resorcinols

Summary

Summary: A water-soluble crystalline benzene-1,3-diol (resorcinol) and its derivatives.

Top Publications

  1. Rimando A, Dayan F, Streibig J. PSII inhibitory activity of resorcinolic lipids from Sorghum bicolor. J Nat Prod. 2003;66:42-5 pubmed
    ..20 microM, respectively). Compound 4 could not be enzymatically converted to a quinone, suggesting that the quinone moiety is not required for its photosystem II inhibitory activity. Compounds 5 and 6 are reported for the first time. ..
  2. Mo F, Offertaler L, Kunos G. Atypical cannabinoid stimulates endothelial cell migration via a Gi/Go-coupled receptor distinct from CB1, CB2 or EDG-1. Eur J Pharmacol. 2004;489:21-7 pubmed
    ..These results indicate that an abn-cbd-sensitive endothelial receptor distinct from cannabinoid CB1, CB2 or EDG-1 receptors mediates not only vasorelaxation but also endothelial cell migration. ..
  3. Knödler M, Conrad J, Wenzig E, Bauer R, Lacorn M, Beifuss U, et al. Anti-inflammatory 5-(11'Z-heptadecenyl)- and 5-(8'Z,11'Z-heptadecadienyl)-resorcinols from mango (Mangifera indica L.) peels. Phytochemistry. 2008;69:988-93 pubmed
  4. Kubo I, Nitoda T, Tocoli F, Green I. Multifunctional cytotoxic agents from Anacardium occidentale. Phytother Res. 2011;25:38-45 pubmed publisher
    ..Both anacardic acids and cardols exhibited moderate cytotoxicity. ..
  5. Landberg R, Kamal Eldin A, Aman P, Christensen J, Overvad K, Tjønneland A, et al. Determinants of plasma alkylresorcinol concentration in Danish post-menopausal women. Eur J Clin Nutr. 2011;65:94-101 pubmed publisher
    ..05), but only ?2% of the total plasma AR concentration was explained by the dietary fiber or cereal fiber intake. In the studied population, AR plasma concentration was mainly affected by rye bread intake among investigated determinants. ..
  6. Patro B, Tyagi M, Saha J, Chattopadhyay S. Comparative nuclease and anti-cancer properties of the naturally occurring malabaricones. Bioorg Med Chem. 2010;18:7043-51 pubmed publisher
    ..26±1.20 ?M) than curcumin (IC(50)=24.46±3.32 ?M) against the MCF-7 human breast cancer cell line. The mal C-induced killing of the MCF-7 cells followed an apoptotic pathway involving oxidative damage to the cellular DNA. ..
  7. Kristensen M, Toubro S, Jensen M, Ross A, Riboldi G, Petronio M, et al. Whole grain compared with refined wheat decreases the percentage of body fat following a 12-week, energy-restricted dietary intervention in postmenopausal women. J Nutr. 2012;142:710-6 pubmed publisher
    ..Serum total and LDL cholesterol, two important risk factors of cardiovascular disease, increased with RW but not WW consumption, which may suggest a cardioprotective role for whole grain. ..
  8. Centenera M, Gillis J, Hanson A, Jindal S, Taylor R, Risbridger G, et al. Evidence for efficacy of new Hsp90 inhibitors revealed by ex vivo culture of human prostate tumors. Clin Cancer Res. 2012;18:3562-70 pubmed publisher
    ..This approach, therefore, has the potential to enable more rational selection of therapeutic agents and biomarkers of response for clinical trials. ..
  9. Montonen J, Landberg R, Kamal Eldin A, Aman P, Knueppel S, Boeing H, et al. Reliability of fasting plasma alkylresorcinol concentrations measured 4 months apart. Eur J Clin Nutr. 2010;64:698-703 pubmed publisher
    ..These findings should be taken into account when using AR as blood biomarkers for whole-grain intake in large-scale epidemiologic studies. ..

More Information

Publications65

  1. Stingl L, Stühmer T, Chatterjee M, Jensen M, Flentje M, Djuzenova C. Novel HSP90 inhibitors, NVP-AUY922 and NVP-BEP800, radiosensitise tumour cells through cell-cycle impairment, increased DNA damage and repair protraction. Br J Cancer. 2010;102:1578-91 pubmed publisher
    ..The results might have important implications for the radiotherapy of solid tumours. ..
