Inhibitor adenosine triphosphate. Medical search. Frequent questions

19. Cytostatic activity of adenosine triphosphate-competitive kinase inhibitors in BRAF mutant thyroid carcinoma cells. (nih.gov)
Tyrosine kinase inhibitors have revolutionized the treatment of certain cancers. (nih.gov)
Currently, mechanisms of hepatotoxicity associated with tyrosine kinase inhibitors are only partially clarified. (nih.gov)
In view of the role that TKs seem to play in the regulation of cellular metabolism [ 8 , 9 , 10 , 11 ], it is crucial to determine whether the antitumor activity of particular tyrosine kinase inhibitors (TKIs) is related to their effect at a given metabolic level. (biomedcentral.com)
Protein kinases constitute an immense enzyme family that emerges as a strikingly valuable set of targets in therapy of various tumors considering their high sensitivity to specific kinase inhibitors, which are often relatively well tolerated by normal cells. (biomedcentral.com)
In this review, we summarize and discuss principal metabolic changes following administration of particular kinase inhibitors on different levels of cellular metabolism (key metabolites and molecules affected by TKIs in cancer are summarized in Table 1 ). (biomedcentral.com)
There are several different types of EGFRIs, including small molecule tyrosine kinase inhibitors, monoclonal antibodies, and multikinase inhibitors. (skintherapyletter.com)
Small molecule tyrosine kinase inhibitors, such as gefitinib and erlotinib, selectively bind the adenosine triphosphate (ATP)-binding site of the EGFR tyrosine kinase receptor, inhibiting the receptor's intracellular domain via preventing phosphorylation. (skintherapyletter.com)
Two classes: humanized monoclonal antibodies against the extra cellular, ligand-binding domain of the receptor, and small molecular tyrosine kinase inhibitors that complete with the intracellular adenosine triphosphate binding domain of the receptor. (standardofcare.com)
Include monoclonal antibodies cetuximab and panitumubab, and tyrosine kinase inhibitors erlotinib, geftinib and lapatinib. (standardofcare.com)
Mutations of the EGFR gene have been exclusively found in a subset of pulmonary adenocarcinomas highly sensitive to tyrosine kinase inhibitors for EGFR. (standardofcare.com)
The presence of EGFR mutations an indicator of clinical efficacy of tyrosine kinase inhibitors (TKI) in patients with metastatic or recurrent NSCLC. (standardofcare.com)
Several small molecule kinase inhibitors with activity against FLT3 have been evaluated in patients with AML as solitary agents and in combination with rigorous chemotherapy, e.g. restorative strategy for the treatment of mutated AML, including mechanisms of resistance to TKIs as well as possible novel strategies to improve FLT3 inhibitor therapy. (stemcellresearchformichigan.com)
In this article, we discuss the use and limitations of tyrosine kinase inhibitors (TKIs) like a therapeutic strategy for the treatment of mutated AML. (stemcellresearchformichigan.com)
Treatment with tyrosine kinase inhibitors Activation of signaling pathways via RTKs plays a central role in the pathogenesis of AML, and inhibition of these tyrosine kinases using small molecules represents an attractive therapeutic concept. (stemcellresearchformichigan.com)

It binds competitively to the adenosine triphosphate (ATP)-binding pocket of these receptors and blocks the intracellular signaling, which is crucial for the proliferation, migration, and transformation of fibroblasts, representing essential mechanisms of the idiopathic pulmonary fibrosis pathology. (medscape.com)
This kit measures the concentration of intracellular adenosine triphosphate (ATP) by the luciferase luminescence method and the amount of lactate released from cells by the absorbance method using water soluble tetrazolium (WST) formazan. (dojindo.com)
Using the inhibitors contained in this kit, it is possible to evaluate a shift in the intracellular metabolism between glycolysis and oxidative phosphorylation (OXPHOS). (dojindo.com)
Selective compounds have been developed that target either the extracellular ligand-binding region of the EGFR (including a number of monoclonal antibodies [MAbs], immunotoxins, and ligand-binding cytotoxic agents) or the intracellular tyrosine kinase region (including various small-molecule inhibitors). (medscape.com)
Elevated intracellular uptake of 2deoxyadenosine accompanied by phosphorylation by deoxycytidine kinase results in deposition of deoxyadenosine triphosphate (dATP) which inhibits ribonucleotide reductase, stopping regular DNA fix and synthesis [5]. (siamtech.net)

