Selectively upregulating proapoptotic proteins. Medical search. Frequent questions

BH3-only proteins are subject to stringent control but develop into transcriptionally upregulated andor posttranslationally modified in response to proapoptotic signals, thereby gaining their full apoptotic prospective (29). (axlinhibitor.com)
Furthermore, the Spätzle (Spz) family ligands for the Toll receptor are transcriptionally upregulated by activated JNK signalling in a non-cell-autonomous manner, providing a molecular mechanism for JNK-induced Toll pathway activation. (sdbonline.org)

BIK selectively inhibits the prosurvival BCL-XL, BFL-1, and BCL-w (35) and has been shown to sensitize tumor cells to apoptosis mediated by a variety of therapeutic agents (368) by a mechanism that is definitely dependent on its BH3 domain (39). (axlinhibitor.com)
It has been shown that, due to its α -tocopheryl moiety, the agent activates protein phosphatase-2A that, in turn, inhibits protein kinase C (PKC). (nature.com)
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ ABL , v-Abl , PDGFR and c-kit kinase activity. (medchemexpress.com)
WT161 selectively inhibits HDAC6 that exhibits effective anti-tumor activities in multiple myeloma. (csnpharm.cn)

Under cell stress conditions, the growth arrest and DNA damage 45 beta (Gadd45ß) protein will interact with MAPK/ERK kinase kinase 4 (MEKK4) to form the Gadd45ß-MEKK4 signaling complex. (wikipedia.org)
GS-002 also induced endoplasmic reticular (ER) stress as evidenced by increases in ER stress-responsive proteins including glucose-regulated protein 78 (GRP78), growth arrest- and DNA damage-inducible gene 153 (GADD153), phosphorylated eukaryotic initiation factor 2 α (eIF2 α ), phosphorylated protein endoplasmic-reticular-resident kinase (PERK), and ATF-3. (hindawi.com)
The induction of ATF-3 expression was mediated by mitogen-activated protein kinase (MAPK) signaling pathways in GS-002-treated cells. (hindawi.com)
However, recent studies have suggested that BRAFi/MEKi and ERK1/2i resistance can arise through activation of a parallel signalling pathway leading to activation of ERK5, an unusual protein kinase that contains both a kinase domain and a transcriptional transactivation domain. (babraham.ac.uk)
Background Pilocytic astrocytoma (PA) is the most common pediatric brain tumor and a mitogen-activated protein kinase (MAPK)-driven disease. (ibecbarcelona.eu)
CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. (medchemexpress.com)
Experimentalists are similarly afflicted: while trying to identify LMs, they are likely to spend a lot of resources, time and ACY-1215 kinase inhibitor effort carrying out experiments within the false motif candidates, which usually vastly outnumber the genuine ones in any set of proteins of interest (1). (insulin-receptor.info)

Furthermore, ATG5 is capable of translocating to the nucleus and interacting with survivin to disturb chromosome segregation by antagonistically competing with the ligand Aurora B. As a key regulator of autophagy, any suppression of the ATG5 protein or loss-of-function mutations in the ATG5 gene will negatively affect autophagy. (wikipedia.org)
Downregulation of ATG5 protein and mutations in the Atg5 gene have also been linked with prostate, gastrointestinal and colorectal cancers as ATG5 plays a role in both cell apoptosis and cell cycle arrest. (wikipedia.org)
These molecules are able to oxidize cellular macromolecules and DNA, potentially resulting in damage and mutations to proteins and genes that usually manage cell growth, proliferation or apoptosis. (5dok.net)
Conventional molecular target drugs can selectively inhibit gene mutations which activate prolifiration of cancer cells, but many patients in which gene mutations cannot be detected are not targets of the molecular target drugs. (justia.com)
Scope includes mutations and abnormal protein expression. (cancerindex.org)

One of such pro-apoptotic gene families is the Secreted Frizzled-Related protein (sFRPs) family, an antagonist of the Wnt signalling pathway. (biomedcentral.com)

In the GC atmosphere, only these B cells that express the highest-affinity immunoglobulins are rescued from stringent proapoptotic pathways that signal by way of transforming development aspect (TGF- ) (22, 23), FAS (24, 25), and B-cell receptors (26). (axlinhibitor.com)
The involvement of multiple signaling pathways (NF-κB and JNK) and proteins (EGF-R, Id-1 and Id-3) was suggested to explain the antiproliferative effect of GTT in prostate cancer (PCa) cells [ 14 ]. (biomedcentral.com)
What pathways are this gene/protein implicaed in? (cancerindex.org)

This complex then activates and selectively targets p38 MAPK to the autophagosome to phosphorylate ATG5 at threonine 75. (wikipedia.org)

