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PubMed Journals Articles About "Mitogen Activated Protein Kinase Kinase MAP2K Inhibitors Pipeline" RSS

00:00 EST 16th February 2019 | BioPortfolio

Mitogen Activated Protein Kinase Kinase MAP2K Inhibitors Pipeline PubMed articles on BioPortfolio. Our PubMed references draw on over 21 million records from the medical literature. Here you can see the latest Mitogen Activated Protein Kinase Kinase MAP2K Inhibitors Pipeline articles that have been published worldwide.

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Showing "Mitogen Activated Protein Kinase Kinase MAP2K Inhibitors Pipeline" PubMed Articles 1–25 of 22,000+

Mitogen and stress- activated protein kinase regulated gene expression in cancer cells.

The mitogen- and stress-activated protein kinases activated by the extracellular-signal-regulated kinase 1/2 and/or stress-activated protein kinase 2/p38 mitogen-activated protein kinase pathways are recruited to the regulatory region of a subset of genes termed immediate-early genes, often leading to their induction. These genes, many of which code for transcription factors, have been directly linked to the phenotypic events in carcinogenesis. In this paper, we focus on the mitogen- and stress-activated pr...


Engineering a Protein Binder Specific for p38α with Interface Expansion.

Protein binding specificities can be manipulated by redesigning contacts that already exist at an interface or by expanding the interface to allow interactions with residues adjacent to the original binding site. Previously, we developed a strategy, called AnchorDesign, for expanding interfaces around linear binding epitopes. The epitope is embedded in a loop of a scaffold protein, in our case a monobody, and then surrounding residues on the monobody are optimized for binding using directed evolution or com...

Regulation of human mitogen-activated protein kinase 15 (extracellular signal-regulated kinase 7/8) and its functions: A recent update.

Mitogen-activated protein kinase 15 (MAPK15), originally also known as extracellular signal-regulated kinase 7/8, is the most recently identified atypical MAPK and the least studied so far. Examinations of the role of MAPK15 in various cell lines and model systems indicate that MAPK15 participates in a variety of cellular activities such as promoting cell proliferation, cell transformation, and apoptosis; stimulating autophagy; regulating cell division, ciliogenesis, and protein secretion; and maintaining g...


Autophagic cell death associated to Sorafenib in renal cell carcinoma is mediated through Akt inhibition in an ERK1/2 independent fashion.

To fully clarify the role of Mitogen Activated Protein Kinase in the therapeutic response to Sorafenib in Renal Cell Carcinoma as well as the cell death mechanism associated to this kinase inhibitor, we have evaluated the implication of several Mitogen Activated Protein Kinases in Renal Cell Carcinoma-derived cell lines.

1,2,4-Trisubstituted imidazolinones with dual carbonic anhydrase and p38 mitogen-activated protein kinase inhibitory activity.

Various 1,2,4 trisubstituted imidazolin-5-one derivatives were synthesized and evaluated for their inhibitory activity against p38 mitogen-activated protein kinase (p38MAPK) and carbonic anhydrase (CA) enzymes aiming to explore potential dual inhibitors. Results revealed that compounds 3c, 3g, 3h, 4a, 6c and 6d were the most effective derivatives against p38αMAPK (IC = 0.14, 0.14, 0.056, 0.14, 0.13 and 0.14 μM, respectively) compared to sorafenib (IC = 1.58 μM) as standard drug. On the other ...

MAPK signaling pathway and erectile dysfunction.

The MAPK signaling pathway plays a key role in the differentiation, proliferation and apoptosis of cells, and its family members mainly include extracellular signal-regulated kinase (ERK), stress-activated protein kinase (JNK), and p38 mitogen-activated protein kinase (p38MAPK). Recent studies have shown that the ERK, JNK and p38MAPK signaling pathways are closely associated with the development and progression of erectile dysfunction (ED). This review focuses on the correlation between the MAPK signaling p...

Synthesis and Biological Evaluation of 3-Arylindazoles as Selective MEK4 Inhibitors.

Herein we report the discovery of a novel series of highly potent and selective mitogen-activated protein kinase kinase 4 (MEK4) inhibitors. MEK4 is an upstream kinase in MAPK signalling pathways that phosphorylates p38 MAPK and JNK in response to mitogenic and cellular stress queues. MEK4 is over-expressed and induces metastasis in advanced prostate cancer lesions. However, the value of MEK4 as an oncology target has not been pharmacologically validated because selective chemical probes targeting MEK4 have...

Hypoxia Activated Prodrugs of PERK Inhibitors.

Tumour hypoxia plays an important role in tumour progression and resistance to therapy. Under hypoxia unfolded proteins accumulate in the endoplasmic reticulum (ER) and this stress is relieved through the protein kinase R-like ER kinase (PERK) signalling arm of the unfolded protein response (UPR). Targeting the UPR through PERK kinase inhibitors provides tumour growth inhibition, but also elicits on-mechanism normal tissue toxicity. Hypoxia presents a target for tumour-selective drug delivery using hypoxia-...