In HepaRG cells, pretreatment with rifampicin decreased membrane toxicity (measured as adenylate kinase release) and dissipation of adenosine triphosphate stores, indicating that toxicity was associated mainly with the parent drugs. (nih.gov)
Epithelial growth factor receptor inhibitor cutaneous toxicity may be positively correlated with clinical response to treatment. (standardofcare.com)
Metabolomic profiling of ENO1 -deleted glioma cells treated with the enolase inhibitor revealed a profound decrease in the TCA cycle metabolites with the toxicity reversible upon exogenous supplementation of supraphysiological levels of anaplerotic substrates, including pyruvate. (biomedcentral.com)

As we burn through ATP the, broken down and now isolated, adenosine builds up in the bloodstream and interacts with cell receptors to inhibit neural activity and cause fatigue and drowsiness. (dreamers.company)
Adenosine and caffeine have an almost identical chemical makeup, allowing the caffeine we ingest to connect to, and block, our adenosine cell receptors - stopping the slow inhibition of neural activity and stopping that drowsy feeling. (dreamers.company)
Adenosine receptors participate in the category of G protein-coupled receptors, which you can find four subtypes (A1, A2A, A2B and A3), which enjoy different jobs in regulating regular mobile physiology in a multitude of tissue including the human brain, heart and lungs [7]. (siamtech.net)
We have previously shown that endogenous adenosine 5'-triphosphate (ATP), via P2X3 and P2X2/3 receptors, plays an essential role in carrageenan-induced articular hyperalgesia model in rats' knee joint. (iasp-pain.org)
The non-selective P2X3 and P2X2/3 receptors agonist αβ-meATP induced a dose-dependent articular hyperalgesia, which was significantly reduced by the selective antagonists for P2X3 and P2X2/3 receptors (A-317491), bradykinin B- (DALBK) or B-receptors (bradyzide), β-(atenolol) or β-adrenoceptors (ICI-118,551), by the pre-treatment with cyclooxygenase inhibitor (indomethacin) or with the nonspecific selectin inhibitor (Fucoidan). (iasp-pain.org)

Despite favorable responses to TKI inhibitors EGFR mutant tumors sustain progression by 1 year, mostly due to the development of resistant mutations. (standardofcare.com)
This contrasts with the enolase inhibitor HEX, which, despite its negative charge, achieved antineoplastic effects in both intracranial and subcutaneous tumors. (biomedcentral.com)
Thus, to exploit this therapeutic opportunity in this subset of tumors, we developed a specific inhibitor of enolase, HEX and a pro-drug thereof, POMHEX. (biomedcentral.com)
RBS2418 (investigational product) is a specific immune modulator, working through ectonucleotide pyrophosphatase/phosphodiesterase I (ENPP1), designed to lead to anti-tumor immunity by increasing endogenous 2'-3'-cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) and adenosine triphosphate (ATP levels) and reducing adenosine production in the tumors. (uclahealth.org)
This study is an open-label, multi-site Phase 1a/1b study of RBS2418, a selective ENPP1 inhibitor, in combination with pembrolizumab or as a monotherapy in subjects with advanced unresectable, recurrent or metastatic tumors. (uclahealth.org)

