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In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.

Vaupel A, Holzer P, Ferretti S, Guagnano V, Kallen J, Mah R, Masuya K, Ruetz S, Rynn C, Schlapbach A, Stachyra T, Stutz S, Todorov M, Jeay S, Furet P.

Bioorg Med Chem Lett. 2018 Nov 1;28(20):3404-3408. doi: 10.1016/j.bmcl.2018.08.027. Epub 2018 Aug 26.


The Potential Role of the Dipeptidyl Peptidase-4-Like Activity From the Gut Microbiota on the Host Health.

Olivares M, Schüppel V, Hassan AM, Beaumont M, Neyrinck AM, Bindels LB, Benítez-Páez A, Sanz Y, Haller D, Holzer P, Delzenne NM.

Front Microbiol. 2018 Aug 22;9:1900. doi: 10.3389/fmicb.2018.01900. eCollection 2018.


Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201.

Jeay S, Ferretti S, Holzer P, Fuchs J, Chapeau EA, Wartmann M, Sterker D, Romanet V, Murakami M, Kerr G, Durand EY, Gaulis S, Cortes-Cros M, Ruetz S, Stachyra TM, Kallen J, Furet P, Würthner J, Guerreiro N, Halilovic E, Jullion A, Kauffmann A, Kuriakose E, Wiesmann M, Jensen MR, Hofmann F, Sellers WR.

Cancer Res. 2018 Nov 1;78(21):6257-6267. doi: 10.1158/0008-5472.CAN-18-0338. Epub 2018 Aug 22.


A step ahead: Exploring the gut microbiota in inpatients with bipolar disorder during a depressive episode.

Painold A, Mörkl S, Kashofer K, Halwachs B, Dalkner N, Bengesser S, Birner A, Fellendorf F, Platzer M, Queissner R, Schütze G, Schwarz MJ, Moll N, Holzer P, Holl AK, Kapfhammer HP, Gorkiewicz G, Reininghaus EZ.

Bipolar Disord. 2018 Jul 26. doi: 10.1111/bdi.12682. [Epub ahead of print]


Gut microbiota, dietary intakes and intestinal permeability reflected by serum zonulin in women.

Mörkl S, Lackner S, Meinitzer A, Mangge H, Lehofer M, Halwachs B, Gorkiewicz G, Kashofer K, Painold A, Holl AK, Bengesser SA, Müller W, Holzer P, Holasek SJ.

Eur J Nutr. 2018 Jul 24. doi: 10.1007/s00394-018-1784-0. [Epub ahead of print]


Towards microbiome-informed dietary recommendations for promoting metabolic and mental health: Opinion papers of the MyNewGut project.

Sanz Y, Romaní-Perez M, Benítez-Páez A, Portune KJ, Brigidi P, Rampelli S, Dinan T, Stanton C, Delzenne N, Blachier F, Neyrinck AM, Beaumont M, Olivares M, Holzer P, Günther K, Wolters M, Ahrens W, Claus SP, Campoy C, Murphy R, Sadler C, Fernández L, Kamp JV.

Clin Nutr. 2018 Jul 9. pii: S0261-5614(18)31209-3. doi: 10.1016/j.clnu.2018.07.007. [Epub ahead of print]


Influence of 4-week multi-strain probiotic administration on resting-state functional connectivity in healthy volunteers.

Bagga D, Aigner CS, Reichert JL, Cecchetto C, Fischmeister FPS, Holzer P, Moissl-Eichinger C, Schöpf V.

Eur J Nutr. 2018 May 30. doi: 10.1007/s00394-018-1732-z. [Epub ahead of print]


Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.

Veenstra SJ, Rueeger H, Voegtle M, Lueoend R, Holzer P, Hurth K, Tintelnot-Blomley M, Frederiksen M, Rondeau JM, Jacobson L, Staufenbiel M, Neumann U, Machauer R.

Bioorg Med Chem Lett. 2018 Jul 1;28(12):2195-2200. doi: 10.1016/j.bmcl.2018.05.003. Epub 2018 May 3.


Probiotics drive gut microbiome triggering emotional brain signatures.

Bagga D, Reichert JL, Koschutnig K, Aigner CS, Holzer P, Koskinen K, Moissl-Eichinger C, Schöpf V.

Gut Microbes. 2018 May 3:1-11. doi: 10.1080/19490976.2018.1460015. [Epub ahead of print]


High-fat diet induces depression-like behaviour in mice associated with changes in microbiome, neuropeptide Y, and brain metabolome.

