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Items: 1 to 20 of 166

1.

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 Sep 11. pii: S0960-894X(18)30744-3. doi: 10.1016/j.bmcl.2018.09.013. [Epub ahead of print]

PMID:
30220607
2.

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.

3.

Elastin is heterogeneously cross-linked.

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

J Biol Chem. 2018 Aug 14. pii: jbc.RA118.004322. doi: 10.1074/jbc.RA118.004322. [Epub ahead of print]

4.

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
5.

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.

6.

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
7.

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.

8.

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
9.

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
10.

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 May 9. doi: 10.1007/s13659-018-0165-y. [Epub ahead of print] Review.

11.

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
12.

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
13.

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.

14.

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 Mar 7. doi: 10.1038/s41418-018-0080-0. [Epub ahead of print]

PMID:
29515255
15.

A Novel Class of Schistosoma mansoni Histone Deacetylase 8 (HDAC8) Inhibitors Identified by Structure-Based Virtual Screening and In Vitro Testing.

Simoben CV, Robaa D, Chakrabarti A, Schmidtkunz K, Marek M, Lancelot J, Kannan S, Melesina J, Shaik TB, Pierce RJ, Romier C, Jung M, Sippl W.

Molecules. 2018 Mar 2;23(3). pii: E566. doi: 10.3390/molecules23030566.

16.

Potent and Selective Inhibitors of Human Sirtuin 5.

Kalbas D, Liebscher S, Nowak T, Meleshin M, Pannek M, Popp C, Alhalabi Z, Bordusa F, Sippl W, Steegborn C, Schutkowski M.

J Med Chem. 2018 Mar 22;61(6):2460-2471. doi: 10.1021/acs.jmedchem.7b01648. Epub 2018 Mar 12.

PMID:
29494161
17.

Identification of Bichalcones as Sirtuin Inhibitors by Virtual Screening and In Vitro Testing.

Karaman B, Alhalabi Z, Swyter S, Mihigo SO, Andrae-Marobela K, Jung M, Sippl W, Ntie-Kang F.

Molecules. 2018 Feb 14;23(2). pii: E416. doi: 10.3390/molecules23020416.

18.

Carbamates as Potential Prodrugs and a New Warhead for HDAC Inhibition.

King K, Hauser AT, Melesina J, Sippl W, Jung M.

Molecules. 2018 Feb 2;23(2). pii: E321. doi: 10.3390/molecules23020321.

19.

Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation.

Temme L, Frehland B, Schepmann D, Robaa D, Sippl W, Wünsch B.

Eur J Med Chem. 2018 Jan 20;144:672-681. doi: 10.1016/j.ejmech.2017.12.054. Epub 2017 Dec 18.

PMID:
29289890
20.

Structure-activity studies on N-Substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation.

Schulz-Fincke J, Hau M, Barth J, Robaa D, Willmann D, Kürner A, Haas J, Greve G, Haydn T, Fulda S, Lübbert M, Lüdeke S, Berg T, Sippl W, Schüle R, Jung M.

Eur J Med Chem. 2018 Jan 20;144:52-67. doi: 10.1016/j.ejmech.2017.12.001. Epub 2017 Dec 6.

PMID:
29247860

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