AG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). (adooq.com)
PCM-075 is a highly-selective adenosine triphosphate (ATP) competitive inhibitor of the serine/threonine polo-like-kinase 1 (PLK 1) enzyme, which is over-expressed in multiple hematologic and solid solid tumor cancers. (salesandmarketingnetwork.com)
ENO1- deleted cells also exhibited selective sensitivity to the glutaminase inhibitor CB-839, in a manner rescuable by supplementation of anaplerotic substrates or plasma-like media Plasmax TM . (biomedcentral.com)
The selective FGFR2 inhibitor RLY-4008 has generated higher response rates compared with historical data for prior pan-FGFR inhibitors in patients with cholangiocarcinoma harboring FGFR2 fusions or alterations who have not been exposed to a prior FGFR inhibitor, according to R. Kate (Katie) Kelley, MD. (onclive.com)
Within the last few years, extra inhibitors have already been created, with acalabrutinib getting more selective, and demonstrating fewer clinical undesireable Lentinan effects recently. (chiflatironsofficial.com)
New york: Limiting, as plasma pde-8-selective inhibitors persists well beyond the great divide. (ardelyx.com)

Various techniques have been developed for targeting cancer cells: gene therapy, monoclonal antibodies (MAbs), antibody toxin conjugates, small-molecule inhibitors, antisense molecules, and tumor vaccines. (medscape.com)

Bempedoic acid is in a class of medications called adenosine triphosphate-citrate lyase (ACL) inhibitors. (medlineplus.gov)
Nexletol is a member of the adenosine triphosphate-citrate lyase (ACL) inhibitor class of drugs. (myheartdiseaseteam.com)

Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). (adooq.com)
Erlotinib and geftinib are highly specific for EGFR and/or reversible inhibitors, meeting they can be competed off the receptor by adenosine try phosphate. (standardofcare.com)

Purification and Characterization of Adenylate Kinase as an Apparent Adenosine Triphosphate-dependent Inhibitor of Ribonuclease II in Escherichia coli . (nih.gov)

In this respect, small molecule inhibitors are the most widely used clinically relevant means for targeted therapy, with a rising number of approvals for TKs inhibitors. (biomedcentral.com)

Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. (adooq.com)

Epidermal growth factor receptor inhibitor papulopustular eruption may be a surrogate marker for the drugs efficacy with a positive correlation between the rash and tumor response, survival or both. (standardofcare.com)
If a tumor acquires T790M mutation EGFR inhibitors are unable to be beneficial. (standardofcare.com)
In addition to targeting mutant EGFR in tumor cells these inhibitors inhibit wild type EGFR residing in normal, healthy tissues such as the skin and lining of the GI tract. (standardofcare.com)
PCM-075 has demonstrated synergy in preclinical studies with over 10 chemotherapeutic and target agents used in hematologic and solid tumor cancers, including FLT3 and HDAC inhibitors, taxanes, and cytotoxins. (salesandmarketingnetwork.com)
We also determined the synergy between enolase inhibitors and the glutaminase inhibitor CB-839 in glioma cells in vitro and in vivo in both intracranial and subcutaneous tumor models. (biomedcentral.com)
CD39, initially discovered as a checkpoint inhibitor by OREGA Biotech's cofounder Dr. Armand Bensussan in collaboration with INSERM, is expressed on both regulatory T cells and tumor cells. (worldpharmatoday.com)
In contrast, adenosine accumulation causes immune suppression and dysregulation of immune cell infiltrates resulting in tumor spreading. (worldpharmatoday.com)
The next areas shall explain the introduction of the brand new BTK inhibitors, and their function in the treatment centers, accompanied by a paragraph where in fact the multifaceted function of BTK for tumor advancement is certainly discussed. (chiflatironsofficial.com)

BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. (adooq.com)
Epidermal growth factor receptor (EGFR) inhibitors are part of an emerging class of anticancer medicines known as "targeted therapy," which target pathways more specific to neoplastic proliferation than traditional chemotherapeutic agents. (skintherapyletter.com)
Epidermal growth factor receptor inhibitor rash biopsies show lymphocytic perifolliculitis or supppurative superficial folliculitis without infection. (standardofcare.com)
Management of epidermal growth factor receptor inhibitor rash includes oral and topical antibiotics, systemic or topical corticosteroids, topical retinoids, and anti-histamines. (standardofcare.com)