Hassan AM, Mancano G, Kashofer K, Fröhlich EE, Matak A, Mayerhofer R, Reichmann F, Olivares M, Neyrinck AM, Delzenne NM, Claus SP, Holzer P.

Nutr Neurosci. 2018 Apr 26:1-17. doi: 10.1080/1028415X.2018.1465713. [Epub ahead of print]


Gut Microbiota and the Neuroendocrine System.

Farzi A, Fröhlich EE, Holzer P.

Neurotherapeutics. 2018 Jan;15(1):5-22. doi: 10.1007/s13311-017-0600-5. Review.


Visceral Inflammation and Immune Activation Stress the Brain.

Holzer P, Farzi A, Hassan AM, Zenz G, Jačan A, Reichmann F.

Front Immunol. 2017 Nov 22;8:1613. doi: 10.3389/fimmu.2017.01613. eCollection 2017. Review.


Gut microbiota and body composition in anorexia nervosa inpatients in comparison to athletes, overweight, obese, and normal weight controls.

Mörkl S, Lackner S, Müller W, Gorkiewicz G, Kashofer K, Oberascher A, Painold A, Holl A, Holzer P, Meinitzer A, Mangge H, Holasek S.

Int J Eat Disord. 2017 Dec;50(12):1421-1431. doi: 10.1002/eat.22801. Epub 2017 Nov 13.


Discovery of Potent and Selective p53-MDM2 Protein-Protein Interaction Inhibitors as Anticancer Drugs.

Holzer P.

Chimia (Aarau). 2017 Oct 25;71(10):716-721. doi: 10.2533/chimia.2017.716. Review.


Penis Transplantation: First US Experience.

Cetrulo CL Jr, Li K, Salinas HM, Treiser MD, Schol I, Barrisford GW, McGovern FJ, Feldman AS, Grant MT, Tanrikut C, Lee JH, Ehrlichman RJ, Holzer PW, Choy GM, Liu RW, Ng ZY, Lellouch AG, Kurtz JM, Austen WG Jr, Winograd JM, Bojovic B, Eberlin KR, Rosales IA, Colvin RB, Ko DSC.

Ann Surg. 2018 May;267(5):983-988. doi: 10.1097/SLA.0000000000002241.


One-Stage Supramaximal Full-Thickness Wedge Resection of Vascular Lip Anomalies.

De Castro DK, Ng ZY, Holzer PW, Waner M, Cetrulo CL Jr, Fay A.

J Oral Maxillofac Surg. 2017 Nov;75(11):2449-2455. doi: 10.1016/j.joms.2017.03.020. Epub 2017 Mar 22.


Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.

Möbitz H, Machauer R, Holzer P, Vaupel A, Stauffer F, Ragot C, Caravatti G, Scheufler C, Fernandez C, Hommel U, Tiedt R, Beyer KS, Chen C, Zhu H, Gaul C.

ACS Med Chem Lett. 2017 Feb 14;8(3):338-343. doi: 10.1021/acsmedchemlett.6b00519. eCollection 2017 Mar 9.


Differences in psychological and somatic symptom cluster score profiles between subjects with Idiopathic environmental intolerance, major depression and schizophrenia.

Weiss EM, Singewald E, Baldus C, Hofer E, Marksteiner J, Nasrouei S, Ruepp B, Kapfhammer HP, Fitz W, Mai C, Bauer A, Papousek I, Holzer P.

Psychiatry Res. 2017 Mar;249:187-194. doi: 10.1016/j.psychres.2016.12.057. Epub 2017 Jan 5.


Visceral hyperalgesia caused by peptide YY deletion and Y2 receptor antagonism.

Hassan AM, Jain P, Mayerhofer R, Fröhlich EE, Farzi A, Reichmann F, Herzog H, Holzer P.

Sci Rep. 2017 Jan 20;7:40968. doi: 10.1038/srep40968.


Vitamin D deficiency as a risk factor for dementia: a systematic review and meta-analysis.

Sommer I, Griebler U, Kien C, Auer S, Klerings I, Hammer R, Holzer P, Gartlehner G.

BMC Geriatr. 2017 Jan 13;17(1):16. doi: 10.1186/s12877-016-0405-0. Review.


Correction: A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097.

Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D.

Elife. 2016 Nov 17;5. pii: e19317. doi: 10.7554/eLife.19317. No abstract available.


Neuropeptides, Microbiota, and Behavior.

Holzer P.

Int Rev Neurobiol. 2016;131:67-89. doi: 10.1016/bs.irn.2016.08.005. Epub 2016 Sep 14. Review.


Diverse action of lipoteichoic acid and lipopolysaccharide on neuroinflammation, blood-brain barrier disruption, and anxiety in mice.

