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Items: 1 to 20 of 172

1.

Preclinical Evaluation of Benzazepine-Based PET Radioligands (R)- and (S)-11C-Me-NB1 Reveals Distinct Enantiomeric Binding Patterns and Tightrope Walk between GluN2B- and Sigma1 Receptor-Targeted PET Imaging.

Haider A, Müller Herder A, Krämer SD, Varisco J, Keller C, Frauenknecht K, Auberson YP, Temme L, Robaa D, Sippl W, Schibli R, Wünsch B, Mu L, Ametamey SM.

J Nucl Med. 2019 Jan 25. pii: jnumed.118.221051. doi: 10.2967/jnumed.118.221051. [Epub ahead of print]

PMID:
30683765
2.

Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.

Vögerl K, Ong N, Senger J, Herp D, Schmidtkunz K, Marek M, Müller M, Bartel K, Shaik TB, Porter NJ, Robaa D, Christianson DW, Romier C, Sippl W, Jung M, Bracher F.

J Med Chem. 2019 Feb 1. doi: 10.1021/acs.jmedchem.8b01090. [Epub ahead of print]

PMID:
30645113
3.

Ursolic and oleanolic acid derivatives with cholinesterase inhibiting potential.

Loesche A, Köwitsch A, Lucas SD, Al-Halabi Z, Sippl W, Al-Harrasi A, Csuk R.

Bioorg Chem. 2018 Dec 15;85:23-32. doi: 10.1016/j.bioorg.2018.12.013. [Epub ahead of print]

PMID:
30599410
4.

Selective agonist of TRPML2 reveals direct role in chemokine release from innate immune cells.

Plesch E, Chen CC, Butz E, Scotto Rosato A, Krogsaeter EK, Yinan H, Bartel K, Keller M, Robaa D, Teupser D, Holdt LM, Vollmar AM, Sippl W, Puertollano R, Medina D, Biel M, Wahl-Schott C, Bracher F, Grimm C.

Elife. 2018 Nov 27;7. pii: e39720. doi: 10.7554/eLife.39720.

5.

Computer-aided design, synthesis and biological characterization of novel inhibitors for PKMYT1.

Najjar A, Platzer C, Luft A, Aßmann CA, Elghazawy NH, Erdmann F, Sippl W, Schmidt M.

Eur J Med Chem. 2019 Jan 1;161:479-492. doi: 10.1016/j.ejmech.2018.10.050. Epub 2018 Oct 24.

PMID:
30388464
6.

Characterization of Histone Deacetylase 8 (HDAC8) Selective Inhibition Reveals Specific Active Site Structural and Functional Determinants.

Marek M, Shaik TB, Heimburg T, Chakrabarti A, Lancelot J, Ramos-Morales E, Da Veiga C, Kalinin D, Melesina J, Robaa D, Schmidtkunz K, Suzuki T, Holl R, Ennifar E, Pierce RJ, Jung M, Sippl W, Romier C.

J Med Chem. 2018 Nov 21;61(22):10000-10016. doi: 10.1021/acs.jmedchem.8b01087. Epub 2018 Nov 8.

PMID:
30347148
7.

Unexpected AChE inhibitory activity of (2E)α,β-unsaturated fatty acids.

Loesche A, Wiemann J, Al Halabi Z, Karasch J, Sippl W, Csuk R.

Bioorg Med Chem Lett. 2018 Nov 1;28(20):3315-3319. doi: 10.1016/j.bmcl.2018.09.013. Epub 2018 Sep 11.

PMID:
30220607
8.

Novel Protein Kinase Inhibitors Related to Tau Pathology Modulate Tau Protein-Self Interaction Using a Luciferase Complementation Assay.

Holzer M, Schade N, Opitz A, Hilbrich I, Stieler J, Vogel T, Neukel V, Oberstadt M, Totzke F, Schächtele C, Sippl W, Hilgeroth A.

Molecules. 2018 Sep 12;23(9). pii: E2335. doi: 10.3390/molecules23092335.

9.

Elastin is heterogeneously cross-linked.

Schräder CU, Heinz A, Majovsky P, Karaman Mayack B, Brinckmann J, Sippl W, Schmelzer CEH.

J Biol Chem. 2018 Sep 28;293(39):15107-15119. doi: 10.1074/jbc.RA118.004322. Epub 2018 Aug 14.

PMID:
30108173
10.

Design of selective histone deacetylase inhibitors: rethinking classical pharmacophore.

