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Items: 1 to 20 of 223

1.

Benzophenones as xanthone-open model CYP11B1 inhibitors potentially useful for promoting wound healing.

Gobbi S, Hu Q, Foschi G, Catanzaro E, Belluti F, Rampa A, Fimognari C, Hartmann RW, Bisi A.

Bioorg Chem. 2019 Jan 30;86:401-409. doi: 10.1016/j.bioorg.2019.01.066. [Epub ahead of print]

PMID:
30769265
2.

2-Aminothiazole derivatives as selective allosteric modulators of the protein kinase CK2. Part 1: Identification of an allosteric binding site.

Bestgen B, Krimm I, Kufareva I, Kamal A, Seetoh WG, Abell C, Hartmann RW, Abagyan R, Cochet C, Le Borgne M, Engel M, Lomberget T.

J Med Chem. 2019 Jan 28. doi: 10.1021/acs.jmedchem.8b01766. [Epub ahead of print]

PMID:
30689953
3.

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action.

Bestgen B, Kufareva I, Seetoh W, Abell C, Hartmann RW, Abagyan R, Le Borgne M, Filhol O, Cochet C, Lomberget T, Engel M.

J Med Chem. 2019 Feb 13. doi: 10.1021/acs.jmedchem.8b01765. [Epub ahead of print]

PMID:
30689946
4.

Targeted Endocrine Therapy: Design, Synthesis, and Proof-of-Principle of 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors in Bone Fracture Healing.

Abdelsamie AS, Herath S, Biskupek Y, Börger C, Siebenbürger L, Salah M, Scheuer C, Marchais-Oberwinkler S, Frotscher M, Pohlemann T, Menger MD, Hartmann RW, Laschke MW, van Koppen CJ.

J Med Chem. 2019 Jan 15. doi: 10.1021/acs.jmedchem.8b01493. [Epub ahead of print]

PMID:
30645111
5.

Highly Potent 17β-HSD2 Inhibitors with a Promising Pharmacokinetic Profile for Targeted Osteoporosis Therapy.

Siebenbuerger L, Hernandez-Olmos V, Abdelsamie AS, Frotscher M, van Koppen CJ, Marchais-Oberwinkler S, Scheuer C, Laschke MW, Menger MD, Boerger C, Hartmann RW.

J Med Chem. 2018 Nov 27. doi: 10.1021/acs.jmedchem.8b01373. [Epub ahead of print]

PMID:
30480443
6.

Tackling Pseudomonas aeruginosa Virulence by a Hydroxamic Acid-Based LasB Inhibitor.

Kany AM, Sikandar A, Yahiaoui S, Haupenthal J, Walter I, Empting M, Köhnke J, Hartmann RW.

ACS Chem Biol. 2018 Sep 21;13(9):2449-2455. doi: 10.1021/acschembio.8b00257. Epub 2018 Aug 24.

PMID:
30088919
7.

Design and synthesis of novel annulated thienopyrimidines as phosphodiesterase 5 (PDE5) inhibitors.

El-Sharkawy LY, El-Sakhawy RA, Abdel-Halim M, Lee K, Piazza GA, Ducho C, Hartmann RW, Abadi AH.

Arch Pharm (Weinheim). 2018 May;351(5):e1800018. doi: 10.1002/ardp.201800018. Epub 2018 Apr 14.

PMID:
29656464
8.

Binding Mode Characterization and Early in Vivo Evaluation of Fragment-Like Thiols as Inhibitors of the Virulence Factor LasB from Pseudomonas aeruginosa.

Kany AM, Sikandar A, Haupenthal J, Yahiaoui S, Maurer CK, Proschak E, Köhnke J, Hartmann RW.

ACS Infect Dis. 2018 Jun 8;4(6):988-997. doi: 10.1021/acsinfecdis.8b00010. Epub 2018 Mar 6.

PMID:
29485268
9.

Pharmacophore Modeling and in Silico/in Vitro Screening for Human Cytochrome P450 11B1 and Cytochrome P450 11B2 Inhibitors.

Akram M, Waratchareeyakul W, Haupenthal J, Hartmann RW, Schuster D.

Front Chem. 2017 Dec 19;5:104. doi: 10.3389/fchem.2017.00104. eCollection 2017.

10.

Glycomimetic, Orally Bioavailable LecB Inhibitors Block Biofilm Formation of Pseudomonas aeruginosa.

Sommer R, Wagner S, Rox K, Varrot A, Hauck D, Wamhoff EC, Schreiber J, Ryckmans T, Brunner T, Rademacher C, Hartmann RW, Brönstrup M, Imberty A, Titz A.