Mayerhofer R, Fröhlich EE, Reichmann F, Farzi A, Kogelnik N, Fröhlich E, Sattler W, Holzer P.

Brain Behav Immun. 2017 Feb;60:174-187. doi: 10.1016/j.bbi.2016.10.011. Epub 2016 Oct 14.


A Comparative Examination of the Clinical Outcome and Histological Appearance of Cryopreserved and Fresh Split-Thickness Skin Grafts.

Holzer PW, Leonard DA, Shanmugarajah K, Moulton KN, Ng ZY, Cetrulo CL Jr, Sachs DH.

J Burn Care Res. 2017 Jan/Feb;38(1):e55-e61. doi: 10.1097/BCR.0000000000000431.


Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.

Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C.

ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11.


Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.

Furet P, Masuya K, Kallen J, Stachyra-Valat T, Ruetz S, Guagnano V, Holzer P, Mah R, Stutz S, Vaupel A, Chène P, Jeay S, Schlapbach A.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4837-4841. doi: 10.1016/j.bmcl.2016.08.010. Epub 2016 Aug 9.


Inhibition of α2A-Adrenoceptors Ameliorates Dextran Sulfate Sodium-Induced Acute Intestinal Inflammation in Mice.

Zádori ZS, Tóth VE, Fehér Á, Al-Khrasani M, Puskár Z, Kozsurek M, Timár J, Tábi T, Helyes Z, Hein L, Holzer P, Gyires K.

J Pharmacol Exp Ther. 2016 Sep;358(3):483-91. doi: 10.1124/jpet.116.235101. Epub 2016 Jul 14.


Environmental enrichment induces behavioural disturbances in neuropeptide Y knockout mice.

Reichmann F, Wegerer V, Jain P, Mayerhofer R, Hassan AM, Fröhlich EE, Bock E, Pritz E, Herzog H, Holzer P, Leitinger G.

Sci Rep. 2016 Jun 16;6:28182. doi: 10.1038/srep28182.


Cognitive impairment by antibiotic-induced gut dysbiosis: Analysis of gut microbiota-brain communication.

Fröhlich EE, Farzi A, Mayerhofer R, Reichmann F, Jačan A, Wagner B, Zinser E, Bordag N, Magnes C, Fröhlich E, Kashofer K, Gorkiewicz G, Holzer P.

Brain Behav Immun. 2016 Aug;56:140-55. doi: 10.1016/j.bbi.2016.02.020. Epub 2016 Feb 23.


Deletion of Monoglyceride Lipase in Astrocytes Attenuates Lipopolysaccharide-induced Neuroinflammation.

Grabner GF, Eichmann TO, Wagner B, Gao Y, Farzi A, Taschler U, Radner FP, Schweiger M, Lass A, Holzer P, Zinser E, Tschöp MH, Yi CX, Zimmermann R.

J Biol Chem. 2016 Jan 8;291(2):913-23. doi: 10.1074/jbc.M115.683615. Epub 2015 Nov 12.


Neuropeptide Y: A stressful review.

Reichmann F, Holzer P.

Neuropeptides. 2016 Feb;55:99-109. doi: 10.1016/j.npep.2015.09.008. Epub 2015 Sep 30. Review.


Neuroimmune pharmacological approaches.

Holzer P, Hassan AM, Jain P, Reichmann F, Farzi A.

Curr Opin Pharmacol. 2015 Dec;25:13-22. doi: 10.1016/j.coph.2015.09.003. Epub 2015 Sep 29. Review.


Behavioral and molecular processing of visceral pain in the brain of mice: impact of colitis and psychological stress.

Jain P, Hassan AM, Koyani CN, Mayerhofer R, Reichmann F, Farzi A, Schuligoi R, Malle E, Holzer P.

Front Behav Neurosci. 2015 Jul 10;9:177. doi: 10.3389/fnbeh.2015.00177. eCollection 2015.


Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.

Holzer P, Masuya K, Furet P, Kallen J, Valat-Stachyra T, Ferretti S, Berghausen J, Bouisset-Leonard M, Buschmann N, Pissot-Soldermann C, Rynn C, Ruetz S, Stutz S, Chène P, Jeay S, Gessier F.

J Med Chem. 2015 Aug 27;58(16):6348-58. doi: 10.1021/acs.jmedchem.5b00810. Epub 2015 Aug 5.


Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53-MDM2 interaction with a distinct binding mode.

Gessier F, Kallen J, Jacoby E, Chène P, Stachyra-Valat T, Ruetz S, Jeay S, Holzer P, Masuya K, Furet P.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3621-5. doi: 10.1016/j.bmcl.2015.06.058. Epub 2015 Jun 23.