Synergistic effects of cAMP-dependent protein kinase A and AMP-activated protein kinase on lipolysis in kinsenoside-treated C3H10T1/2 adipocytes.

We previously showed that 3-O-β-D-glucopyranosyl-(3R)-hydroxybutanolide (kinsenoside), a major compound of Anoectochilus formosanus, increased lipolysis through an AMP-activated protein kinase (AMPK)-dependent pathway.

Safety and Tolerability of Anaplastic Lymphoma Kinase Inhibitors in Non-Small-Cell Lung Cancer.

The chimeric protein echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase, resulting from the rearrangement of the homonym genes, is one of the currently targetable oncogenic drivers in anaplastic lymphoma kinase-positive non-small-cell lung cancer. In fact, four first- and second-generation anaplastic lymphoma kinase tyrosine kinase inhibitors, crizotinib (PF-02341066), ceritinib (LDK378), alectinib (CH5424802), and brigatinib (AP26113), are presently approved for clinical practice; ...

Mitogen-activated protein kinase kinase 6 negatively regulates anthocyanin induction in Arabidopsis.

Arabidopsis mitogen-activated protein (MAP) kinase kinase 6 (MKK6) has previously been shown to play important roles in plant immunity and cytokinesis. Here we report that it is also involved in the negative regulation of anthocyanin biosynthesis in Arabidopsis. Elevated anthocyanin levels are observed in mkk6 knock out mutant plants. RNA-sequencing analysis revealed that the expression level of MYB75 (Myb transcription factor 75), which encodes a key positive regulator of anthocyanin biosynthesis, is up-re...

MIP-1α induces inflammatory responses by upregulating chemokine receptor 1/chemokine receptor 5 and activating c-Jun N-terminal kinase and mitogen-activated protein kinase signaling pathways in acute pancreatitis.

We aimed to investigate the association of macrophage inflammatory protein (MIP)-1α (CCL3) expression with the severity of acute pancreatitis (AP).

p38 mitogen activated protein kinase mediates cardiac Na+/H+ exchanger inhibition induced by Sildenafil.

Since the original description as potent antianginal compounds, phosphodiesterase 5A inhibitors have continuously increased their possible therapeutic applications. In the heart, Sildenafil was shown to protect against an ischemic insult by decreasing cardiac Na/H exchanger (NHE1) activity, action that was mediated by protein kinase G. p38 mitogen activated protein kinase (p38MAPK) activation was described in cardiac ischemia, but its precise role remains elusive. It has been shown that p38MAPK is activated...

Cell-permeable p38 MAP kinase protects adult hippocampal neurons from cell death.

p38 mitogen-activated protein (MAP) kinase (p38) is a member of the MAP kinase family. Previous reports using p38 chemical inhibitors have suggested that its activation contributes to hippocampal neuronal cell death rather than cell survival. In this study, we used both a cell-permeable p38 protein containing the HIV protein transduction domain (PTD) and cultured adult hippocampal neurons, which were differentiated from cultured adult hippocampal neural stem/progenitor cells (NPCs), to evaluate the direct f...

3β,23,28-Trihydroxy-12-oleanene 3β-caffeate from Desmodium sambuense induced neurogenesis in PC12 cells mediated by ER stress and BDNF-TrkB signalling pathways.

3β,23,28-Trihydroxy-12-oleanene 3β-caffeate (compound 1) is a neuritogenic pentacyclic triterpenoid, which was isolated from Desmodium sambuense based on a PC12 cell bioassay system. Compound 1 induced neurite outgrowth dose-dependently in PC12 cells and primary cortical neurons at doses of 0.1, 0.3 and 1 μM. The potential target of compound 1 was predicted by ChemProteoBase profiling, and the mechanism of action was investigated using specific inhibitors, western blot analysis, and PC12 (rasN17) and PC1...

Evaluation of MBP tagged-hATR kinase domain catalytic activity with p53 Ser-15 phosphorylation.

DNA damage response (DDR) pathways form an integral part of the body's repair machinery and Ataxia telangiectasia mutated and Rad-3 related (ATR) is one of the key mediators in DDR pathway. Increasing evidence suggests that inhibition of ATR can help sensitize tumor cells towards combinatorial treatment. However, specific ATR kinase inhibitors have largely remained elusive till date. Despite much interest in the protein for more than a decade, there has been little characterization available for the kinase ...

CaMKK2 kinase domain interacts with the autoinhibitory region through the N-terminal lobe including the RP insert.

Calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2), a member of the Ca⁠/calmodulin-dependent kinase (CaMK) family, functions as an upstream activator of CaMKI, CaMKIV and AMP-activated protein kinase. Thus, CaMKK2 is involved in the regulation of several key physiological and pathophysiological processes. Previous studies have suggested that Ca/CaM binding may cause unique conformational changes in the CaMKKs compared with other CaMKs. However, the underlying mechanistic details remain unclear.

microRNA-542-5p protects against acute lung injury in mice with severe acute pancreatitis by suppressing the mitogen-activated protein kinase signaling pathway through the negative regulation of P21-activated kinase 1.

Severe acute pancreatitis (SAP) is a condition associated with high rates of mortality and lengthy hospital stays. In the current study, SAP mouse models were established in BALB/c wild-type and P21-activated kinase 1 (PAK1) knockdown mice with the objective of determining the expression of microRNA-542-5p (miR-542-5p) and the subsequent elucidation of the mechanism by which it influences acute lung injury (ALI) by mediating mitogen-activated protein kinase (MAPK) signaling and binding to PAK1. The targeti...

Phase II Trial of MEK Inhibitor Binimetinib (MEK162) in RAS-mutant Acute Myeloid Leukemia.

Relapsed and refractory (R/R) acute myeloid leukemia (AML) continues to be a therapeutic challenge with poor outcomes. Dysregulation of the mitogen-activated protein (MAP) kinase/extracellular-signal regulated kinase (ERK) pathway frequently occurs in AML and myelodysplastic syndrome (MDS). Preclinical studies and early-phase trials have shown promise for MAP-ERK kinase (MEK) inhibition in AML. We evaluated the safety and efficacy of the MEK 1/2 inhibitor binimetinib in advanced myeloid malignancies.

Epithelial-Immune Cell Interactions for Drug Discovery in Chronic Obstructive Pulmonary Disease.

New studies of chronic obstructive pulmonary disease (COPD) are revealing the key role of airway epithelial cells and innate immune cells in the initiation, exacerbation, and progression of airway disease. An emerging scheme focuses on expansion of airway progenitor epithelial cells that feed forward for a type 2 immune response and consequent IL-13-driven mucus production that is linked to the morbidity and mortality of COPD. Analysis of human airway progenitor epithelial cells and airway tissue shows that...

Aflatoxin-induced upregulation of protein arginine methyltransferase 5 is mediated by protein kinase C and extracellular signal-regulated kinase.

Aflatoxins are fungal metabolites classified into four major groups such as B, B, G, and G. These natural aflatoxins are designated as group I carcinogen by the International Agency for Research on Cancer. Among these, the aflatoxin B is more potent. Protein arginine methyltransferase 5, an epigenetic modulator, emerged as an oncoprotein, is overexpressed in diverse forms of cancers. The present study aims to explore the AFB-mediated overexpression of PRMT5. The AFB at nanomolar concentrations increased the...

Lithium interacts with cardiac remodeling: the fundamental value in the pharmacotherapy of bipolar disorder.

Patients with bipolar disorder (BD) have an increased risk of cardiovascular morbidity and mortality during the course of their illness. For over half a century, lithium has been the gold-standard medication used to treat the mood burdens of BD. In addition, lithium possesses several biological effects that may modulate cardiovascular risk in patients with BD. In this review, we update the current knowledge of cellular and molecular mechanisms underlying the possible cardiac actions of lithium. The mechanis...

Measurements of Photoreaction and Kinase Activity of Phototropin, a Photoreceptor Protein for Tropic Response in Plants: Involvement of Kinase Activity in the Photosensitivity of Tropic Response.

Phototropin is a photoreceptor protein responsible for phototropic responses in plants. A phototropin molecule has two photoreceptive domains named LOV1 and LOV2 in the N-terminal region. Blue light absorbed by a chromophore in these domains triggers conformational changes in the protein moiety. The C-terminal region of phototropin forms a Ser/Thr kinase that is activated by these conformational changes. The activated phototropin kinase transmits signals downstream leading to tropic responses. The lifetime ...

PKC and PKN in heart disease.

The protein kinase C (PKC) and closely related protein kinase N (PKN) families of serine/threonine protein kinases play crucial cellular roles. Both kinases belong to the AGC subfamily of protein kinases that also include the cAMP dependent protein kinase (PKA), protein kinase B (PKB/AKT), protein kinase G (PKG) and the ribosomal protein S6 kinase (S6K). Involvement of PKC family members in heart disease has been well documented over the years, as their activity and levels are mis-regulated in several patho...

Protein kinase A (PKA) inhibition reduces human aortic smooth muscle cell calcification stimulated by inflammatory response and inorganic phosphate.

Smooth muscle cells (SMCs) play a role in medial vascular calcification, which can be stimulated by high levels of serum phosphate and inflammatory mediators. The aim of this study was to investigate whether mitogen-activated protein kinases (MAPKs) (p38 MAPK, ERK1/2, and JNK) and protein kinase A (PKA) can participate in inorganic phosphate (Pi)- and inflammation response-stimulated SMC calcification.


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