Sameek Singh
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View article: Non-Enzymatic Structural Modifications Reshape Peptide Presentation and Antigen Recognition
Non-Enzymatic Structural Modifications Reshape Peptide Presentation and Antigen Recognition Open
For cytotoxic T-cells to identify and eliminate infected and transformed cells, the adaptive immune system requires the presentation of antigenic peptides by major histocompatibility complex class I (MHC-I) molecules. These peptides, typic…
View article: Phosphorylation-Inducing Molecules for Regulating Dynamic Cellular Processes
Phosphorylation-Inducing Molecules for Regulating Dynamic Cellular Processes Open
Dynamic cellular processes often employ protein phosphorylation for rapid information transfer within and between cells. Phosphorylation-inducing chimeric small molecules (PHICS) have been developed for targeted protein phosphorylation by …
View article: Proximity-induced rewiring of oncogenic kinase triggers apoptosis
Proximity-induced rewiring of oncogenic kinase triggers apoptosis Open
The active site’s electric field is integral to enzymatic catalysis (e.g., substrate recognition) and nature employs charge-altering post-translational modifications (e.g., phosphorylation) to perturb this electric field and regulate enzym…
View article: Orthogonal resistance mechanisms of classical- and induced-proximity inhibitors
Orthogonal resistance mechanisms of classical- and induced-proximity inhibitors Open
Resistance development is an inevitable failure mode of many drugs, pointing to the need to develop agents with orthogonal resistance mechanisms. Induced-proximity modalities, an emergent class of therapeutics, operate by forming a ternary…
View article: Phosphorylation-inducing molecules for regulating dynamic cellular processes
Phosphorylation-inducing molecules for regulating dynamic cellular processes Open
Dynamic cellular processes often employ protein phosphorylation for rapid information transfer within and between cells. Phosphorylation-inducing chimeric small molecules (PHICS) have been developed for targeted protein phosphorylation by …
View article: Development and Applications of Chimera Platforms for Tyrosine Phosphorylation
Development and Applications of Chimera Platforms for Tyrosine Phosphorylation Open
Chimeric small molecules that induce post-translational modification (PTM) on a target protein by bringing it into proximity to a PTM-inducing enzyme are furnishing novel modalities to perturb protein function. Despite recent advances, suc…
View article: Novel Cannabinoid Receptor 2 (CB2) Low Lipophilicity Agonists Produce Distinct cAMP and Arrestin Signalling Kinetics without Bias
Novel Cannabinoid Receptor 2 (CB2) Low Lipophilicity Agonists Produce Distinct cAMP and Arrestin Signalling Kinetics without Bias Open
Cannabinoid Receptor 2 (CB2) is a promising target for treating inflammatory diseases. We designed derivatives of 3-carbamoyl-2-pyridone and 1,8-naphthyridin-2(1H)-one-3-carboxamide CB2-selective agonists with reduced lipophilicity. The ne…
View article: Development and applications of chimera platforms for tyrosine phosphorylation
Development and applications of chimera platforms for tyrosine phosphorylation Open
Chimeric small molecules that induce post-translational modification (PTM) on a target protein by bringing it in proximity to a PTM-inducing enzyme are furnishing novel modalities to perturb protein function. Despite recent advances, such …
View article: Development of selective, fluorescent cannabinoid type 2 receptor ligands based on a 1,8-naphthyridin-2-(1<i>H</i>)-one-3-carboxamide scaffold
Development of selective, fluorescent cannabinoid type 2 receptor ligands based on a 1,8-naphthyridin-2-(1<i>H</i>)-one-3-carboxamide scaffold Open
High affinity, cannabinoid type 2 receptor selective ligand.
View article: Development of fluorescent ligands for A1 adenosine receptor and cannabinoid receptors
Development of fluorescent ligands for A1 adenosine receptor and cannabinoid receptors Open
Adenosine A1 receptor (A1AR), cannabinoid type 1 receptor (CB1R) and cannabinoid type 2 receptor (CB2R) are class A G protein-coupled receptors (GPCRs) and play important roles in human pathophysiological conditions such as cardiovascular,…
View article: Synthesis of novel (benzimidazolyl)isoquinolinols and evaluation as adenosine A1 receptor tools
Synthesis of novel (benzimidazolyl)isoquinolinols and evaluation as adenosine A1 receptor tools Open
Mild, metal free aromatization of tetrahydroisoquinolinols. Synthesis of (benzimidazolyl)isoquinolinols.
View article: Chemical Tools for Studying Lipid-Binding Class A G Protein–Coupled Receptors
Chemical Tools for Studying Lipid-Binding Class A G Protein–Coupled Receptors Open