  2. Massey A, Schoepfer J, Brough P, Brueggen J, Chene P, Drysdale M, et al. Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800. Mol Cancer Ther. 2010;9:906-19 pubmed publisher
    ..Mol Cancer Ther; 9(4); 906-19. (c)2010 AACR. ..
  3. Cheung F, Li C, Che C, Liu B, Wang L, Liu W. Geoditin A induces oxidative stress and apoptosis on human colon HT29 cells. Mar Drugs. 2010;8:80-90 pubmed publisher
    ..Our results provide a better understanding of the apoptotic properties and chemotherapeutical potential of this marine triterpene. ..
  4. Andersson A, Marklund M, Diana M, Landberg R. Plasma alkylresorcinol concentrations correlate with whole grain wheat and rye intake and show moderate reproducibility over a 2- to 3-month period in free-living Swedish adults. J Nutr. 2011;141:1712-8 pubmed publisher
    ..05) when using mean values from both occasions. This suggests that plasma AR concentration in fasting samples can be used as a biomarker of rye + wheat WG intake in free-living populations with a high and consistent WG intake. ..
  5. Landberg R, Aman P, Hallmans G, Johansson I. Long-term reproducibility of plasma alkylresorcinols as biomarkers of whole-grain wheat and rye intake within Northern Sweden Health and Disease Study Cohort. Eur J Clin Nutr. 2013;67:259-63 pubmed publisher
    ..The objective was therefore to estimate the reproducibility of plasma AR concentrations over 0.1-3.9 years...
  6. Jeong S, Lee J, Jeong N, Kim T, Yoo K, Song S, et al. A novel resveratrol analogue HS-1793 treatment overcomes the resistance conferred by Bcl-2 and is associated with the formation of mature PML nuclear bodies in renal clear cell carcinoma Caki-1 cells. Int J Oncol. 2009;35:1353-60 pubmed
    ..Our findings show that the resveratrol analogue HS-1793 might provide a novel promising strategy for overcoming the resistance conferred by Bcl-2 via PML protein and the formation of mature PML-NBs. ..
  7. Oude Munnink T, Korte M, Nagengast W, Timmer Bosscha H, Schröder C, Jong J, et al. (89)Zr-trastuzumab PET visualises HER2 downregulation by the HSP90 inhibitor NVP-AUY922 in a human tumour xenograft. Eur J Cancer. 2010;46:678-84 pubmed publisher
    ..This technique is currently under clinical evaluation and might serve as an early biomarker for HSP90 inhibition in HER2 positive metastatic breast cancer patients. ..
  8. Gaspar N, Sharp S, Eccles S, Gowan S, Popov S, Jones C, et al. Mechanistic evaluation of the novel HSP90 inhibitor NVP-AUY922 in adult and pediatric glioblastoma. Mol Cancer Ther. 2010;9:1219-33 pubmed publisher
  9. Kovacic P, Somanathan R. Cell signaling and receptors with resorcinols and flavonoids: redox, reactive oxygen species, and physiological effects. J Recept Signal Transduct Res. 2011;31:265-70 pubmed publisher
    ..However, the resorcinol class has received less attention. This review deals with resorcinols and flavonoids...
  10. Kim J, Song B, Hong I, Kim J, Lee J, Park S, et al. Reactivation of fear memory renders consolidated amygdala synapses labile. J Neurosci. 2010;30:9631-40 pubmed publisher
    ..Our findings suggest that, upon memory reactivation, consolidated T-LA synapses enter a temporary labile state, displaying insensitivity to mGluRI-depotentiation. ..
  11. Porter J, Fritz C, Depew K. Discovery and development of Hsp90 inhibitors: a promising pathway for cancer therapy. Curr Opin Chem Biol. 2010;14:412-20 pubmed publisher
    ..The most advanced candidates are now in Phase 2 clinical trials and defining the therapeutic window, dosing schedule, and indication are the primary challenges for these potential first-in-class inhibitors. ..
  12. Moult P, Schnabel R, Kilpatrick I, Bashir Z, Collingridge G. Tyrosine dephosphorylation underlies DHPG-induced LTD. Neuropharmacology. 2002;43:175-80 pubmed
    ..These data suggest that DHPG-induced LTD involves activation of a protein tyrosine phosphatase. ..
