Holger Gohlke
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View article: DDX3X syndrome: a multicenter genotype-phenotype study
DDX3X syndrome: a multicenter genotype-phenotype study Open
DDX3X dysfunction causes an X-linked multisystem disorder with high penetrance and variable expressivity. The phenotypic spectrum spans from learning disability without somatic involvement to profound intellectual disability with severe im…
View article: Molecular mechanism and structural models of protein-mediated copper transfer to the Arabidopsis thaliana ethylene receptor ETR1 at the ER membrane
Molecular mechanism and structural models of protein-mediated copper transfer to the Arabidopsis thaliana ethylene receptor ETR1 at the ER membrane Open
View article: Influence of α-Helical Content on the Thermodiffusion of Apomyoglobin
Influence of α-Helical Content on the Thermodiffusion of Apomyoglobin Open
Apo-myoglobin (Apo-Mb) is an extensively studied model system for investigating protein folding due to its distinct stable native, partially folded molten globule (MG), and unfolded states at acidic pH. This study examines the impact of st…
View article: Molecular Insights into CLD Domain Dynamics and Toxin Recruitment of the HlyA E. coli T1SS
Molecular Insights into CLD Domain Dynamics and Toxin Recruitment of the HlyA E. coli T1SS Open
Escherichia coli is a Gram-negative opportunistic pathogen causing nosocomial infections through the production of various virulence factors. Type 1 secretion systems (T1SS) contribute to virulence by mediating the one-step secretion of un…
View article: Mechanistic Insights into the Structural Asymmetry of the LanFEG Transporter NisFEG in Lantibiotic Immunity
Mechanistic Insights into the Structural Asymmetry of the LanFEG Transporter NisFEG in Lantibiotic Immunity Open
Nisin is one of the best studied antimicrobial peptides. Still, how nisin-producing strains can protect themselves against nisin’s bactericidal effects is only partially understood. Located within the nisin biosynthesis operon, the heterot…
View article: A farnesoid X receptor T296I variant disrupts ligand-induced FXR activation and thus bile acid transport in progressive familial intrahepatic cholestasis
A farnesoid X receptor T296I variant disrupts ligand-induced FXR activation and thus bile acid transport in progressive familial intrahepatic cholestasis Open
View article: The extracellular domain of SaNSrFP binds bacitracin and allows the identification of new members of the BceAB transporter family
The extracellular domain of SaNSrFP binds bacitracin and allows the identification of new members of the BceAB transporter family Open
Peptidoglycan serves as the first permeability barrier of Gram-positive bacteria. Intermediates of the peptidoglycan synthesis cycle are typical targets of antimicrobial compounds, including the peptide antibiotics nisin and bacitracin. In…
View article: The bacterial ESCRT-III PspA rods thin lipid tubules and increase membrane curvature through helix α0 interactions
The bacterial ESCRT-III PspA rods thin lipid tubules and increase membrane curvature through helix α0 interactions Open
The phage shock protein A (PspA), a bacterial member of the endosomal sorting complexes required for transport (ESCRT)-III superfamily, forms rod-shaped helical assemblies that internalize membrane tubules. The N-terminal helix α0 of PspA …
View article: A novel biosensor for ferrous iron developed via CoBiSe: A computational method for rapid biosensor design
A novel biosensor for ferrous iron developed via CoBiSe: A computational method for rapid biosensor design Open
Genetically encoded biosensors enable monitoring of metabolite dynamics in living organisms. We present CoBiSe, a computational approach using Constraint Network Analysis to identify optimal insertion sites for reporter modules in molecula…
View article: The coming of age of DNA‐based catalysts for therapeutic applications
The coming of age of DNA‐based catalysts for therapeutic applications Open
View article: The bacterial ESCRT-III PspA rods thin lipid tubules and increase membrane curvature through helix α0 interactions
