketal unit
208. B-[3-((Diisopropylamino)-dimethylsilyl)allyl]diisopinocamphenylborane: An excellent reagent for the stereoselective synthesis of anti-vicinal diols
209. Calyculins - Asymmetric synthesis of the C26-C32 fragment
210. Enantiospecific synthesis of polyhydroxyamino acids. Synthesis of the C33-C38 portion of calyculins
211. A synthesis of the spiroketal subunit of (-)-Calyculin A
212. Total synthesis of (+)-Calyculin A and (-)Calyculin B
213. Total synthesis of(+)-Calyculin A and (-)-Calyculin B: Asymmetric synthesis of the C(9-25) spiroketal dipropionate subunit
214. Total synthesis of (+)-Calyculin A and (-)-Calyculin B: Cyanotetraene construction, asymmetric synthesis of the C(26-37) oxazole, fragment assembly, and final elaboration
215. Total synthesis of thyrsiferyl 23-acetate, a specific inhibitor of protein phosphatase 2A and an anti-leukemic inducer of apoptosis
216. Total syntheses of (+)-thyrsiferol, (+)-thyrsiferyl 23-acetate, and (+)-venustatriol
217. Total synthesis of fostriecin (CL920)
218. Synthesis of the 5R, 8R, 9S, 11R dephosphorylated derivative of CI-920, a novel antitumor agent
219. Total synthesis of(-)-Palasonin and (+)-Palasonin and related chemistry
220. Endothall thioanhydride: Structural aspects of unusually high mouse toxicity and specific binding site in liver
221. Synthesis of (±)-Palasonin
222. Simple, efficient total synthesis of cantharidin via a high-pressure Diels-Alder reaction
223. Organic reactions at high pressure. The preparative scale synthesis of cantharidin
224. Brain protein serine/threonine phosphatases
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226. Gating of CaMKII by cAMP-regulated protein phosphatase activity during LTP
227. Protein phosphatase 1 modulation of neostriatal AMPA channels: Regulation by DARPP-32 and spinophilin
228. Localization of the calcium/calmodulin-dependent protein phosphatase, calcineurin, in the hindbrain and spinal cord of the rat
229. Regulation of F-actin stability in dendritic spines by glutamate receptors and calcineurin
230. Calcineurin inhibition of dynamin-GTPase activity is coupled to nerve terminal depolarisation
231. Calcineurin regulation of synaptic function: From ion channels to transmitter release and gene transcription
232. Genetic and pharmacological evidence for a novel, intermediate phase of long-term potentiation suppressed by calcineurin
233. Differential activity of protein phosphatase types 1 and 2A in cytosolic and particulate fractions from rat forebrain
234. A novel pool of protein phosphatase 2A is associated with microtubules and is regulated during the cell cycle
235. Phosphatase activity toward abnormally phosphorylated τ: Decrease in Alzheimer disease brain
236. cAMP counter-regulates insulin-mediated protein phosphatase-2A inactivation in rat skeletal muscle cells
237. Altered regulation of insulin signaling components in adipocytes of insulin-resistant type II diabetic Goto-kakizaki rats
238. Polymorphism in the glycogen-associated regulatory subunit of type 1 protein phosphatase (PPP1R3) gene and insulin sensitivity
239. Phosphatase inhibitors activate normal and defective CFTR chloride channels
240. Association of cystic fibrosis transmembrane conductance regulator and protein phosphatase 2C
241. Protein phosphatase 2C dephosphorylates and inactivates cystic fibrosis transmembrance conductance regulator
242. Transient translocation and activation of protein phosphatase 2A during mast cell secretion
243. The cell cycle, signal transduction, and immunophilin ligand complexes
244. An oligiopeptide from linseed
245. Mapping of the immunophilin-immunosuppressant site of interaction on calcineurin
246. Immunosuppressant FK506 enhances phosphorylation of nitric oxide synthase and protects against glutamate neurotoxicity
247. A novel neuronal messenger molecule in brain: The free radical, nitric oxide