Recent efforts in personalizing anti-cancer treatments have focused on therapies that selectively reactivate apoptosis within malignant cells, such as those that promote apoptosis via the Bcl-2 family of regulatory proteins and those that act by binding to death receptors expressed on the surface of the cell. (radarcon2008.org)
However, useful advances are now being made in the bioinformatics tools that address the amazing modularity of eukaryotic regulatory proteins. (insulin-receptor.info)

The diversified effects of cannabinoids are now known to be mediated through the activation of G-protein-coupled receptors that are normally bound by a family of endogenous ligands, the endocannabinoids ( 1 ). (aacrjournals.org)
Immunoglobulin E (IgE) is usually a glycosylated protein belonging to the immunoglobulin family and plays Ginsenoside Rg3 a central role in allergic disease, exerting its effector functions through two receptors: FcRI and CD23 [2]. (treatmentforprostatecancer.info)
This gene encodes a member of the beta chemokine receptor family, which is predicted to be a seven transmembrane protein similar to G protein-coupled receptors. (cancerindex.org)

Small molecules that antagonize pro-survival Bcl-2 proteins, namely BH3 mimetics, are currently under pre-clinical and clinical evaluation as single agent anti-cancer therapies and as sensitizers to apoptosis-inducing drugs [33, 34]. (radarcon2008.org)

To determine the antiproliferative effect of gamma-tocotrienol (GTT) treatment on differential protein expression in HepG2 cells. (biomedcentral.com)
Combinatorial effect of QUE and resveratrol has been found to be antiproliferative via suppression of oncogenic microRNA-27a and induction of zinc finger protein ZBTB10 against HT-29 colon cancer (Del Follo-Martinez et al. (pi3k-inhibitors.com)
JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor with improved antiproliferative and proapoptotic activities over SAHA and ruxolitinib in several hematological cell lines. (csnpharm.cn)

In response to DNA damage, ATG5 expression is upregulated, increasing autophagy, preventing caspase activation and apoptosis. (wikipedia.org)
Bcl-2 proteins are vital for setting the threshold of resistance to apoptosis and initiating the apoptotic cascade, and members are grouped mainly by reference to distinct Bcl-2 homology (BH) domains (to get a assessment, see reference 27). (axlinhibitor.com)
Further, we studied the effect of HSP70-2 protein ablation on signaling cascades involved in apoptosis, cell cycle and Epithelial-Mesenchymal-Transition both in culture as well as in-vivo human breast xenograft mouse model. (biomedcentral.com)
Activating transcription factor-(ATF-) 3, a stress-inducible transcription factor, is rapidly upregulated under various stress conditions and plays an important role in inducing cancer cell apoptosis. (hindawi.com)
Other mechanisms of TRAIL and TMZ resistance are shared, such as an up-regulation of anti-apoptotic and down-regulation of pro-apoptotic Bcl-2 proteins and an over-expression of inhibitor of apoptosis AZD 7545 (IAP) proteins [23, 32]. (radarcon2008.org)
These findings indicate that MUC16 protects EOC cells against TRAIL-induced apoptosis through multiple mechanisms including the blockade of TRAIL R2 expression and the regulation of cFLIP expression at both the transcriptional and the protein level. (biomedcentral.com)

BIK is upregulated in B cells following antigen receptor stimulation (40, 41) and is vital for the apoptotic collection of mature B lymphocytes. (axlinhibitor.com)
The ligand of this receptor is macrophage inflammatory protein 3 alpha (MIP-3 alpha). (cancerindex.org)

Autophagy related 5 (ATG5) is a protein that, in humans, is encoded by the ATG5 gene located on Chromosome 6. (wikipedia.org)
As a result, deficiencies in the ATG5 protein and variations in the gene have been associated with various inflammatory and degenerative diseases as aggregates of ubiquitinated targets are not cleared out via autophagy. (wikipedia.org)
Alternatively spliced transcript variants that encode the same protein have been described for this gene. (cancerindex.org)
What does this gene/protein do? (cancerindex.org)
Mechanistically, the CCL20/CCR6 signaling pathway upregulates HIF-1α by stimulating nuclear factor kappa B-driven transactivation of the HIF1A gene. (cancerindex.org)
Midostaurin also upregulates endothelial nitric oxide synthase ( eNOS ) gene expression. (medchemexpress.com)

Programmed Cell Death Protein 4 (PDCD4) is known to inhibit ATG5 expression via inhibition of protein translation. (wikipedia.org)
A set of twenty-five thioxanthene-9-one and xanthene-9-one derivatives, that were previously shown to inhibit cholinesterases (ChEs) and amyloid β (Aβ40) aggregation, were evaluated for the inhibition of tau protein aggregation. (ibecbarcelona.eu)