Dr. Countouriotis was Chief Medical Officer at Ambit Biosciences through the initial development of quizartinib, a small molecule FLT3 inhibitor for the treatment of Acute Myeloid Leukemia, and ultimate acquisition of the company by Daiichi Sankyo. (salesandmarketingnetwork.com)
In particular, NSF can bind an energy source molecule, adenosine triphosphate (ATP), and the ATP-bound NSF develops internal tension via cleavage of ATP. (news-medical.net)

AEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2. (adooq.com)
Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). (adooq.com)
EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis. (adooq.com)
in contrast, EGFR inhibitors (EGFRIs) target pathways more specific to survival of neoplastic cells, thus belonging to a new class of chemotherapeutic agents - so-called "targeted therapy. (skintherapyletter.com)
Later degeneration EGFR inhibitors such as afatinib are irreversibly bound to the receptor forming a covalent bond inside the cell between the drug and the receptor. (standardofcare.com)
Patients with EGFR-mutant lung cancers should be treated up front with EGFR inhibitors rather than chemotherapy as randomized trials show this improves progression free survival and quality of life. (standardofcare.com)
Rash the cause of treatment cessation or dose modification in 8-17% of patients on EGFR inhibitors. (standardofcare.com)
Second-generation EGFR inhibitors have more rash and diarrhea due to the fact they are irreversible bound agents. (standardofcare.com)

As this enables for covalent, irreversible inhibitor binding, it offers these substances using a advantageous personality highly. (chiflatironsofficial.com)

Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. (adooq.com)
Pretomanid, the novel agent in the regimen, is a nitroimidazooxazine that blocks cell-wall production in actively replicating MTB organisms and acts as a respiratory poison and protein synthesis inhibitor to kill nonreplicating persister organisms ( 2 ). (cdc.gov)
Bedaquiline is a diarylquinoline that inhibits mycobacterial adenosine triphosphate synthase in replicating and persister organisms, and linezolid is an oxazolidinone that also inhibits protein synthesis ( 3 , 4 ). (cdc.gov)
The majority of these compounds share a common mechanism of action - they competitively inhibit adenosine triphosphate (ATP) at the catalytic binding site of the targeted protein [ 13 ]. (biomedcentral.com)
Naghdi N, Majlessi N, Bozorgmehr T (2003) The effects of Anisomycin (a protein synthesis inhibitor) on spatial learning and memory in CA1 region of rats hippocampus. (toku-e.com)
This metabolic switch depends on the phosphatidyl inositol 3′-kinase/Akt pathway, is antagonized by the adenosine monophosphate (AMP)-activated protein kinase (AMPK), and is required for DC maturation. (ashpublications.org)
Cytoplasmic proteins targeted for turnover are covalently linked to the small protein ubiquitin , which then interacts with a large protein complex, the proteasome , to degrade the protein in an adenosine triphosphate (ATP)-dependent process. (basicmedicalkey.com)

Soellner published on the interplay between allosteric and adenosine triphosphate (ATP)-competitive inhibitors of ABL kinase, showing that the latter preferably binds to different conformational states of ABL compared to allosteric agents that specifically target the ABL myristate pocket (STAMP) and deducing that asciminib cannot bind to ABL simultaneously with ATP-competitive drugs. (unibas.ch)

We analyzed polar metabolites in sensitive ( ENO1 -deleted) and resistant ( ENO1 -WT) glioma cells treated with enolase and glutaminase inhibitors. (biomedcentral.com)
We investigated whether sensitivity to enolase inhibitors could be attenuated by exogenous anaplerotic metabolites. (biomedcentral.com)
Impaired or Absent ADA function results in the deposition from the dangerous metabolites adenosine, 2deoxyadenosine and deoxyadenosine triphosphate (dATP). (siamtech.net)

3. mTOR inhibitors sensitize thyroid cancer cells to cytotoxic effect of vemurafenib. (nih.gov)

Cyclic adenosine monophosphate (cAMP) is the most important secondary messenger involved in endocrine system development and function. (spandidos-publications.com)