248. Nitric oxide: Physiology, pathophysiology, and pharmacology
249. Glutamate, nitric oxide and cell-cell signaling in the nervous system
250. Nitric oxide mediates glutamate neurotoxicity in primary cortical cultures
251. P59 (FK506 binding protein 59) interaction with heat shock proteins is highly conserved and may involve proteins other than steroid receptors
252. Permeability of the blood-brain barrier to the immunosuppressive cyclic peptide cyclosporin A
253. Neuropathologic findings in liver transplantation: A comparative study of cyclosporine and FK 506
254. PP2C - Gamma - A human protein phosphatase with a unique acidic domain
255. Cdc25 protein phosphatases in cell proliferation
256. Serine/threonine protein phosphatases
257. 2 phase checkpoints
258. Cyclins and cyclin-dependent kinases: Theme and variations
259. Regulation of protein kinase cascades by protein phosphatase 2A
260. Cell cycle regulation of a Xenopus Wee 1-like kinase
261. Hyperphosphorylation of the N-terminal domain of cdc25 regulates activity toward cyclin B1/cde2 but not cyelin A/cdk2
262. INH, a negative regulator of MPF, is a form of protein phosphatase 2A
263. Antitumor drug fostriecin inhibits the mitotic entry checkpoint and protein phosphatases 1 and 2A
264. Okadaie acid, a potent inhibitor of type 1 and 2A protein phosphatases, activates cdc2/H1 kinase and transiently induces a premature mitosis-like state in BHK21 cells
265. The phosphatase inhibitor okadaic acid stimulates the TSH-induces G1-S phase transition in thyroid cells
266. Okadaic acid overrides the S-phase checkpoint and accelerates progression of G2-phase to induce premature mitosis in HeLa cells
267. The retinoblastoma protein associates with the protein phosphatase type 1 catalytic subunit
268. High molecular weight protein phosphatase type 1 dephosphorylates the retinoblastoma protein
269. Distinct roles for PP1 and PP2A in phosphorylation of the retinoblastoma protein
270. 1 arrest in quiescent cells treated with phosphatase inhibitors
271. Cell cycle-dependent phosphorylation of mammalian protein phosphatase 1 by cdc2 kinase
272. Identification of protein phosphatase 1 as a mitotic lamin phosphatase
273. Stimulatory effect of okadaic acid, an inhibitor of protein phosphatases, on nuclear envelope breakdown and protein phosphorylation in mouse oocytes and one cell embryos
274. Protein phosphatase 1 is targeted to microtubules by the microtubule-associated protein tau
275. Protein phosphatase inhibitors induce the selective breakdown of stable microtubules in fibroblasts and epithelial cells
276. Regulation of Saccharomyces cerevisiae kinetochores by the type 1 phosphatase Glc7p
277. Okadaic acid co-induces vimentin expression and cell cycle arrest in MPC-11 mouse plasmacytoma cells
278. Balance between activities of rho kinase and type 1 protein phosphatase modulates turnover of phosphorylation and dynamics of desmin/vimentin filaments
279. Vimentin is hyperphosphorylated in primary human fibroblasts treated with okadaic acid
280. Cdc2-independent induction of premature mitosis by okadaic acid in HeLa cells
281. Reinitiation of host DNA synthesis in senescent human diploid cells by infection with simian virus 40
282. The interaction of SV40 small tumour antigen with protein phosphatase 2A stimulates the MAP kinase pathway and induces cell proliferation
283. Protein phosphatase 2A is a critical regulator of protein kinase C ζ signaling targeted by SV40 small t to promote cell growth and NF-κB activation
284. Expression of SET, an inhibitor of protein phosphatase 2A, in renal development and Wilms-tumor
285. Calyculin A, an inhibitor of protein phosphatases, a potent tumor promoter on CD-1 mouse skin
286. Unique features of the okadaic acid acitivity class of tumor promotors
287. Cantharidin
288. Anticancer activity and protein phosphatase 1 and 2A inhibition of a new generation of cantharidin analogues
