[HTML][HTML] Encoded library technologies as integrated lead finding platforms for drug discovery
J Ottl, L Leder, JV Schaefer, CE Dumelin - Molecules, 2019 - mdpi.com
The scope of targets investigated in pharmaceutical research is continuously moving into
uncharted territory. Consequently, finding suitable chemical matter with current compound …
uncharted territory. Consequently, finding suitable chemical matter with current compound …
[HTML][HTML] Programmable DARPin-based receptors for the detection of thrombotic markers
…, PC Freitag, PG Ray, P Stuecheli, JV Schaefer… - Nature chemical …, 2022 - nature.com
Cellular therapies remain constrained by the limited availability of sensors for disease markers.
Here we present an integrated target-to-receptor pipeline for constructing a customizable …
Here we present an integrated target-to-receptor pipeline for constructing a customizable …
[HTML][HTML] Structural basis of adenylyl cyclase 9 activation
…, I Mohammed, Y Li, M Lazaratos, JV Schaefer… - Nature …, 2022 - nature.com
Adenylyl cyclase 9 (AC9) is a membrane-bound enzyme that converts ATP into cAMP. The
enzyme is weakly activated by forskolin, fully activated by the G protein Gαs subunit and is …
enzyme is weakly activated by forskolin, fully activated by the G protein Gαs subunit and is …
[HTML][HTML] Asymmetric requirement of Dpp/BMP morphogen dispersal in the Drosophila wing disc
How morphogen gradients control patterning and growth in developing tissues remains largely
unknown due to lack of tools manipulating morphogen gradients. Here, we generate two …
unknown due to lack of tools manipulating morphogen gradients. Here, we generate two …
[HTML][HTML] Intermolecular biparatopic trapping of ErbB2 prevents compensatory activation of PI3K/AKT via RAS–p110 crosstalk
…, DC Schaefer, WPR Verdurmen, JV Schaefer… - Nature …, 2016 - nature.com
Compensatory mechanisms, such as relief of AKT-ErbB3-negative feedback, are known to
desensitize ErbB2-dependent tumours to targeted therapy. Here we describe an adaptation …
desensitize ErbB2-dependent tumours to targeted therapy. Here we describe an adaptation …
[PDF][PDF] Disrupting the HDAC6-ubiquitin interaction impairs infection by influenza and Zika virus and cellular stress pathways
…, Y Miyake, BIO Esteves, A Fahmi, JV Schaefer… - Cell reports, 2022 - cell.com
The deacetylase HDAC6 has tandem catalytic domains and a zinc finger domain (ZnF)
binding ubiquitin (Ub). While the catalytic domain has an antiviral effect, the ZnF facilitates …
binding ubiquitin (Ub). While the catalytic domain has an antiviral effect, the ZnF facilitates …
[HTML][HTML] Nuclear myosin VI maintains replication fork stability
…, V Arz, T Strauch, JB Heidelberger, JV Schaefer… - Nature …, 2023 - nature.com
The actin cytoskeleton is of fundamental importance for cellular structure and plasticity.
However, abundance and function of filamentous actin in the nucleus are still controversial. Here …
However, abundance and function of filamentous actin in the nucleus are still controversial. Here …
[HTML][HTML] Distinct conformations of the HIV-1 V3 loop crown are targetable for broad neutralization
…, T Liechti, B Ivan, T Reinberg, JV Schaefer… - Nature …, 2021 - nature.com
The V3 loop of the HIV-1 envelope (Env) protein elicits a vigorous, but largely non-neutralizing
antibody response directed to the V3-crown, whereas rare broadly neutralizing antibodies …
antibody response directed to the V3-crown, whereas rare broadly neutralizing antibodies …
Engineering aggregation resistance in IgG by two independent mechanisms: lessons from comparison of Pichia pastoris and mammalian cell expression
JV Schaefer, A Plückthun - Journal of molecular biology, 2012 - Elsevier
Aggregation is an important concern for therapeutic antibodies, since it can lead to reduced
bioactivity and increase the risk of immunogenicity. In our analysis of immunoglobulin G (IgG…
bioactivity and increase the risk of immunogenicity. In our analysis of immunoglobulin G (IgG…
[HTML][HTML] A DARPin promotes faster onset of botulinum neurotoxin A1 action
…, S Furler, T Reinberg, J Marinho, JV Schaefer… - Nature …, 2023 - nature.com
In this study, we characterize Designed Ankyrin Repeat Proteins (DARPins) as investigative
tools to probe botulinum neurotoxin A1 (BoNT/A1) structure and function. We identify …
tools to probe botulinum neurotoxin A1 (BoNT/A1) structure and function. We identify …