We evaluated the metabolic pathway dependence of HeLa cells treated with a glycolytic inhibitor (2-DG concentration: 2 mmol/l). (dojindo.com)
It plays a major role in promoting immunosuppression through the pathway degrading adenosine triphosphate (ATP) into adenosine. (worldpharmatoday.com)
With purine nucleoside phosphorylase, it forms an important element of the purine salvage pathway, in charge of the irreversible deamination of adenosine and 2deoxyadenosine into inosine and 2deoxyinosine respectively. (siamtech.net)

This indicates that metabolism in HeLa cells in the absence of glycolytic inhibitor treatment is highly dependent on the glycolytic system. (dojindo.com)

LAE001, Laekna's other Core Product, is an androgen synthesis inhibitor that inhibits both CYP17A1 and CYP11B2. (laekna.com)

Epithelial growth factor receptor inhibitor rash is dose dependent. (standardofcare.com)

Dr. Countouriotis has incredible expertise in the clinical development of oncology therapeutics, including multiple compounds in leukemia such as Sprycel, Mylotarg, Bosulif and Quizartinib, which is a FLT3 inhibitor in AML. (salesandmarketingnetwork.com)

13. Apoptotic cell death induction and angiogenesis inhibition in large established medullary thyroid carcinoma xenografts by Ret inhibitor RPI-1. (nih.gov)
Since glycolysis inhibition would deprive the cell of a key source of pyruvate, we hypothesized that enolase inhibitors might inhibit anaplerosis and synergize with other inhibitors of anaplerosis, such as the glutaminase inhibitor, CB-839. (biomedcentral.com)
Metabolomic and biochemical data strongly indicated both specific and dose-dependent inhibition of glycolysis by these enolase inhibitors [ 9 ]. (biomedcentral.com)

Higher rate of lymphomas and lung cancers with another JAK inhibitor vs. TNF blockers in RA patients. (nih.gov)
AKT inhibitors have demonstrated their ability to reverse drug resistance in numerous clinical studies and showed their potential to address the urgent unmet medical needs in those selected cancers. (laekna.com)

CIBINQO is a Janus kinase (JAK) inhibitor indicated for the treatment of adults with refractory, moderate-to-severe atopic dermatitis whose disease is not adequately controlled with other systemic drug products, including biologics, or when use of those therapies is inadvisable. (nih.gov)

The inhibitor can bind to a site remote from the enzyme active site. (iwp-2inhibitor.com)
Furthermore, our X-ray crystallographic, solution nuclear magnetic resonance (NMR), and isothermal titration calorimetry studies show that asciminib can bind ABL concomitantly with type-1 or -2 ATP-competitive inhibitors to form ternary complexes. (unibas.ch)

It blocks purine synthesis and 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), thus increasing anti-inflammatory adenosine concentration at sites of inflammation. (medscape.com)

Nateglinide interacts with the adenosine triphosphate (ATP) ̶ sensitive potassium channel on pancreatic beta cells. (medscape.com)

Moderate to strong inhibitors of both CYP2C19 and CYP2C9, or strong CYP2C19 or CYP2C9 inducers: Avoid concomitant use. (nih.gov)

We have [seen] improvements in first-line therapy with the addition of immune checkpoint inhibitors to standard chemotherapy with gemcitabine and cisplatin. (onclive.com)

11 PDE gene families have been identified based on amino acid sequences, biochemical properties, and inhibitor profiles ( 6 , 7 ). (spandidos-publications.com)

Since RLY-4008 has a different mechanism of action compared with prior pan-FGFR inhibitors, Kelley noted that it could have a different mechanism of resistance, which could delay resistance in this patient population. (onclive.com)

Increased incidence of pulmonary embolism, venous and arterial thrombosis with another JAK inhibitor vs. TNF blockers. (nih.gov)
For example, inhibitors of PDE5 serve as therapeutic agents for male erectile dysfunction and pulmonary hypertension ( 11 , 12 ). (spandidos-publications.com)