The bacterial ESCRT-III PspA rods thin lipid tubules and increase membrane curvature through helix α0 interactions Open
The phage shock protein A (PspA), a bacterial member of the ESCRT-III superfamily, forms rod-shaped helical assemblies that internalize membrane tubules. The N-terminal helix α0 of PspA (and other ESCRT-III members) has been suggested to a…
View article: Molecular Insights into CLD Domain Dynamics and Toxin Recruitment of the HlyA <i>E. coli</i> T1SS
Molecular Insights into CLD Domain Dynamics and Toxin Recruitment of the HlyA <i>E. coli</i> T1SS Open
Escherichia coli is a Gram-negative opportunistic pathogen causing nosocomial infections through the production of various virulence factors. Type 1 secretion systems (T1SS) contribute to virulence by mediating one-step secretion of unfold…
View article: Influence of ionic liquids on enzymatic asymmetric carboligations
Influence of ionic liquids on enzymatic asymmetric carboligations Open
The asymmetric mixed carboligation of aldehydes catalyzed by thiamine diphosphate (ThDP)-dependent enzymes provides a sensitive system for monitoring changes in activity, chemo-, and enantioselectivity. While previous studies have shown th…
View article: The mycotoxin Beauvericin is an uncompetitive inhibitor of Cathepsin B
The mycotoxin Beauvericin is an uncompetitive inhibitor of Cathepsin B Open
Beauvericin (BEA), a cyclic depsipeptide, is a mycotoxin of the enniatin family and the secondary metabolite of various toxigenic fungi. Multiple biological functions of BEA have been well investigated, such as anti‐cancer, anti‐inflammato…
View article: Identification of non-charged 7.44 analogs interacting with the NHR2 domain of RUNX1-ETO with improved antiproliferative effect in RUNX-ETO positive cells
Identification of non-charged 7.44 analogs interacting with the NHR2 domain of RUNX1-ETO with improved antiproliferative effect in RUNX-ETO positive cells Open
View article: TopCysteineDB: A Cysteinome-wide Database Integrating Structural and Chemoproteomics Data for Cysteine Ligandability Prediction
TopCysteineDB: A Cysteinome-wide Database Integrating Structural and Chemoproteomics Data for Cysteine Ligandability Prediction Open
Development of targeted covalent inhibitors and covalent ligand-first approaches have emerged as a powerful strategy in drug design, with cysteines being attractive targets due to their nucleophilicity and relative scarcity. While structur…
View article: A Novel Approach to Combat <i>Pseudomonas aeruginosa</i>: Repurposing Pharmaceuticals for Inhibition of Phospholipase A
A Novel Approach to Combat <i>Pseudomonas aeruginosa</i>: Repurposing Pharmaceuticals for Inhibition of Phospholipase A Open
Phospholipases A (PLAs) play critical roles in cellular physiology, making human PLAs established drug targets. On the other hand, the potential of bacterial PLAs as targets for antimicrobial drug development remains underexplored. In this…
View article: TopEC: prediction of Enzyme Commission classes by 3D graph neural networks and localized 3D protein descriptor
TopEC: prediction of Enzyme Commission classes by 3D graph neural networks and localized 3D protein descriptor Open
View article: Cyclophilin A Regulates Tripartite Motif 5 Alpha Restriction of HIV-1
Cyclophilin A Regulates Tripartite Motif 5 Alpha Restriction of HIV-1 Open
The peptidyl-prolyl isomerase A (PPIA), also known as cyclophilin A (CYPA), is involved in multiple steps of the HIV-1 replication cycle. CYPA regulates the restriction of many host factors by interacting with the CYPA-binding loop on the …
View article: Influence of ionic liquids on enzymatic asymmetric carboligations
Influence of ionic liquids on enzymatic asymmetric carboligations Open
The asymmetric mixed carboligation of aldehydes catalyzed by thiamine diphosphate (ThDP)-dependent enzymes provides a sensitive system for monitoring changes in activity, chemo-, and enantioselectivity. While previous studies have shown th…
View article: Characterization of a C-methyltransferase from <i>Streptomyces griseoviridis</i> – crystal structure, mechanism, and substrate scope