289. Positive regulation of cdc2 gene activity by protein phosphatase type 2A
290. Comparitive effects of protein phosphatase inhibitors (okadaic acid and calyculin A) on human leukaemia HL60, HL60/ADR and K562
291. 3H] Cantharidin binding site in relation to cytotoxicity
292. Establishment of a human small-cell lung cancer subline resistant to okadaic acid
293. Unstable expression of the multi-drug resistant phenotype in chinese hamster ovary cells resistant to okadaic acid
294. Anticancer activity of the structurally novel antibiotic CI-920 and its analogues
295. In vitro activity of the novel antitumour antibiotic fostriecin (CI-920) in a human tumour cloning assay
296. Transport of the antitumour antibiotic CI-920 into L1210 leukaemis cells by the reduced folate carrier system
297. Fostriecin: A review of the preclinical data
298. Renal toxicity of the anticancer drug fostriecin
299. Phase 1 and pharmacokinetic study of the topoisomerase II catalytic inhibitor
300. The effects of cantharidin on epithelial cells in tissue culture
301. Medical uses of mylabris in ancient china and recent studies
302. Chemosensitivity of salivary gland and oral cancer cell lines
303. Activity of camptothecin, harrington, cantharidin and curcumae in the human stem cell assay
304. Doxorubicin-resistant LoVo adenocarcinoma cells display resistance to apoptosis induction by some but not all inhibitors of set thr phosphatases 1 and 2A
305. Inhibitory effect of norcantharidin on K562 human myeloid leukaemia cells in vitro
306. Effects of norcantharidin, a protein phosphatase type-2A inhibitor, on the growth of normal and malignant haemopoletIc cells
307. 2-M-phase growth arrest correlates with abnormal centrosome replication, the formation of aberrant mitotic spindles, and the inhibition of serine/threonine protein phosphatase activity
308. Selective solid tumor anticancer activity of cantharidin (Spanish Fly) analogues
309. Enhancement of X-ray cell killing in cultured mammalian cells by the protein phosphatase inhibitor calyculin A
310. Induction of apoptosis in human oral squamous carcinoma cell lines by protein phosphatase inhibitors
311. New apoptosis-inducing agents: Thyrsiferyl 23-acetate, tautomycin and related compounds
312. Norcantharidin-induced post-G(2)/M apoptesis is dependent on wild-type p53 gene
313. Ultrarapid caspase-3 dependent apoptosis induction by serine/threonine phosphatase inhibitors
314. A combination of cyclosporin-A (CsA) and interferon gamma (INF-gamma) induces apoptosis in human gastric carcinoma cells
315. Induction of apoptosis by adenovirus E4orf4 protein
316. Induction of p53-independent apoptosis by the adenovirus E4orf4 protein requires binding to the B alpha subunit of protein phosphatase 2A
317. Protein phosphatase 1 alpha is a Ras-activated Bad phosphatase that regulates interleukin-2 deprivation-induced apoptesis
318. The involvement of protein phosphatases in the activation of ICE/CED-3 protease, intracellular acidification, DNA digestion, and apoptosis
319. High level calcineurin acitivity predisposes neuronal cells to apoptosis
320. Protein phosphatase-1 activation and association with the retinoblastoma protein in colcemid-induced apoptosis
321. Versatility of BCP/ABL-expressing leukemic cells in circumventing proapoptotic BAD effects
322. 2+-induced apoptetic cell death through calcineurin dephosphorylation of BAD
323. Ceramide induces Bcl2 dephosphorylation via a mechanism involving mitechondrial PP2A
324. Inactivation of bcl-2 by phosphorylation
325. Bcl-2 protects against apoptosis-related microtubule alterations in neuronal cells
326. Disruption of the outer mitochondrial membrane as a result of large amplitude swelling: The impact of irreversible permeability transition
327. Thymidylate synthase inhibition induces S-phase arrest, biphasic mitochondrial alterations and caspase dependent apoptosis in leukaemia cells