Dextran sulfate sodium-induced colitis alters stress-associated behaviour and neuropeptide gene expression in the amygdala-hippocampus network of mice.

Reichmann F, Hassan AM, Farzi A, Jain P, Schuligoi R, Holzer P.

Sci Rep. 2015 Jun 12;5:9970. doi: 10.1038/srep09970.


A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097.

Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D.

Elife. 2015 May 12;4. pii: e06498. doi: 10.7554/eLife.06498. Erratum in: Elife. 2016 Nov 17;5:null.


Toll-like receptor 4 contributes to the inhibitory effect of morphine on colonic motility in vitro and in vivo.

Farzi A, Halicka J, Mayerhofer R, Fröhlich EE, Tatzl E, Holzer P.

Sci Rep. 2015 Mar 26;5:9499. doi: 10.1038/srep09499.


Reevaluating the hype: four bacterial metabolites under scrutiny.

Fröhlich EE, Mayerhofer R, Holzer P.

Eur J Microbiol Immunol (Bp). 2015 Mar;5(1):1-13. doi: 10.1556/EUJMI-D-14-00030. Epub 2015 Mar 26. Review.


Acid-sensing ion channels in gastrointestinal function.

Holzer P.

Neuropharmacology. 2015 Jul;94:72-9. doi: 10.1016/j.neuropharm.2014.12.009. Epub 2015 Jan 9. Review.


The homeostatic role of neuropeptide Y in immune function and its impact on mood and behaviour.

Farzi A, Reichmann F, Holzer P.

Acta Physiol (Oxf). 2015 Mar;213(3):603-27. doi: 10.1111/apha.12445. Epub 2015 Jan 9. Review.


A novel unbiased counting method for the quantification of synapses in the mouse brain.

Reichmann F, Painsipp E, Holzer P, Kummer D, Bock E, Leitinger G.

J Neurosci Methods. 2015 Jan 30;240:13-21. doi: 10.1016/j.jneumeth.2014.10.020. Epub 2014 Nov 3.


Repeated predictable stress causes resilience against colitis-induced behavioral changes in mice.

Hassan AM, Jain P, Reichmann F, Mayerhofer R, Farzi A, Schuligoi R, Holzer P.

Front Behav Neurosci. 2014 Nov 6;8:386. doi: 10.3389/fnbeh.2014.00386. eCollection 2014.


Synergistic effects of NOD1 or NOD2 and TLR4 activation on mouse sickness behavior in relation to immune and brain activity markers.

Farzi A, Reichmann F, Meinitzer A, Mayerhofer R, Jain P, Hassan AM, Fröhlich EE, Wagner K, Painsipp E, Rinner B, Holzer P.

Brain Behav Immun. 2015 Feb;44:106-20. doi: 10.1016/j.bbi.2014.08.011. Epub 2014 Sep 11.


Naloxegol increases frequency of bowel movements and combats inadequate response to laxatives.

Holzer P.

Evid Based Med. 2015 Feb;20(1):5. doi: 10.1136/ebmed-2014-110071. Epub 2014 Sep 10. No abstract available.


Neuropeptides and the microbiota-gut-brain axis.

Holzer P, Farzi A.

Adv Exp Med Biol. 2014;817:195-219. doi: 10.1007/978-1-4939-0897-4_9. Review.


GAL3 receptor KO mice exhibit an anxiety-like phenotype.

Brunner SM, Farzi A, Locker F, Holub BS, Drexel M, Reichmann F, Lang AA, Mayr JA, Vilches JJ, Navarro X, Lang R, Sperk G, Holzer P, Kofler B.

Proc Natl Acad Sci U S A. 2014 May 13;111(19):7138-43. doi: 10.1073/pnas.1318066111. Epub 2014 Apr 29.


The pharmacology of TRP channels.

Holzer P, Izzo AA.

Br J Pharmacol. 2014 May;171(10):2469-73. doi: 10.1111/bph.12723.


SPLIT rectus abdominis myocutaneous double free flap for extremity reconstruction.

Nyame TT, Holzer PW, Helm DL, Maman DY, Winograd JM, Cetrulo CL Jr.

Microsurgery. 2014 Jan;34(1):54-7. doi: 10.1002/micr.22160. Epub 2013 Oct 7.


Combined soliton pulse compression and plasma-related frequency upconversion in gas-filled photonic crystal fiber.

Chang W, Hölzer P, Travers JC, Russell PS.

Opt Lett. 2013 Aug 15;38(16):2984-7. doi: 10.1364/OL.38.002984.


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