Dr. Kilian V. M. Huber received his doctorate in Medicinal and Pharmaceutical Chemistry from the Ludwig - Maximilians - Universität (LMU) in Munich working on the design and synthesis of natural product - inspired
kinase inhibitors in the group Prof. Franz Bracher.
Novel drug therapies and novel indications of drug therapy, e.g. tyrosine
kinase inhibitors in lung disease other than lung cancer, biological treatments for asthma, COPD, cystic fibrosis and interstitial lung disease.
Vorinostat interferes with the signaling transduction pathway of T - cell receptor and synergizes with phosphoinositide - 3
kinase inhibitors in cutaneous T - cell lymphoma
This finding is the latest from Georgetown University Medical Center's Translational Neurotherapeutics Program (TNP) examining tyrosine
kinase inhibitors in the treatment of neurodegenerative diseases.
Not exact matches
Pfizer (pfe) breast cancer treatment Ibrance burst onto the scene
in early 2015 and proceeded to dominate
in a new therapeutic arena called cyclin - dependent
kinase (CDK) 4 and 6
inhibitors.
In contrast, HPV - inactive tumors often have mutations in the PIK3CA / PTEN / AKT pathway, indicating that AKT kinase inhibitors may be effective treatment options for these patients.&raqu
In contrast, HPV - inactive tumors often have mutations
in the PIK3CA / PTEN / AKT pathway, indicating that AKT kinase inhibitors may be effective treatment options for these patients.&raqu
in the PIK3CA / PTEN / AKT pathway, indicating that AKT
kinase inhibitors may be effective treatment options for these patients.»
The authors also found that a novel small molecule
inhibitor of the salvage pathway enzyme deoxycytidine
kinase blocked leukemia growth
in mice
in combination with thymidine (to inhibit the de novo pathway).
Therefore, a novel therapeutic approach
in inflammatory breast cancer could involve a combination of conventional chemotherapy with small - molecule
inhibitors of the Cdk2 cell cycle
kinase.
An approach often used
in treating CML is to block the Bcr - Abl activity using tyrosine
kinase inhibitors (TKIs).
And none of these
kinase inhibitors have yet been rigorously tested
in a head - to - head comparison with the protein therapies already on the market.
These results not only show promise on a new targeted therapy to treat this malignancy, as PI3K
inhibitors are already used
in the clinical practice, but also unravel a new function of the PI3K
kinase in cancer biology through its role
in promoting metastasis.
Imatinib is an
inhibitor that blocks the ATP - binding site of the tyrosine
kinase Abl
in affected blood cells, thereby suppressing their overactivity.
These studies will investigate whether Src
kinase inhibitors are best used
in the adjuvant setting post-surgery or after chemotherapy to prevent the formation of local and distant disease recurrence.
One of the more intriguing findings
in the study was that increasing histone crotonylation works synergistically with other known anti-HIV latency molecules, such as the protein
kinase C agonist PEP005 and the HDAC
inhibitor vorinostat.
However, advances
in therapy have been made, notably the emergence of
kinase inhibitors for patients whose disease relapsed, according to the study background.
Researchers found that genetically disrupting this pathway, or using the FDA - approved Src
kinase inhibitor dasatinib, increases PUMA levels and decreases tumor progression and metastasis
in mice by up to fivefold.
In the study, the authors suggest that using Src
kinase inhibitors may be more effectively used as adjuvant therapies to block αvβ3 signaling and prevent disease spread.
For example, epidermal growth factor (EGFR) mutations may result
in sensitivity to drugs that are EGFR tyrosine
kinase inhibitors (TKIs), such as erlotinib or gefitinib, whereas individuals with the EGFR T790M mutation are more resistant to these drugs.
Among patients with advanced non-small cell lung cancer without a mutation of a certain gene (EGFR), conventional chemotherapy, compared with treatment using epidermal growth factor receptor tyrosine
kinase inhibitors, was associated with improvement
in survival without progression of the cancer, but not with overall survival, according to a study
in the April 9 issue of JAMA.
