Search results for: Ulrike Leurs

Items from 1 to 8 out of 8 results

article

Improved prediction of HLA antigen presentation hotspots: Applications for immunogenicity risk assessment of therapeutic proteins

Anders Steenholdt Attermann, Carolina Barra, Birkir Reynisson, Heidi Schiøler Schultz, more

Immunogenicity risk assessment is a critical element in protein drug development. Currently, the risk assessment is most often performed using MHC‐associated peptide proteomics (MAPPs) and/or T‐cell activation assays. However, this is a highly costly procedure that encompasses limited sensitivity imposed by sample sizes, the MHC repertoire of the tested donor cohort and the experimental procedures...

article

Silencing of spontaneous activity at α4β1/3δ GABA_A receptors in hippocampal granule cells reveals different ligand pharmacology

Nils Ole Dalby, Christina Birkedahl Falk‐Petersen, Ulrike Leurs, Petra Scholze, more

British Journal of Pharmacology > 177 > 17 > 3975 - 3990

Background and Purpose The δ‐subunit‐containing GABA_A receptors, α₄β₁δ and α₄β₃δ, in dentate gyrus granule cells (DGGCs) are known to exhibit both spontaneous channel openings (i.e. constitutive activity) and agonist‐induced current. The functional implications of spontaneous gating are unclear. In this study, we tested the hypothesis that constitutively active α₄β_1/3δ receptors limit agonist efficacy...

article

Getting to the core of protein pharmaceuticals – Comprehensive structure analysis by mass spectrometry

Ulrike Leurs, Ulrik H. Mistarz, Kasper D. Rand

European Journal of Pharmaceutics and Biopharmaceutics > 2015 > 93 > Complete > 95-109

Protein pharmaceuticals are the fastest growing class of novel therapeutic agents, and have been a major research and development focus in the (bio)pharmaceutical industry. Due to their large size and structural diversity, biopharmaceuticals represent a formidable challenge regarding analysis and characterization compared to traditional small molecule drugs. Any changes to the primary, secondary,...

article

Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C)

Ulrike Leurs, Rasmus P. Clausen, Jesper L. Kristensen, Brian Lohse

Bioorganic & Medicinal Chemistry Letters > 2012 > 22 > 18 > 5811-5813

The human histone demethylases of the KDM4 (JMJD2) family have been associated to diseases such as prostate and breast cancer, as well as X-linked mental retardation. Therefore, these enzymes are considered oncogenes and their selective inhibition might be a possible therapeutic approach to treat cancer. Here we describe a heterocyclic ring system library screened against the histone demethylase KDM4C...

article

GnRH-III based multifunctional drug delivery systems containing daunorubicin and methotrexate

Ulrike Leurs, Eszter Lajkó, Gábor Mező, Erika Orbán, more

European Journal of Medicinal Chemistry > 2012 > 52 > Complete > 173-183

Here we report on the design, synthesis and biochemical characterization of multifunctional bioconjugates containing two chemotherapeutic agents, daunorubicin and methotrexate, coupled to the GnRH-III decapeptide, which served as a targeting moiety. This represents a possible approach to increase the receptor mediated tumor targeting and consequently the cytostatic effect of anticancer drug-peptide...

article

Design, synthesis, in vitro stability and cytostatic effect of multifunctional anticancer drug‐bioconjugates containing GnRH‐III as a targeting moiety

Ulrike Leurs, Gábor Mező, Erika Orbán, Peter Öhlschläger, more

Biopolymers > 98 > 1 > 1 - 10

Bioconjugates containing the GnRH‐III hormone decapeptide as a targeting moiety are able to deliver chemotherapeutic agents specifically to cancer cells expressing GnRH receptors, thereby increasing their local efficacy while limiting the peripheral toxicity. However, the number of GnRH receptors on cancer cells is limited and they desensitize under continuous hormone treatment. A possible approach...

article

Enhanced Enzymatic Stability and Antitumor Activity of Daunorubicin-GnRH-III Bioconjugates Modified in Position 4

Marilena Manea, Ulrike Leurs, Erika Orbán, Zsuzsa Baranyai, more

Bioconjugate Chemistry > 2011 > 22 > 7 > 1320 - 1329

article

Efficient synthesis of an (aminooxy) acetylated‐somatostatin derivative using (aminooxy)acetic acid as a ‘carbonyl capture’ reagent

Gábor Mezö, Ildikó Szabó, István Kertész, Rózsa Hegedüs, more

Journal of Peptide Science > 17 > 1 > 39 - 46

Owing to the high chemoselectivity between an aminooxy function and a carbonyl group, oxime ligation is one of the most preferred procedures for the preparation of peptide conjugates. However, the sensitivity of (aminooxy)acetylated peptides to ketones and aldehydes makes their synthesis and storage difficult. In our study, we established the efficient synthesis of an (aminooxy)acetylated‐somatostatin...

Filter options

Publication date

Set your own date range

INFONA - science communication portal

Search results for: Ulrike Leurs

Add recipient

Sending message cancelled

Are you sure you want to cancel sending this message?

Send message

Filter options

Publication date

Date range setting

Set the date range to filter the displayed results. You can set a starting date, ending date or both. You can enter the dates manually or choose them from the calendar.

Keywords

Data set

Journal

Reporting an error / abuse

Sending the report failed

Accessibility options