Bernd Gerhartz

A CRISPR Cas12a/Cpf1 strategy to facilitate robust multiplex gene editing in Aspergillus Niger

Abel Peter van Esch, Samuel Mathew Maurice Prudence, Fabiano Jares Contesini, Bernd Gerhartz et autres

BACKGROUND: CRISPR technologies have revolutionized strain engineering of Aspergillus species, and drastically increased the ease and speed at which genomic modifications can be performed. One of the advantages of CRISPR technologies is the possibility of rapid strain engineering using multiplex experiments. This …

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Discovery of 4-((2 S ,4 S )-4-Ethoxy-1-((5-methoxy-7-methyl-1 H -indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases

Nello Mainolfi, Takeru Ehara, Rajeshri G. Karki, Karen Anderson et autres

The alternative pathway (AP) of the complement system is a key contributor to the pathogenesis of several human diseases including age-related macular degeneration, paroxysmal nocturnal hemoglobinuria (PNH), atypical hemolytic uremic syndrome (aHUS), and various glomerular diseases. The serine protease factor B (FB) …

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Complement factor B in complex with (S)-5,7-Dimethyl-4-((2-phenylpiperidin-1-yl)methyl)-1H-indole

Nello Mainolfi, Takashi Ehara, R. Karki, Kenton L. Anderson et autres

Small-molecule factor B inhibitor for the treatment of complement-mediated diseases

Anna Schubart, Karen Anderson, Nello Mainolfi, Holger Sellner et autres

Dysregulation of the alternative complement pathway (AP) predisposes individuals to a number of diseases including paroxysmal nocturnal hemoglobinuria, atypical hemolytic uremic syndrome, and C3 glomerulopathy. Moreover, glomerular Ig deposits can lead to complement-driven nephropathies. Here we describe the discovery of a highly …

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Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors

Anna Vulpetti, Stefan Randl, Simon Rüdisser, Nils Ostermann et autres

Chronic dysregulation of alternative complement pathway activation has been associated with diverse clinical disorders including age-related macular degeneration and paroxysmal nocturnal hemoglobinurea. Factor D is a trypsin-like serine protease with a narrow specificity for arginine in the P1 position, which catalyzes the …

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Small-molecule factor D inhibitors targeting the alternative complement pathway

Jürgen Maibaum, Sha-Mei Liao, Anna Vulpetti, Nils Ostermann et autres

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Transfection of insect cell in suspension for efficient baculovirus generation

Susan Roest, Sandra Kapps-Fouthier, Julia Klopp, S. Rieffel et autres

Baculovirus (BV) mediated insect cell expression system utilizes transfection as a first step to introduce recombinant baculovirus DNA into insect cells. Many labs are still relying on the conventional liposome based transfection method in adherent culture. Here we describe a more efficient …

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Discovery of small-molecule reversible Factor D inhibitors targeting the alternative complement pathway

Juergen Maibaum, Sha-Mei Liao, Anna Vulpetti, Nils Ostermann et autres

CCDC 898747: Experimental Crystal Structure Determination

Nils Ostermann, Simon Ruedisser, Claus Ehrhardt, Werner Breitenstein et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Inside Cover: Gift from Nature: Cyclomarin A Kills Mycobacteria and Malaria Parasites by Distinct Modes of Action (ChemBioChem 17/2015)

Nathalie Bürstner, Silvio Roggo, Nils Ostermann, Jutta Blank et autres

The inside cover picture shows the malaria parasite Plasmodium falciparum at the late schizont stage in a red blood cell. It is filled with invasive merozoites. The natural product cyclomarin A is a potent inhibitor of the growth of P. falciparum. It …

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Gift from Nature: Cyclomarin A Kills Mycobacteria and Malaria Parasites by Distinct Modes of Action

Nathalie Bürstner, Silvio Roggo, Nils Ostermann, Jutta Blank et autres

Malaria continues to be one of the most devastating human diseases despite many efforts to limit its spread by prevention of infection or by pharmaceutical treatment of patients. We have conducted a screen for antiplasmodial compounds by using a natural product library. …

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Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV

Kenji Namoto, Finton Sirockin, Nils Ostermann, F. Gessier et autres

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