J Am Chem Soc. 2018 Feb 21;140(7):2537-2545. doi: 10.1021/jacs.7b11133. Epub 2018 Jan 22.

PMID:
29272578
11.

Crocadepsins-Depsipeptides from the Myxobacterium Chondromyces crocatus Found by a Genome Mining Approach.

Surup F, Viehrig K, Rachid S, Plaza A, Maurer CK, Hartmann RW, Müller R.

ACS Chem Biol. 2018 Jan 19;13(1):267-272. doi: 10.1021/acschembio.7b00900. Epub 2017 Dec 28.

PMID:
29220569
12.

Accelerated skin wound healing by selective 11β-Hydroxylase (CYP11B1) inhibitors.

Emmerich J, van Koppen CJ, Burkhart JL, Engeli RT, Hu Q, Odermatt A, Hartmann RW.

Eur J Med Chem. 2018 Jan 1;143:591-597. doi: 10.1016/j.ejmech.2017.11.018. Epub 2017 Nov 21.

PMID:
29207342
13.

CYP17A1-independent production of the neurosteroid-derived 5α-pregnan-3β,6α-diol-20-one in androgen-responsive prostate cancer cell lines under serum starvation and inhibition by Abiraterone.

de Mello Martins AGG, Allegretta G, Unteregger G, Haupenthal J, Eberhard J, Hoffmann M, van der Zee JA, Junker K, Stöckle M, Müller R, Hartmann RW, Ohlmann CH.

J Steroid Biochem Mol Biol. 2017 Nov;174:183-191. doi: 10.1016/j.jsbmb.2017.09.006. Epub 2017 Sep 7.

PMID:
28890368
14.

Discovery of a Potent Inhibitor Class with High Selectivity toward Clostridial Collagenases.

Schönauer E, Kany AM, Haupenthal J, Hüsecken K, Hoppe IJ, Voos K, Yahiaoui S, Elsässer B, Ducho C, Brandstetter H, Hartmann RW.

J Am Chem Soc. 2017 Sep 13;139(36):12696-12703. doi: 10.1021/jacs.7b06935. Epub 2017 Aug 31.

15.

Biophysical Screening of a Focused Library for the Discovery of CYP121 Inhibitors as Novel Antimycobacterials.

Brengel C, Thomann A, Schifrin A, Allegretta G, Kamal AAM, Haupenthal J, Schnorr I, Cho SH, Franzblau SG, Empting M, Eberhard J, Hartmann RW.

ChemMedChem. 2017 Oct 9;12(19):1616-1626. doi: 10.1002/cmdc.201700363. Epub 2017 Sep 26.

PMID:
28815923
16.

Drifting of heme-coordinating group in imidazolylmethylxanthones leading to improved selective inhibition of CYP11B1.

Gobbi S, Hu Q, Zimmer C, Belluti F, Rampa A, Hartmann RW, Bisi A.

Eur J Med Chem. 2017 Oct 20;139:60-67. doi: 10.1016/j.ejmech.2017.07.078. Epub 2017 Aug 2.

PMID:
28797884
17.

In-depth Profiling of MvfR-Regulated Small Molecules in Pseudomonas aeruginosa after Quorum Sensing Inhibitor Treatment.

Allegretta G, Maurer CK, Eberhard J, Maura D, Hartmann RW, Rahme L, Empting M.

Front Microbiol. 2017 May 24;8:924. doi: 10.3389/fmicb.2017.00924. eCollection 2017.

18.

Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.

Emmerich J, van Koppen CJ, Burkhart JL, Hu Q, Siebenbürger L, Boerger C, Scheuer C, Laschke MW, Menger MD, Hartmann RW.

J Med Chem. 2017 Jun 22;60(12):5086-5098. doi: 10.1021/acs.jmedchem.7b00437. Epub 2017 Jun 9.

PMID:
28570067
19.

Structure-functionality relationship and pharmacological profiles of Pseudomonas aeruginosa alkylquinolone quorum sensing modulators.

Kamal AAM, Petrera L, Eberhard J, Hartmann RW.

Org Biomol Chem. 2017 May 31;15(21):4620-4630. doi: 10.1039/c7ob00263g.

PMID:
28513746
20.

Regulation of Burkholderia cenocepacia biofilm formation by RpoN and the c-di-GMP effector BerB.

Fazli M, Rybtke M, Steiner E, Weidel E, Berthelsen J, Groizeleau J, Bin W, Zhi BZ, Yaming Z, Kaever V, Givskov M, Hartmann RW, Eberl L, Tolker-Nielsen T.

Microbiologyopen. 2017 Aug;6(4). doi: 10.1002/mbo3.480. Epub 2017 Apr 16.

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