Two decades later, pioneering studies suggested that lectin-like molecules constitutively expressed on the surface of macrophages can selectively recognize changes on glycans decorating the surface of apoptotic thymocytes, 4 , 5 although these studies likewise did not provide substantial insight into the mechanisms by which lectin-glycan interactions regulate cell death. (nature.com)
The secreted Frizzled-Related Protein (sFRP) family is pro-apoptotic and also a negative modulator of the Wnt signalling cascade. (biomedcentral.com)

Glycans, either alone or complexed with glycan-binding proteins, can deliver intracellular signals or control extracellular processes that promote initiation, execution and resolution of cell death programs. (nature.com)
The MUC16CTD anchors the protein at the cell surface and consists of a 229 amino acid extracellular region containing a potential proteolytic cleavage site, a 23 residue transmembrane domain, and a 31 amino acid cytoplasmic tail. (biomedcentral.com)
They can be found in telomeric proteins (6), in proteins of the extracellular matrix (7)and seemingly every macromolecular complex in between. (insulin-receptor.info)

CD23 belongs to the C\type (calcium\dependent) lectin\like (CTLD) superfamily of proteins and is a trimer in its membrane\bound form. (treatmentforprostatecancer.info)

HMOX2 is constitutively expressed to encode a 36 kDa HO-2 protein, mainly functioning to maintain the basal heme metabolism and may also play a role in inflammatory responses [ 4 ] . (encyclopedia.pub)

It also downregulated the expression of glial fibrillary acidic protein and reduced retinal reactive gliosis. (molvis.org)
However, activation of heme oxygenase-1 (HO-1) can upregulate ferritin expression, which binds to ferrous iron and detoxifies its pro-oxidant effect. (encyclopedia.pub)
In MDA-MB-231 cells, treatment by tocotrienols led to several fold increase of NRF2 expression marked by corresponding decrease in Kelch-like ECH-associated protein 1 (KEAP1) levels [ 15 ]. (biomedcentral.com)
18 ]. They reported that the expression of Prx1 and Prx6 is selectively regulated in alveolar type II cells isolated from vitamin E-depleted rats, depending on the severity of oxidative load. (biomedcentral.com)
Conversely, HRS decreased Bcl2-associated X protein expression, cleaved caspase-3, and oxidant-stress product malondialdehyde (MDA) in a Sirt1-dependent manner. (arvojournals.org)
In the present study, we have investigated the possible association of HSP70-2 mRNA and protein expression with various stages, grades and histotypes of breast cancer patients. (biomedcentral.com)

When this conversion occurs in the coding region of mRNA, it results in an altered nucleotide codon and, therefore, can change the amino acid sequence of the coded protein in what is referred to as a re-coding editing event. (biomedcentral.com)

Overexpression of the RNA-binding protein HuR (ELAVL1) occurs during colon tumorigenesis and is abnormally present within the cytoplasm, where it post-transcriptionally regulates genes through its interaction with 3'UTR AU-rich elements (AREs). (oncotarget.com)

The so-called BH3-only proteins are proapoptotic and bind via their short -helical BH3 domain to prosurvival Bcl-2 family members, and this interaction is essential for their ability to kill cells (28). (axlinhibitor.com)

HepG2 cells were treated with 70 μM GTT for 48 hours and differentially expressed protein spots were determined by two-dimensional electrophoresis (2DE), identified by MALDI-TOF mass spectrometer (MS) and validated by quantitative real-time polymerase chain reaction (qRT-PCR). (biomedcentral.com)
GTT treatment on HepG2 cells showed a total of five differentially expressed proteins when compared to their respective untreated cells where three proteins were down-regulated and two proteins were up-regulated. (biomedcentral.com)
Lower DRI values may protect normal cells while selectively destroying tumor cells (Chou 2010). (pi3k-inhibitors.com)
And d) Another very basic problem is that cancer cells tend to be remarkably clever and naturally seek to take advantage of numerous cellular survival mechanisms to stay alive under stress, for example by upregulating heat shock proteins or DNA repair mechanisms. (anti-agingfirewalls.com)
Results Senescent PA cells upregulate BCL-XL upon senescence induction and show dependency on BCL-XL for survival. (ibecbarcelona.eu)

(b) There are four main proteins of the ADAR enzyme family: two isoforms of ADAR1 (p110 and p150), ADAR2 and ADAR3. (biomedcentral.com)
Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. (medchemexpress.com)