  13. Ross A, Kochhar S. Rapid and sensitive analysis of alkylresorcinols from cereal grains and products using HPLC-Coularray-based electrochemical detection. J Agric Food Chem. 2009;57:5187-93 pubmed publisher
    ..This method allows rapid throughput analysis of cereal samples, required for validation studies on the use of AR as biomarkers of wholegrain cereal intake. ..
  14. Jensen M, Schoepfer J, Radimerski T, Massey A, Guy C, Brueggen J, et al. NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models. Breast Cancer Res. 2008;10:R33 pubmed publisher
    ..On the basis of its mechanism of action, preclinical activity profile, tolerability, and pharmaceutical properties, the compound recently has entered clinical phase I breast cancer trials. ..
  15. Wiśniewski K, Car H. (S)-3,5-DHPG: a review. CNS Drug Rev. 2002;8:101-16 pubmed
    ..S)-3,5-DHPG may be useful as a cognitive enhancing agent in memory impairment associated with ischemia or hypoxia. Recent investigations suggested possible beneficial effects of (S)-3,5-DHPG in Alzheimer's disease. ..
  16. Taura F, Tanaka S, Taguchi C, Fukamizu T, Tanaka H, Shoyama Y, et al. Characterization of olivetol synthase, a polyketide synthase putatively involved in cannabinoid biosynthetic pathway. FEBS Lett. 2009;583:2061-6 pubmed publisher
    ..The possibility that OLS could be involved in OLA biosynthesis was discussed based on its catalytic properties and expression profile. ..
  17. Patro B, Bauri A, Mishra S, Chattopadhyay S. Antioxidant activity of Myristica malabarica extracts and their constituents. J Agric Food Chem. 2005;53:6912-8 pubmed
    ..The radioprotective activity was found to correlate with its (*)OH radical scavenging property, which matched well with that of d-mannitol...
  18. Zhang W, Che C. Isomalabaricane-type nortriterpenoids and other constituents of the marine sponge Geodia japonica. J Nat Prod. 2001;64:1489-92 pubmed
    ..All chemical structures were established by interpretation of the spectroscopic data. ..
  19. Mannaioni G, Marino M, Valenti O, Traynelis S, Conn P. Metabotropic glutamate receptors 1 and 5 differentially regulate CA1 pyramidal cell function. J Neurosci. 2001;21:5925-34 pubmed
    ..These data suggest that mGluR1 and mGluR5 play distinct roles in the regulation of the excitability of hippocampal CA1 pyramidal neurons. ..
  20. Brough P, Aherne W, Barril X, Borgognoni J, Boxall K, Cansfield J, et al. 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. J Med Chem. 2008;51:196-218 pubmed
    ..Compound 40f is retained in tumors in vivo when administered i.p., as evaluated by cassette dosing in tumor-bearing mice. In a human colon cancer xenograft model, 40f inhibits tumor growth by approximately 50%. ..
  21. Landberg R, Kamal Eldin A, Andersson S, Johansson J, Zhang J, Hallmans G, et al. Reproducibility of plasma alkylresorcinols during a 6-week rye intervention study in men with prostate cancer. J Nutr. 2009;139:975-80 pubmed publisher
    ..This suggests that the plasma AR concentration can be used as a reliable short- to medium-term biomarker for whole-grain wheat and rye under intervention conditions where intake is kept constant. ..
  22. Bellafiore S, Shen Z, Rosso M, Abad P, Shih P, Briggs S. Direct identification of the Meloidogyne incognita secretome reveals proteins with host cell reprogramming potential. PLoS Pathog. 2008;4:e1000192 pubmed publisher
    ..incognita secretome overlaps the reported secretome of mammalian parasitic nematodes (e.g., Brugia malayi), suggesting a common parasitic behavior and a possible conservation of function between metazoan parasites of plants and animals. ..