Epidermal growth factor receptor (EGFR) tyrosine
kinase inhibitors (TKIs) are the preferred treatment option for patients with advanced non-small cell lung cancer (NSCLC) who have mutations
in the EGFR gene.
Vemurafenib joins other multi-targeted
kinase inhibitors (MKIs)(sorafenib, lenvatinib) shown to be effective
in this patient population;
in spite of responses to these drugs, the responses are temporary and additional treatment options are needed.
DDRs inhibition with a tyrosine
kinase inhibitor appears to insulate the brain via blood - brain barrier repair, which prevents harmful immune cells that circulate
in the body from getting into the brain where they can indiscriminately attack and kill healthy and sick neurons, like those that have been unable to perform autophagy to «take out their trash,» says Moussa.
One option is an MEK
inhibitor, which inhibits the mitogen - activated protein
kinase enzymes used to therapeutically affect the MAPK pathway that is often overactive
in cancers.
In experiments using enzyme
inhibitors, the possibility that cinnamtannin B - 1 enhanced mobilization through the use of activation of enzymes such as PI3
kinase near the cell membrane was shown.
Pao was involved
in studies of EGFR tyrosine -
kinase inhibitors while at MSKCC, where he trained
in medical oncology.
The Structural Genomics Consortium at the University of North Carolina at Chapel Hill (SGC - UNC),
in partnership with the DiscoverX Corporation, has reached the milestone halfway point
in its development of the
Kinase Chemogenomic Set, a potent group of
inhibitors which allow deeper exploration of the human kinome, a family of enzymes critical to understanding human disease and developing new therapies.
Approximately 10 - 15 % of Caucasian and 30 - 35 % of Asian patients with NSCLC have a mutation
in the epidermal growth factor receptor (EGFR), which can be successfully targeted with EGFR
inhibitors called tyrosine
kinase inhibitors (TKI), such as erlotinib, gefitinib and afatinib.
THE STUDIES A trilogy of papers published
in the September 28 issue of Nature examine the role of a protein — cyclin - dependent
kinase inhibitor p16INK4a —
in aging, healing, and cancer.
«Through our collaboration with DiscoverX, we screened a large set of compounds that we call Published
Kinase Inhibitor Set 2, and these results allowed us to reach the halfway point
in constructing the KCGS» said David Drewry, a research associate professor at the UNC Eshelman School of Pharmacy and SGC - UNC principal investigator who is leading the project to develop the
Kinase Chemogenomic Set.
The drug is a multi -
kinase inhibitor (MKI)-- meaning it targets the specific enzymes that are required for growth
in DTC.
In a proof - of - concept study, Fourches and Ash looked at the ERK2
kinase — an enzyme associated with several types of cancer — and a group of 87 known ERK2
inhibitors, ranging from very active to inactive.
This visual abstract depicts how Wei et al. utilize single - cell phosphoproteomic analysis of patient derived glioblastoma models to identify shifts
in signaling coordination following short - term treatment with
kinase inhibitors, which facilitates the design of combination therapy approaches with reduced resistance and improved efficacy.
The researchers, including scientists from pharmaceutical company AstraZeneca, report
in an advanced online publication
in Nature Medicine on May 4, that their findings indicate «an underappreciated genomic heterogeneity»
in mechanisms of resistance to tyrosine
kinase inhibitor (TKI) drugs that target the Epidermal Growth Factor Receptor (EGFR) mutation that drive some cases of non-small cell lung cancer (NSCLC).
In practice, this means that when medicinal chemists discover a promising
kinase inhibitor that exists as two interchanging arrangements, they actually have two different
inhibitors.
This review focuses on
kinase inhibitors that are
in the clinic or
in clinical trials and for which structural information is available.
But whether p38 MAP
kinase inhibitors could be used to treat arthritis
in humans is unclear, she says.
A class of therapeutic drugs known as protein
kinase inhibitors has
in the past decade become a powerful weapon
in the fight against various life - threatening diseases, including certain types of leukemia, lung cancer, kidney cancer and squamous cell cancer of the head and neck.