Restoration of the calcium\binding site was confirmed by NMR spectroscopy, and structures of mutant human CD23 proteins were determined by X\ray crystallography, although no electron density for calcium was observed. (treatmentforprostatecancer.info)
Using the links, experts can explore the motifs, proteins, complex structures and associated literature to evaluate whether candidate motifs might be worth experimental investigation. (insulin-receptor.info)

Heat shock family of proteins (HSPs) is proposed to play pivotal role in breast tumor development owing to their intrinsic molecular chaperone properties [ 5 ]. (biomedcentral.com)

D) Cytoplasmic and nuclear ZKSCAN5 protein levels in two types of breast cancer cell lines, ZR75-1 and MDA-MB-231. (bms-911543.com)
Tubulin was used as the cytoplasmic control, and lamin A/C was used as the nuclear protein-loading control. (bms-911543.com)

90% and demonstrates an excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein. (bvsalud.org)

At that time, glycobiology, which is the study of carbohydrates and their recognition by motif-specific carbohydrate-binding proteins or lectins, lagged far behind the studies that defined the structural and cellular biology of cell death. (nature.com)
The SWI/SNF complex was originally described in yeast as the protein complex critical for cellular responses to mating-type switching (SWI) or sucrose fermentation (SNF). (justia.com)
The cellular FLICE inhibitory protein (cFLIP) regulates both recruitment and processing of pro-caspase-8 within the DISC [ 13 ]. (biomedcentral.com)

TSPO is a ubiquitous mitochondrial protein and is involved in numerous biological functions. (uni-regensburg.de)
Herein, we report the design, synthesis, and biological evaluation of selective SMARCA2 protein degraders developed using the proteolysis targeting chimera (PROTAC) technology. (bvsalud.org)
Compound 20 showed outstanding biological data, inhibiting tau protein and Aβ40 aggregation with IC50 = 1.8 and 1.3 μM, respectively. (ibecbarcelona.eu)

This complex is necessary for LC3-I (microtubule-associated proteins 1A/1B light chain 3B) conjugation to PE (phosphatidylethanolamine) to form LC3-II (LC3-phosphatidylethanolamine conjugate). (wikipedia.org)
It belongs to a multimeric complex and is associated with other proteins.The pleiotropic actions of TSPO render this protein an interesting target in the nervous system. (uni-regensburg.de)

It also directly links a parasite protein to cancer-causing cell processes, giving us a real insight into how infection with parasites and other organisms might lead to cancer in humans. (breastcancerstudyandsupport.org)

And, in addition, " 'We also found that an anti-parasite drug can target this protein and reverse the cancer-like state. (breastcancerstudyandsupport.org)

This protein is then able to 'mess around' with the cell and trigger mechanisms which control cell behaviour -so it starts acting like a cancer cell. (breastcancerstudyandsupport.org)

INTRODUCTION Linear motifs (LMs) are short elements embedded within larger protein Rabbit polyclonal to ZFP161 sequence segments that operate as sites of regulation (1C5). (insulin-receptor.info)
The bioinformatics problem is simple to state: LMs are too short (and the information content too poor) to be statistically significant in protein sequence searches. (insulin-receptor.info)

Herein, we review the role of glycans and glycan-binding proteins as essential components of the cell death machinery during physiologic and pathologic settings. (nature.com)

This is an exciting example of how parasites hijack the host cell and how these parasite proteins can be targeted by drugs. (breastcancerstudyandsupport.org)

To determine whether the absence of this calcium\binding site affects the structure and function of human CD23, CD23 mutant proteins with increasingly murine\like sequences were generated. (treatmentforprostatecancer.info)

Furthermore, several predictive tools for identifying natively disordered protein segmentsthe main harbour for LMs (28C30)have become available (31,32), complementing the more established globular domain resources Pfam, SMART, PROSITE and InterPro (33C36). (insulin-receptor.info)

Many protein kinases can regulate activity of the ATG5 protein. (wikipedia.org)

Anatomy32

Organisms8

Diseases14

Chemicals and Drugs120

Analytical, Diagnostic and Therapeutic Techniques and Equipment24

Phenomena and Processes54

Disciplines and Occupations1

Information Science3

Transcriptionally upregulated2

Inhibits4

Kinase7

Mutations5

Signalling pathway1

Pathways3

MAPK1

Regulatory proteins2

Receptors3

Mimetics1

Antiproliferative3

Apoptosis6

Receptor2

Gene6

Inhibit2

Apoptotic2

Extracellular3

Membrane-bound1

Constitutively expressed1

Expression6

MRNA1

Genes1

Bind1

Cells5

Enzyme2

Structures2

Family1

Nuclear2

Degradation1

Cellular3

Biological3

Complex2

Processes1

Target1

Control1

Short2

Role1

Drugs1

Human1

Domain1

Activity1