  23. Camon L, Vives P, de Vera N, Martinez E. Seizures and neuronal damage induced in the rat by activation of group I metabotropic glutamate receptors with their selective agonist 3,5-dihydroxyphenylglycine. J Neurosci Res. 1998;51:339-48 pubmed
  24. Palmer M, Irving A, Seabrook G, Jane D, Collingridge G. The group I mGlu receptor agonist DHPG induces a novel form of LTD in the CA1 region of the hippocampus. Neuropharmacology. 1997;36:1517-32 pubmed
    ..These data show that activation of group I mGlu receptors (probably mGlu5) can induce LTD and that this mGlu receptor-mediated LTD may, or may not, require activation of NMDA receptors, depending on the experimental conditions. ..
  25. Dayan F, Kagan I, Rimando A. Elucidation of the biosynthetic pathway of the allelochemical sorgoleone using retrobiosynthetic NMR analysis. J Biol Chem. 2003;278:28607-11 pubmed
    ..The lipid resorcinol intermediate is then methylated by a S-adenosylmethionine-dependent O-methyltransferase and subsequently dihydroxylated by a P450 monooxygenase to yield the reduced form of sorgoleone. ..
  26. Ross A, Kamal Eldin A, Lundin E, Zhang J, Hallmans G, Aman P. Cereal alkylresorcinols are absorbed by humans. J Nutr. 2003;133:2222-4 pubmed
    ..AR absorbed by humans may be of importance as bioactive compounds, or as a biomarker of whole grain wheat and rye intake. ..
  27. Dayan F, Watson S, Nanayakkara N. Biosynthesis of lipid resorcinols and benzoquinones in isolated secretory plant root hairs. J Exp Bot. 2007;58:3263-72 pubmed
    ..The activity of the key enzymes involved in the biosynthesis of lipid resorcinols and benzoquinones was measured directly in isolated root hair preparations obtained from 6-d-old roots...
  28. Jaubert S, Ledger T, Laffaire J, Piotte C, Abad P, Rosso M. Direct identification of stylet secreted proteins from root-knot nematodes by a proteomic approach. Mol Biochem Parasitol. 2002;121:205-11 pubmed
    ..The potential roles of this secreted protein in pathogenesis and the advantages of developing this strategy to obtain new insights into plant-nematode interactions are discussed. ..
  29. Franklin A, Stella N. Arachidonylcyclopropylamide increases microglial cell migration through cannabinoid CB2 and abnormal-cannabidiol-sensitive receptors. Eur J Pharmacol. 2003;474:195-8 pubmed
    ..Our results suggest that cannabinoid CB(2) receptors and abn-CBD receptors, rather than cannabinoid CB(1) receptors, regulate microglial cell migration, and that ACPA is a broad cannabinoid receptor agonist. ..
  30. Trevisan M, Pfundstein B, Haubner R, Wurtele G, Spiegelhalder B, Bartsch H, et al. Characterization of alkyl phenols in cashew (Anacardium occidentale) products and assay of their antioxidant capacity. Food Chem Toxicol. 2006;44:188-97 pubmed
  31. Jeong S, Jo W, Song S, Suh H, Seol S, Leem S, et al. A novel resveratrol derivative, HS1793, overcomes the resistance conferred by Bcl-2 in human leukemic U937 cells. Biochem Pharmacol. 2009;77:1337-47 pubmed publisher
    ..Further understanding exactly how HS-1793 overcomes the resistance conferred by Bcl-2 via 14-3-3 may guide the development of future anticancer agents. ..
  32. Landberg R, Man P, Kamal Eldin A. A rapid gas chromatography-mass spectrometry method for quantification of alkylresorcinols in human plasma. Anal Biochem. 2009;385:7-12 pubmed publisher
    ..Approximately 30 to 50 samples could be analyzed within 1 day. The improved GC-MS method presented can be used for rapid analysis of ARs in relatively small sample volumes. ..
  33. Huang Y, Zhao K, Shen X, Chaudhry M, Jiang C, Liu S. Genetic characterization of the resorcinol catabolic pathway in Corynebacterium glutamicum. Appl Environ Microbiol. 2006;72:7238-45 pubmed
    ..NCgl2953 encoded a putative transporter, but disruption of this gene did not affect resorcinol degradation by C. glutamicum. The function of NCgl2953 remains unclear. ..
