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View article: Author Correction: Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis
Author Correction: Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis Open
View article: The small-molecule SMARt751 reverses <i>Mycobacterium tuberculosis</i> resistance to ethionamide in acute and chronic mouse models of tuberculosis
The small-molecule SMARt751 reverses <i>Mycobacterium tuberculosis</i> resistance to ethionamide in acute and chronic mouse models of tuberculosis Open
The sensitivity of Mycobacterium tuberculosis , the pathogen that causes tuberculosis (TB), to antibiotic prodrugs is dependent on the efficacy of the activation process that transforms the prodrugs into their active antibacterial moieties…
View article: Patient-derived gene and protein expression signatures of NGLY1 deficiency
Patient-derived gene and protein expression signatures of NGLY1 deficiency Open
N-Glycanase 1 (NGLY1) deficiency is a rare and complex genetic disorder. Although recent studies have shed light on the molecular underpinnings of NGLY1 deficiency, a systematic characterization of gene and protein expression changes in pa…
View article: Loss of N-Glycanase 1 Alters Transcriptional and Translational Regulation in K562 Cell Lines
Loss of N-Glycanase 1 Alters Transcriptional and Translational Regulation in K562 Cell Lines Open
N-Glycanase 1 (NGLY1) deficiency is an ultra-rare, complex and devastating neuromuscular disease. Patients display multi-organ symptoms including developmental delays, movement disorders, seizures, constipation and lack of tear production.…
View article: Development of Chemical Entities Endowed with Potent Fast-Killing Properties against <i>Plasmodium falciparum</i> Malaria Parasites
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against <i>Plasmodium falciparum</i> Malaria Parasites Open
One of the attractive properties of artemisinins is their extremely fast-killing capability, quickly relieving malaria symptoms. Nevertheless, the unique benefits of these medicines are now compromised by the prolonged parasite clearance t…
View article: CCDC 1857125: Experimental Crystal Structure Determination
CCDC 1857125: Experimental Crystal Structure Determination Open
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 …
View article: CCDC 1857128: Experimental Crystal Structure Determination
CCDC 1857128: Experimental Crystal Structure Determination Open
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 …
View article: Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis
Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis Open
The leishmaniases are diseases that affect millions of people across the world, in particular visceral leishmaniasis (VL) which is fatal unless treated. Current standard of care for VL suffers from multiple issues and there is a limited pi…
View article: Development of Chemical Proteomics for the Folateome and Analysis of the Kinetoplastid Folateome
Development of Chemical Proteomics for the Folateome and Analysis of the Kinetoplastid Folateome Open
The folate pathway has been extensively studied in a number of organisms, with its essentiality exploited by a number of drugs. However, there has been little success in developing drugs that target folate metabolism in the kinetoplastids.…
View article: Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis
Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis Open
View article: Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies Open
A BioFocus DPI SoftFocus library of ∼35 000 compounds was screened against Mycobacterium tuberculosis (Mtb) in order to identify novel hits with antitubercular activity. The hits were evaluated in biology triage assays to exclude compounds…
View article: Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds Open
In 2010 the identities of thousands of anti-Plasmodium compounds were released publicly to facilitate malaria drug development. Understanding these compounds' mechanisms of action--i.e., the specific molecular targets by which they kill th…