CIBINQO is not recommended for use in combination with other JAK inhibitors, biologic immunomodulators, or with other immunosuppressants. (nih.gov)

5. Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer. (nih.gov)

2. The MEK1/2 Inhibitor AZD6244 Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib. (nih.gov)
9. Tyrosine kinase inhibitor therapy and metabolic remodelling in papillary thyroid cancer. (nih.gov)
Trovagene believes the combination of its targeted PLK-1 inhibitor, PCM-075, with other compounds has the potential for improved clinical efficacy in Acute Myeloid Leukemia (AML), Castration-Resistant Prostate Cancer (CRPC), Non-Hodgkin Lymphoma (NHL), Triple Negative Breast Cancer (TNBC) and Adrenocortical Carcinoma (ACC). (salesandmarketingnetwork.com)
According to Frost & Sullivan, LAE001 is the only dual CYP17A1/CYP11B2 inhibitor in clinical trials for the treatment of prostate cancer globally. (laekna.com)

Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA. (adooq.com)
The addition of valsartan to an ACE inhibitor improves cardiac sympathetic nerve activity, left ventricular function, and symptoms in patients with CHF. (snmjournals.org)

Trovagene plans to initiate a Phase 1b/2 clinical trial with PCM-075 in AML, since it has shown significant advantages over prior PLK1 inhibitors evaluated in this indication, including a higher selectivity, greater potency, oral bioavailability and shorter half-life. (salesandmarketingnetwork.com)
According to Frost & Sullivan, LAE002 is one of the only two AKT inhibitors that have currently ongoing registrational clinical trials globally. (laekna.com)

Angiotensin-converting enzyme (ACE) inhibitors increase survival when introduced at any stage of CHF ( 2 - 7 ). (snmjournals.org)

Introduction The introduction of the BTK inhibitors implemented seminal research that initially had been made currently in the 1930s. (chiflatironsofficial.com)

In contrast, oligomycin treatment did not increase lactate production in the glycolytic inhibitor-treated cells, and ATP levels were markedly reduced by oligomycin treatment. (dojindo.com)

The glycolytic capacity of HeLa cells treated with a glycolytic inhibitor (2-DG concentration: 2 mmol/l) was compared with that of untreated HeLa cells (control). (dojindo.com)
We evaluated whether treatment with a glycolytic inhibitor (2-DG concentration: 2 mmol/l) would cause a metabolic shift in HeLa cells. (dojindo.com)
After incubation of RBCs with either inhibitor, the dielectric response of water in the cytoplasm, and specifically its relaxation time, demonstrated minimal sensitivity to the change of D-glucose concentration in the medium. (huji.ac.il)

AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling. (adooq.com)
Angiotensin-receptor blockers (ARBs) inhibit the angiotensin type 1 receptor and exert hemodynamic effects similar to those of ACE inhibitors in the setting of CHF ( 13 , 14 ). (snmjournals.org)

Anatomy16

Organisms12

Diseases6

Chemicals and Drugs172

Analytical, Diagnostic and Therapeutic Techniques and Equipment10

Phenomena and Processes35

Disciplines and Occupations1

Information Science3

Health Care1

Kinase inhibitors15

Intracellular5

Toxicity3

Receptors5

Tumors5

Selective6

Monoclonal antibodies1

Lyase2

Erlotinib2

Adenylate kinase1

Small molecule inhibitors1

Gefitinib1

Tumor8

Epidermal4

Molecule2

EGFR8

Irreversible inhibitor1

Protein7

Allosteric1

Metabolites3

MTOR1

Monophosphate1

Pathway3

Metabolism1

Inhibits1

Growth factor r1

FLT31

Inhibition3

Cancers2

Janus1

Bind2

Anti-inflammatory1

Interacts1

CYP2C191

Chemotherapy1

Acid1

Mechanism of act1

Pulmonary2

CIBINQO1

Antitumor1

Cancer4

Activity2

Clinical2

Survival1

Initially1

Contrast1

Concentration3

Receptor2