  34. Fitzjohn S, Bortolotto Z, Palmer M, Doherty A, Ornstein P, Schoepp D, et al. The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology. 1998;37:1445-58 pubmed
    ..Since in the same inputs these forms of LTP were blocked by (S)-MCPG, a novel type of mGlu receptor may be involved in their induction. ..
  35. Huber K, Roder J, Bear M. Chemical induction of mGluR5- and protein synthesis--dependent long-term depression in hippocampal area CA1. J Neurophysiol. 2001;86:321-5 pubmed
    ..DHPG-LTD should be useful for biochemical analysis of mGluR5- and protein synthesis-dependent synaptic modification...
  36. Nadlewska A, Car H, Oksztel R, Wiśniewski K. Effect of (S)-3,5-DHPG on learning, exploratory activity and anxiety in rats with experimental hypoxia. Pol J Pharmacol. 2002;54:11-8 pubmed
    ..In rats subjected to hypoxia, (S)-3,5-DHPG, the agonist of I mGluRs, improved consolidation and retrieval and exhibited anxiolytic activity in dose-dependent manner. ..
  37. Liu W, Ho J, Che C. Apoptotic activity of isomalabaricane triterpenes on human promyelocytic leukemia HL60 cells. Cancer Lett. 2005;230:102-10 pubmed
    ..Taken together our results suggest that geoditin A markedly induced reactive oxygen species, decreased mitochondrial membrane potential and mediated a caspases 3 apoptosis pathway...
  38. Ross A, Shepherd M, Schüpphaus M, Sinclair V, Alfaro B, Kamal Eldin A, et al. Alkylresorcinols in cereals and cereal products. J Agric Food Chem. 2003;51:4111-8 pubmed
    ..Cereal products varied greatly in AR content, with those containing wheat bran or whole rye having the highest content. ..
  39. Landberg R, Kamal Eldin A, Andersson R, Aman P. Alkylresorcinol content and homologue composition in durum wheat (Triticum durum) kernels and pasta products. J Agric Food Chem. 2006;54:3012-4 pubmed
    ..The ratio of the homologues C17:0 to C21:0 was < or =0.02 for whole grain durum wheat products, which is different from those of common wheat (0.1) and rye (0.9). ..
  40. Stühmer T, Zollinger A, Siegmund D, Chatterjee M, Grella E, Knop S, et al. Signalling profile and antitumour activity of the novel Hsp90 inhibitor NVP-AUY922 in multiple myeloma. Leukemia. 2008;22:1604-12 pubmed publisher
    ..Thus, NVP-AUY922 may be a promising drug for treatment of MM and clinical studies are warranted. ..
  41. Suzuki Y, Kurano M, Esumi Y, Yamaguchi I, Doi Y. Biosynthesis of 5-alkylresorcinol in rice: incorporation of a putative fatty acid unit in the 5-alkylresorcinol carbon chain. Bioorg Chem. 2003;31:437-52 pubmed
    ..These results obviously show that the fatty acid unit acts as a direct precursor and forms the side-chain moiety of 5-n-alkylresorcinol via the predicted biosynthesis pathway. ..
  42. Ross A, Pineau N, Kochhar S, Bourgeois A, Beaumont M, Decarli B. Validation of a FFQ for estimating whole-grain cereal food intake. Br J Nutr. 2009;102:1547-51 pubmed publisher
    ..72, 0.81 and 0.57, respectively). Adjustment for age, sex, BMI and total energy intake did not affect the results. This FFQ appears to give a rapid and adequate estimate of WG cereal intake in free-living subjects. ..
  43. Przeworska E, Gubernator J, Kozubek A. Formation of liposomes by resorcinolic lipids, single-chain phenolic amphiphiles from Anacardium occidentale L. Biochim Biophys Acta. 2001;1513:75-81 pubmed
    ..The retention of the captured solute depends upon the type of resorcinolic lipid and on the temperature, but in general, is lower than control phospholipid liposomes. ..
  44. Johnson M, Chamberlain M, Kelly G. Phosphoinositide hydrolysis in vivo with group I metabotropic glutamate receptor agonists. Brain Res. 1999;821:539-45 pubmed
    ..This method could be quite useful in determining the doses and routes of administration of agonists and antagonists that are required to interact with group I mGluRs. ..
