Ocular Toxicity of Mitogen-Activated Protein Kinase Inhibitors
Sign Up to like & getrecommendations! Published in 2017 at "JAMA Oncology"
DOI: 10.1001/jamaoncol.2016.4213
Abstract: Ocular Toxicity of Mitogen-Activated Protein Kinase Inhibitors The Oxford Eye Hospital and the Oxford Experimental Cancer Centre collaborate in monitoring patients in a number of early-phase clinical trials. In this study, we report the ocular… read more here.
Keywords: kinase inhibitors; protein kinase; mitogen activated; activated protein ... See more keywords
An NMR portrait of functional and dysfunctional allosteric cooperativity in cAMP‐dependent protein kinase A
Sign Up to like & getrecommendations! Published in 2023 at "FEBS Letters"
DOI: 10.1002/1873-3468.14610
Abstract: The cAMP‐dependent protein kinase A (PKA) is the archetypical eukaryotic kinase. The catalytic subunit (PKA‐C) structure is highly conserved among the AGC‐kinase family. PKA‐C is a bilobal enzyme with a dynamic N‐lobe, harbouring the Adenosine‐5′‐triphosphate… read more here.
Keywords: cooperativity; protein kinase; kinase; camp dependent ... See more keywords
The protective mechanism of protein kinase R to inhibit neuronal ferroptosis in cerebral injury from subarachnoid hemorrhage
Sign Up to like & getrecommendations! Published in 2022 at "Brain and Behavior"
DOI: 10.1002/brb3.2722
Abstract: Purpose: To investigate the role and mechanism of protein kinase R (PKR) in subarachnoid hemorrhage (SAH)‐mediated ferroptosis. read more here.
Keywords: mechanism protein; subarachnoid hemorrhage; protein kinase; ferroptosis ... See more keywords
Oncogenic functions of protein kinase D2 and D3 in regulating multiple cancer‐related pathways in breast cancer
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DOI: 10.1002/cam4.1938
Abstract: Protein Kinase D (PKD) family contains PKD1, PKD2, and PKD3 in human. Compared to consistent tumor‐suppressive functions of PKD1 in breast cancer, how PKD2/3 functions in breast cancer are not fully understood. In the current… read more here.
Keywords: cancer related; breast cancer; protein kinase; cancer ... See more keywords
AMP‐activated protein kinase is a key regulator of obesity‐associated factors
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DOI: 10.1002/cbf.3767
Abstract: An imbalance between caloric intake and energy expenditure leads to obesity. Obesity is an important risk factor for the development of several metabolic diseases including insulin resistance, metabolic syndrome, type 2 diabetes mellitus, and cardiovascular… read more here.
Keywords: protein kinase; amp activated; activated protein; associated factors ... See more keywords
Slowly on, Slowly off: Bisubstrate‐Analogue Conjugates of 5‐Iodotubercidin and Histone H3 Peptide Targeting Protein Kinase Haspin
Sign Up to like & getrecommendations! Published in 2017 at "ChemBioChem"
DOI: 10.1002/cbic.201600697
Abstract: The atypical protein kinase haspin is a key player in mitosis by catalysing the phosphorylation of Thr3 in histone H3, and thus ensuring the normal function of the chromosomal passenger complex. Here, we report the development… read more here.
Keywords: kinase haspin; kinase; bisubstrate analogue; protein kinase ... See more keywords
Design of Aminobenzothiazole Inhibitors of Rho Kinases 1 and 2 by Using Protein Kinase A as a Structure Surrogate
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DOI: 10.1002/cbic.201700547
Abstract: We describe the design, synthesis, and structure–activity relationships (SARs) of a series of 2‐aminobenzothiazole inhibitors of Rho kinases (ROCKs) 1 and 2, which were optimized to low nanomolar potencies by use of protein kinase A (PKA)… read more here.
Keywords: rho kinases; protein kinase; aminobenzothiazole inhibitors; inhibitors rho ... See more keywords
Characterization of Competitive Inhibitors of Plasmodium falciparum cGMP‐Dependent Protein Kinase **
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DOI: 10.1002/cbic.202100704
Abstract: Plasmodium falciparum cGMP‐dependent protein kinase (PfPKG) is an enticing antimalarial drug target. Novel chemotypes are needed because existing inhibitors have safety issues that may prevent further development. This work demonstrates isoxazole‐based compounds are potent ATP… read more here.
Keywords: plasmodium falciparum; protein kinase; competitive inhibitors; falciparum cgmp ... See more keywords
The role of vasodilator‐stimulated phosphoprotein in podocyte functioning
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DOI: 10.1002/cbin.11149
Abstract: Vasodilator‐stimulated phosphoprotein (VASP) is a 39‐kDa protein belonging to the Ena/VASP protein family, which is involved in adhesion, migration, cell–cell interaction, and regulation of pathways connected with actin cytoskeleton remodeling. VASP is phosphorylated at Tyr39,… read more here.
Keywords: stimulated phosphoprotein; vasodilator stimulated; podocyte; protein kinase ... See more keywords
An Angle on MK2 Inhibition—Optimization and Evaluation of Prevention of Activation Inhibitors
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DOI: 10.1002/cmdc.201900303
Abstract: The mitogen‐activated protein kinase p38α pathway has been an attractive target for the treatment of inflammatory conditions such as rheumatoid arthritis. While a number of p38α inhibitors have been taken to the clinic, they have… read more here.
Keywords: prevention activation; activated protein; mk2; p38 ... See more keywords
Identification of 4-anilino-quin(az)oline as a cell active Protein Kinase Novel 3 (PKN3) inhibitor chemotype.
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DOI: 10.1002/cmdc.202200161
Abstract: Deep annotation of a library of 4-anilinoquinolines led to the identification of 7-iodo- N -(3,4,5-trimethoxyphenyl)quinolin-4-amine 16 as a potent inhibitor (IC 50 = 14 nM) of Protein Kinase Novel 3 (PKN3) with micromolar activity in… read more here.
Keywords: kinase novel; protein kinase; identification; cell ... See more keywords