Rho -
kinase inhibitor Y - 27632 and hypoxia synergistically enhance chondrocytic phenotype and change the S100 protein profile
in human chondrosarcoma cells
We used the janus
kinase (JAK)
inhibitor baricitinib with IFN - blocking activity
in vitro, to ameliorate disease.
Kinases are also druggable targets, as seen by the success of
kinase -
inhibitors in earning FDA approval (including, for example, crizotinib against ALK - fusion and erlotinib against EGFR).
Rho -
kinase inhibitor Y - 27632 increases cellular proliferation and migration
in human foreskin fibroblast cells
These data reveal that the tissue damage present
in this SIRS model is reflected,
in part, by breaks
in the vasculature due to endothelial cell necroptosis and thereby predict that RIPK1
kinase inhibitors may provide clinical benefit to shock and / or sepsis patients.
This thesis primarily investigates the effects of mechanical cyclic stretching, a 5 % low oxygen atmosphere and the Rho -
kinase inhibitor, Y - 27632, on protein responses
in chondrocytic human chondrosarcoma (HCS - 2 / 8) cells.
In 2005, Cagan's team created a general fly model of a human thyroid tumor caused by mutations in the Ret receptor tyrosine kinase gene, then screened a panel of drugs including a kinase inhibitor called vandetanib that suppressed the tumor (Cancer Res, 65:3538 - 41, 2005
In 2005, Cagan's team created a general fly model of a human thyroid tumor caused by mutations
in the Ret receptor tyrosine kinase gene, then screened a panel of drugs including a kinase inhibitor called vandetanib that suppressed the tumor (Cancer Res, 65:3538 - 41, 2005
in the Ret receptor tyrosine
kinase gene, then screened a panel of drugs including a
kinase inhibitor called vandetanib that suppressed the tumor (Cancer Res, 65:3538 - 41, 2005).
PHIb Trial of Fulvestrant, Palbociclib (CDK4 / 6
inhibitor) and Erdafitinib (JNJ - 42756493, pan-FGFR Tyrosine Kinase Inhibitor) in ER + / HER2 - / FGFR - amplified Metastatic Breast Can
inhibitor) and Erdafitinib (JNJ - 42756493, pan-FGFR Tyrosine
Kinase Inhibitor) in ER + / HER2 - / FGFR - amplified Metastatic Breast Can
Inhibitor)
in ER + / HER2 - / FGFR - amplified Metastatic Breast Cancer (MBC)
Clough BH, Zeitouni S, Krause U, et al., Rapid Osteogenic Enhancement of Stem Cells
in Human Bone Marrow Using a Glycogen ‐ Synthease ‐ Kinase ‐ 3 ‐ Beta Inhibitor Improves Osteogenic Efficacy In Vitro and In Viv
in Human Bone Marrow Using a Glycogen ‐ Synthease ‐
Kinase ‐ 3 ‐ Beta
Inhibitor Improves Osteogenic Efficacy
In Vitro and In Viv
In Vitro and
In Viv
In Vivo.
In the late 1990s, STI - 571 (imatinib, Gleevec / Glivec) was identified by the pharmaceutical company Novartis (then known as Ciba Geigy) in high - throughput screens for tyrosine kinase inhibitor
In the late 1990s, STI - 571 (imatinib, Gleevec / Glivec) was identified by the pharmaceutical company Novartis (then known as Ciba Geigy)
in high - throughput screens for tyrosine kinase inhibitor
in high - throughput screens for tyrosine
kinase inhibitors.
This lab,
in collaboration with the lab of Ruben Shaw at the Salk Institute, recently identified SBI - 0206965, the first potent and selective small molecule
inhibitor of ULK1, a serine / threonine
kinase that is a critical regulator of autophagy.
A combination of the FLT3
kinase inhibitor quizartinib with 5 - azacitidine or low - dose cytarabine is active
in patients with FLT3 - ITD mutated myeloid leukemias, according to a new study.
Glennie et al 134 have shown that T cells stimulated
in co-cultures with MSC exhibit an extensive inhibition of cyclin D2 and upregulation of the cyclin dependent
kinase inhibitor p27kip1.