  45. Hou L, Klann E. Activation of the phosphoinositide 3-kinase-Akt-mammalian target of rapamycin signaling pathway is required for metabotropic glutamate receptor-dependent long-term depression. J Neurosci. 2004;24:6352-61 pubmed
    ..Together, our findings indicate that activation of the PI3K-Akt-mTOR signaling cascade is required for mGluR-LTD and suggest that this pathway may couple group I mGluRs to translation initiation in hippocampal area CA1. ..
  46. Eccles S, Massey A, Raynaud F, Sharp S, Box G, Valenti M, et al. NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis. Cancer Res. 2008;68:2850-60 pubmed publisher
    ..NVP-AUY922 has entered phase I clinical trials. ..
  47. van Dam R, Hu F. Are alkylresorcinols accurate biomarkers for whole grain intake?. Am J Clin Nutr. 2008;87:797-8 pubmed
  48. Banerjee D, Bauri A, Guha R, Bandyopadhyay S, Chattopadhyay S. Healing properties of malabaricone B and malabaricone C, against indomethacin-induced gastric ulceration and mechanism of action. Eur J Pharmacol. 2008;578:300-12 pubmed
  49. Funa N, Awakawa T, Horinouchi S. Pentaketide resorcylic acid synthesis by type III polyketide synthase from Neurospora crassa. J Biol Chem. 2007;282:14476-81 pubmed
    ..ORAS is the first type III PKS that synthesizes pentaketide resorcylic acids. ..
  50. Funa N, Ozawa H, Hirata A, Horinouchi S. Phenolic lipid synthesis by type III polyketide synthases is essential for cyst formation in Azotobacter vinelandii. Proc Natl Acad Sci U S A. 2006;103:6356-61 pubmed
  51. Holt M, Moreau R, DerMarderosian A, McKeown N, Jacques P. Accelerated solvent extraction of alkylresorcinols in food products containing uncooked and cooked wheat. J Agric Food Chem. 2012;60:4799-802 pubmed publisher
    ..Furthermore, the extraction time for ASE (approximately 40 min) is much more convenient and less tedious and time-consuming than previously established methods, which range from 5 h for processed foods to 24 h for raw grains. ..
  52. Pochorovski I, Ebert M, Gisselbrecht J, Boudon C, Schweizer W, Diederich F. Redox-switchable resorcin[4]arene cavitands: molecular grippers. J Am Chem Soc. 2012;134:14702-5 pubmed publisher
    ..The intramolecular H-bonds were characterized using X-ray, IR, and NMR spectroscopies. Guests were bound in the closed, reduced state and fully released in the open, oxidized state. ..
  53. Mann T, Scherner C, Röhm K, Kolbe L. Structure-Activity Relationships of Thiazolyl Resorcinols, Potent and Selective Inhibitors of Human Tyrosinase. Int J Mol Sci. 2018;19: pubmed publisher
    ..Recently, we reported that thiazolyl resorcinols (4-resorcinylthiazol-2-amines and -amides) are both selective and efficacious inhibitors of hTyr in vitro and ..
  54. Yamamoto K, Hirota K, Kono K, Takeda S, Sakamuru S, Xia M, et al. Characterization of environmental chemicals with potential for DNA damage using isogenic DNA repair-deficient chicken DT40 cell lines. Environ Mol Mutagen. 2011;52:547-61 pubmed publisher
    ..The results demonstrate the utility of this DT40 screen for detecting genotoxic compounds, for characterizing the nature of the DNA damage, and potentially for analyzing mechanisms of mutagenesis. ..
  55. Arizono M, Bannai H, Nakamura K, Niwa F, Enomoto M, Matsu ura T, et al. Receptor-selective diffusion barrier enhances sensitivity of astrocytic processes to metabotropic glutamate receptor stimulation. Sci Signal. 2012;5:ra27 pubmed publisher
  56. Wainberg Z, Anghel A, Rogers A, Desai A, Kalous O, Conklin D, et al. Inhibition of HSP90 with AUY922 induces synergy in HER2-amplified trastuzumab-resistant breast and gastric cancer. Mol Cancer Ther. 2013;12:509-19 pubmed publisher
    ..The combination of HSP90 inhibition and direct HER2 blockade represents a novel approach to the treatment of HER2-amplified cancers and clinical trials based on the above data are ongoing. ..