Characterization of a C-methyltransferase from <i>Streptomyces griseoviridis</i> – crystal structure, mechanism, and substrate scope Open
This study elucidates the structure, catalytic mechanism, and substrate selectivity of the SAM-dependent methyltransferase from Streptomyces griseoviridis , which catalyses the synthesis of pyrroloindole motifs in tryptophan-based diketopi…
View article: Human chitinases and chitinase-like proteins as emerging drug targets – a medicinal chemistry perspective
Human chitinases and chitinase-like proteins as emerging drug targets – a medicinal chemistry perspective Open
Human chitinases and chitinase-like proteins are attractive drug targets. This review focuses on medicinal chemistry efforts directed at acidic mammalian chitinase (AMCase), chitotriosidase (CHIT1), and chitinase-3-like protein 1 (CHI3L1/Y…
View article: TopCysteineDB: A Cysteinome-Wide Database Integrating Structural and Chemoproteomics Data for Cysteine Ligandability Prediction
TopCysteineDB: A Cysteinome-Wide Database Integrating Structural and Chemoproteomics Data for Cysteine Ligandability Prediction Open
View article: Novel 4-alkoxy Meriolin Congeners Potently Induce Apoptosis in Leukemia and Lymphoma Cells
Novel 4-alkoxy Meriolin Congeners Potently Induce Apoptosis in Leukemia and Lymphoma Cells Open
Meriolins (3-(pyrimidin-4-yl)-7-azaindoles) are synthetic hybrids of the naturally occurring alkaloids variolin and meridianin and display a strong cytotoxic potential. We have recently shown that the novel derivative meriolin 16 is highly…
View article: Small-molecule inhibitor of C-terminal HSP90 dimerization modulates autophagy and functions synergistically with mTOR inhibition to kill cisplatin-resistant cancer cells
Small-molecule inhibitor of C-terminal HSP90 dimerization modulates autophagy and functions synergistically with mTOR inhibition to kill cisplatin-resistant cancer cells Open
Background A major obstacle for the successful treatment of cancer is the primary presence or development of resistance mechanisms toward therapeutic intervention. In urothelial cancer, cisplatin-based regimens are still routinely employed…
View article: CD63 as novel target for nanoemulsion-based <sup>19</sup>F MRI imaging and drug delivery to activated cardiac fibroblasts
CD63 as novel target for nanoemulsion-based <sup>19</sup>F MRI imaging and drug delivery to activated cardiac fibroblasts Open
Rationale: Cardiac fibroblasts are activated following myocardial infarction (MI) and cardiac fibrosis is a major driver of the growing burden of heart failure. A non-invasive targeting method for activated cardiac fibroblasts would…
View article: Aplospojaveedins A–C, unusual sulfur-containing alkaloids produced by the endophytic fungus Aplosporella javeedii using OSMAC strategy
Aplospojaveedins A–C, unusual sulfur-containing alkaloids produced by the endophytic fungus Aplosporella javeedii using OSMAC strategy Open
Three sulfur-containing alkaloids aplospojaveedins A–C (1–3) with a hitherto undescribed carbon skeleton comprising octahy-dronaphthalene, α , β -unsaturated lactam and glycine-cysteine moieties were isolated from Aplosporella javeedii . T…
View article: Long-read transcriptome sequencing of CLL and MDS patients uncovers molecular effects of <i>SF3B1</i> mutations
Long-read transcriptome sequencing of CLL and MDS patients uncovers molecular effects of <i>SF3B1</i> mutations Open
Mutations in splicing factor 3B subunit 1 ( SF3B1 ) frequently occur in patients with chronic lymphocytic leukemia (CLL) and myelodysplastic syndromes (MDSs). These mutations have different effects on the disease prognosis with beneficial …
View article: Structure and dimerization properties of the plant-specific copper chaperone CCH
Structure and dimerization properties of the plant-specific copper chaperone CCH Open
View article: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells
The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells Open
Anti-estrogenic therapy is established in the management of estrogen receptor (ER)-positive breast cancer. However, to overcome resistance and improve therapeutic outcome, novel strategies are needed such as targeting widely recognized abe…