Melesina J, Praetorius L, Simoben CV, Robaa D, Sippl W.

Future Med Chem. 2018 Jul 1;10(13):1537-1540. doi: 10.4155/fmc-2018-0125. Epub 2018 Jul 3.

PMID:
29966452
11.

The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines.

Kolbinger FR, Koeneke E, Ridinger J, Heimburg T, Müller M, Bayer T, Sippl W, Jung M, Gunkel N, Miller AK, Westermann F, Witt O, Oehme I.

Arch Toxicol. 2018 Aug;92(8):2649-2664. doi: 10.1007/s00204-018-2234-8. Epub 2018 Jun 9.

12.

Identification of PKMYT1 inhibitors by screening the GSK published protein kinase inhibitor set I and II.

Platzer C, Najjar A, Rohe A, Erdmann F, Sippl W, Schmidt M.

Bioorg Med Chem. 2018 Aug 7;26(14):4014-4024. doi: 10.1016/j.bmc.2018.06.027. Epub 2018 Jun 20.

PMID:
29941193
13.

Pharmacogenetic Aspects of the Interaction of AT1 Receptor Antagonists With ATP-Binding Cassette Transporter ABCG2.

Ripperger A, Krischer A, Robaa D, Sippl W, Benndorf RA.

Front Pharmacol. 2018 May 14;9:463. doi: 10.3389/fphar.2018.00463. eCollection 2018.

14.

Computational Drug Repurposing: Current Trends.

Karaman B, Sippl W.

Curr Med Chem. 2018 May 29. doi: 10.2174/0929867325666180530100332. [Epub ahead of print]

PMID:
29848268
15.

Synthesis, Crystallization Studies, and in vitro Characterization of Cinnamic Acid Derivatives as SmHDAC8 Inhibitors for the Treatment of Schistosomiasis.

Bayer T, Chakrabarti A, Lancelot J, Shaik TB, Hausmann K, Melesina J, Schmidtkunz K, Marek M, Erdmann F, Schmidt M, Robaa D, Romier C, Pierce RJ, Jung M, Sippl W.

ChemMedChem. 2018 Aug 10;13(15):1517-1529. doi: 10.1002/cmdc.201800238. Epub 2018 Jul 4.

PMID:
29806110
16.

Compounds from African Medicinal Plants with Activities Against Selected Parasitic Diseases: Schistosomiasis, Trypanosomiasis and Leishmaniasis.

Simoben CV, Ntie-Kang F, Akone SH, Sippl W.

Nat Prod Bioprospect. 2018 Jun;8(3):151-169. doi: 10.1007/s13659-018-0165-y. Epub 2018 May 9. Review.

17.

Isoform-selective HDAC1/6/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity.

Lecointre B, Narozny R, Borrello MT, Senger J, Chakrabarti A, Jung M, Marek M, Romier C, Melesina J, Sippl W, Bischoff L, Ganesan A.

Philos Trans R Soc Lond B Biol Sci. 2018 Jun 5;373(1748). pii: 20170364. doi: 10.1098/rstb.2017.0364.

PMID:
29685969
18.

New chemical tools for probing activity and inhibition of the NAD+-dependent lysine deacylase sirtuin 2.

Swyter S, Schiedel M, Monaldi D, Szunyogh S, Lehotzky A, Rumpf T, Ovádi J, Sippl W, Jung M.

Philos Trans R Soc Lond B Biol Sci. 2018 Jun 5;373(1748). pii: 20170083. doi: 10.1098/rstb.2017.0083.

PMID:
29685963
19.

Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites.

Chua MJ, Robaa D, Skinner-Adams TS, Sippl W, Andrews KT.

Int J Parasitol Drugs Drug Resist. 2018 Aug;8(2):189-193. doi: 10.1016/j.ijpddr.2018.03.001. Epub 2018 Mar 26.

20.

A kinome-wide RNAi screen identifies ALK as a target to sensitize neuroblastoma cells for HDAC8-inhibitor treatment.

Shen J, Najafi S, Stäble S, Fabian J, Koeneke E, Kolbinger FR, Wrobel JK, Meder B, Distel M, Heimburg T, Sippl W, Jung M, Peterziel H, Kranz D, Boutros M, Westermann F, Witt O, Oehme I.

Cell Death Differ. 2018 Dec;25(12):2053-2070. doi: 10.1038/s41418-018-0080-0. Epub 2018 Mar 7.

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