Potent Pyrimidine and Pyrrolopyrimidine Inhibitors of Testis‐Specific Serine/Threonine Kinase 2 (TSSK2)
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DOI: 10.1002/cmdc.201700503
Abstract: Testis‐specific serine/threonine kinase 2 (TSSK2) is an important target for reversible male contraception. A high‐throughput screen of ≈17 000 compounds using a mobility shift assay identified two potent series of inhibitors having a pyrrolopyrimidine or pyrimidine core.… read more here.
Keywords: specific serine; serine threonine; kinase; pyrimidine ... See more keywords
Targeting the messengers: Serine/threonine protein kinases as potential targets for antimycobacterial drug development
Sign Up to like & getrecommendations! Published in 2018 at "IUBMB Life"
DOI: 10.1002/iub.1871
Abstract: The emergence of increasingly drug‐resistant Mycobacterium tuberculosis strains has become a crucial public health concern. In order to effectively treat tuberculosis, it is imperative to find newer drug targets, which are important for the in… read more here.
Keywords: serine threonine; protein kinases; drug; tuberculosis ... See more keywords
Cerebrospinal fluid amino acids glycine, serine, and threonine in nonketotic hyperglycinemia
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Inherited Metabolic Disease"
DOI: 10.1002/jimd.12500
Abstract: Nonketotic hyperglycinemia (NKH) is caused by deficient glycine cleavage enzyme activity and characterized by elevated brain glycine. Metabolism of glycine is connected enzymatically to serine through serine hydroxymethyltransferase and shares transporters with serine and threonine.… read more here.
Keywords: serine threonine; glycine serine; nkh patients; serine ... See more keywords
Allosteric Small-Molecule Serine/Threonine Kinase Inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Advances in experimental medicine and biology"
DOI: 10.1007/978-981-13-8719-7_11
Abstract: Deregulation of protein kinase activity has been linked to many diseases ranging from cancer to AIDS and neurodegenerative diseases. Not surprisingly, drugging the human kinome - the complete set of kinases encoded by the human… read more here.
Keywords: kinase inhibitors; serine threonine; kinase; atp binding ... See more keywords
Species-specific serine-threonine protein kinase Pkb2 of Bifidobacterium longum subsp. longum: Genetic environment and substrate specificity.
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DOI: 10.1016/j.anaerobe.2018.03.003
Abstract: The objective of this study was to determine for phosphorylated substrates of the species-specific serine-threonine protein kinase (STPK) Pkb2 from Bifidobacterium longum subsp. longum GT15. Two approaches were employed: analyses of phosphorylated membrane vesicles protein… read more here.
Keywords: protein; serine threonine; atpase; species specific ... See more keywords
The serine/threonine protein phosphatase 2A controls autoimmunity.
Sign Up to like & getrecommendations! Published in 2018 at "Clinical immunology"
DOI: 10.1016/j.clim.2017.07.012
Abstract: Protein phosphatase 2A (PP2A) is the first serine/threonine phosphatase recognized to contribute to human and murine lupus immunopathology. PP2A expression in SLE is controlled both epigenetically and genetically, and it is increased in patients with… read more here.
Keywords: threonine protein; serine threonine; phosphatase; protein phosphatase ... See more keywords
The serine/threonine phosphatase DhSIT4 modulates cell cycle, salt tolerance and cell wall integrity in halo tolerant yeast Debaryomyces hansenii.
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DOI: 10.1016/j.gene.2016.12.022
Abstract: The highly conserved family of Phosphoprotein phosphatases (PPP) regulates several major physiological processes in yeast. However, very little is known about the PPP orthologs from the yeast species inhabiting extreme environmental niches. In the present… read more here.
Keywords: serine threonine; cell cycle; dhsit4; cell wall ... See more keywords
Deletion of serine/threonine-protein kinase pknL from Mycobacterium tuberculosis reduces the efficacy of isoniazid and ethambutol.
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DOI: 10.1016/j.tube.2021.102066
Abstract: Serine/threonine-protein kinases in Mycobacterium tuberculosis (Mtb) form a preeminent regulatory system required to establish and maintain the infection in the host. Herein, we sought to decipher the biological role of PknL with the help of… read more here.
Keywords: serine threonine; isoniazid ethambutol; tuberculosis; threonine protein ... See more keywords
Strategies for Targeting Serine/Threonine Protein Phosphatases with Small Molecules in Cancer.
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DOI: 10.1021/acs.jmedchem.1c00631
Abstract: Among numerous posttranslational regulation patterns, phosphorylation is reversibly controlled by the balance of kinases and phosphatases. The major form of cellular signaling involves the reversible phosphorylation of proteins on tyrosine, serine, or threonine residues. However,… read more here.
Keywords: serine threonine; small molecules; targeting serine; phosphatases small ... See more keywords
Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-a]pyrimidine-Based Macrocycles.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00173
Abstract: Serine/threonine kinase 17A (death-associated protein kinase-related apoptosis-inducing protein kinase 1─DRAK1) is a part of the death-associated protein kinase (DAPK) family and belongs to the so-called dark kinome. Thus, the current state of knowledge of the… read more here.
Keywords: threonine kinase; pyrazolo pyrimidine; kinase 17a; kinase ... See more keywords
Discovery of Potent and Selective Receptor-Interacting Serine/Threonine Protein Kinase 2 (RIPK2) Inhibitors for the Treatment of Inflammatory Bowel Diseases (IBDs).
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00604
Abstract: Receptor-interacting serine/threonine protein kinase 2 (RIPK2) has been demonstrated to be a promising target for treating inflammatory diseases. Herein, we describe the discovery and optimization of a series of RIPK2 inhibitors derived from an FLT3… read more here.
Keywords: protein kinase; kinase ripk2; receptor interacting; interacting serine ... See more keywords