Vojtěch Duchoslav
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View article: SPR is a fast and straightforward method to estimate the binding constants of cyclic dinucleotides to their binding partners, such as STING or poxin
SPR is a fast and straightforward method to estimate the binding constants of cyclic dinucleotides to their binding partners, such as STING or poxin Open
The development of small molecule drugs that target protein binders is the central goal in medicinal chemistry. During the lead compound development process, hundreds or even thousands of compounds are synthesized, with the primary focus o…
View article: Fluorinated cGAMP analogs, which act as STING agonists and are not cleavable by poxins: Structural basis of their function
Fluorinated cGAMP analogs, which act as STING agonists and are not cleavable by poxins: Structural basis of their function Open
The cGAS-STING pathway is a crucial part of innate immunity; it serves to detect DNA in the cytoplasm and to defend against certain cancers, viruses, and bacteria. We designed and synthesized fluorinated carbocyclic cGAMP analogs, MD1203 a…
View article: Fluorinated cGAMP analogs, which act as STING agonists and are not cleavable by poxins: structural basis of their function
Fluorinated cGAMP analogs, which act as STING agonists and are not cleavable by poxins: structural basis of their function Open
The Stimulator of Interferon Genes (STING) plays a crucial role in the cGAS-STING pathway of innate immunity, detecting DNA in the cytoplasm and defending against certain cancers, viruses, and bacteria. We designed and synthesized fluorina…
View article: Structure of monkeypox virus poxin: implications for drug design
Structure of monkeypox virus poxin: implications for drug design Open
Monkeypox, or mpox, is a disease that has recently resurfaced and spread across the globe. Despite the availability of an FDA-approved vaccine (JYNNEOS) and an effective drug (tecovirimat), concerns remain over the possible recurrence of a…
View article: Discovery of Novel Human Constitutive Androstane Receptor Agonists with the Imidazo[1,2-<i>a</i>]pyridine Structure
Discovery of Novel Human Constitutive Androstane Receptor Agonists with the Imidazo[1,2-<i>a</i>]pyridine Structure Open
The nuclear constitutive androstane receptor (CAR, NR1I3) plays significant roles in many hepatic functions, such as fatty acid oxidation, biotransformation, liver regeneration, as well as clearance of steroid hormones, cholesterol, and bi…
View article: Localization of SARS-CoV-2 Capping Enzymes Revealed by an Antibody against the nsp10 Subunit
Localization of SARS-CoV-2 Capping Enzymes Revealed by an Antibody against the nsp10 Subunit Open
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent of the coronavirus disease-19 pandemic. One of the key components of the coronavirus replication complex are the RNA methyltransferases (MTases), RNA-modif…
View article: Affinity switching of the LEDGF/p75 IBD interactome is governed by kinase-dependent phosphorylation
Affinity switching of the LEDGF/p75 IBD interactome is governed by kinase-dependent phosphorylation Open
Significance The transcription coactivator LEDGF/p75 contributes to regulation of gene expression by tethering other factors to actively transcribed genes on chromatin. Its chromatin-tethering activity is hijacked in two important disease …