Recent submissions
Now showing items 221-240 of 658
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Salmonella-based platform for efficient delivery of functional binding proteins to the cytosol.
(NATURE PUBLISHING GROUP, 2020-07-03)Protein-based affinity reagents (like antibodies or alternative binding scaffolds) offer wide-ranging applications for basic research and therapeutic approaches. However, whereas small chemical molecules efficiently reach ... -
Fadraciclib (CYC065), a novel CDK inhibitor, targets key pro-survival and oncogenic pathways in cancer.
(PUBLIC LIBRARY SCIENCE, 2020-07-09)Cyclin-dependent kinases (CDKs) contribute to the cancer hallmarks of uncontrolled proliferation and increased survival. As a result, over the last two decades substantial efforts have been directed towards identification ... -
Optimising the value of immunomodulatory drugs during induction and maintenance in transplant ineligible patients with newly diagnosed multiple myeloma: results from Myeloma XI, a multicentre, open-label, randomised, Phase III trial.
(WILEY, 2021-03-01)Second-generation immunomodulatory agents, such as lenalidomide, have a more favourable side-effect profile than the first-generation thalidomide, but their optimum combination and duration for patients with newly diagnosed ... -
The landscape of RNA polymerase II-associated chromatin interactions in prostate cancer.
(AMER SOC CLINICAL INVESTIGATION INC, 2020-08-03)Transcriptional dysregulation is a hallmark of prostate cancer (PCa). We mapped the RNA polymerase II-associated (RNA Pol II-associated) chromatin interactions in normal prostate cells and PCa cells. We discovered thousands ... -
Intermittent schedules of the oral RAF-MEK inhibitor CH5126766/VS-6766 in patients with RAS/RAF-mutant solid tumours and multiple myeloma: a single-centre, open-label, phase 1 dose-escalation and basket dose-expansion study.
(ELSEVIER SCIENCE INC, 2020-11-01)BACKGROUND: CH5126766 (also known as VS-6766, and previously named RO5126766), a novel MEK-pan-RAF inhibitor, has shown antitumour activity across various solid tumours; however, its initial development was limited by ... -
ALDEHYDE COMPOUNDS AS INHIBITORS OF DUST MITE GROUP 1 PEPTIDASE ALLERGEN AND THEIR USE
(2012-01-12)The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aldehyde compounds of the following formula (A) (for convenience, collectively referred to herein as "ALD ... -
COMPOUNDS AND THEIR USES
(2013-02-21)The invention provides a compound that is an inhibitor of one or both of TBK1 and IKKe, or a down-regulator of the expression of one or both of TBK1 and IKKe, for use in a method of treating a cancer that is dependent on ... -
PYRIMIDINE COMPOUNDS AS INHIBITORS OF PROTEIN KINASES IKK EPSILON AND/OR TBK-1, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
(2012-01-26)Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKKe and/or TBK-1 : in which: R1 represents an aliphatic heterocyclyl ... -
(2-carboxamido)(3-amino)thiophene compounds
(2005-09-27)Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is R2 is and R3 is C 0-4 alkyl, are useful in the treatment of cancer. -
PYRUVAMIDE COMPOUNDS AS INHIBITORS OF DUST MITE GROUP 1 PEPTIDASE ALLERGEN AND THEIR USE
(2011-07-28)The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as "PVA compounds"), ... -
PYRIMIDINE COMPOUNDS USEFUL IN THE TREATMENT OF DISEASES MEDIATED BY IKKE AND/OR TBK1 MECHANISMS
(2014-08-28)Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases &Igr;&Kgr;&Kgr;&egr; and/or TBK-1 in which one of V and W is N, and ... -
5-(PYRIMIDIN-4-YL)-2-(PYRROLIDIN-1-YL)NICOTINONITRILE COMPOUNDS AS IKKE, TBK1 AND/OR SIK2 KINASES INHIBITORS
(2018-08-30)The invention provides compounds of formula (I) wherein R is −CH3 or −CH2CH3 and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of diseases or disorders mediated by IKKE, ... -
MAP4K4 Inhibitors
(2019-04-18)This invention relates to pyrrolopyrimidine comprising compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these ... -
MAP4K4 Inhibitors
(2020-06-11)This invention relates to compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these compounds, for example in a method ... -
Fragment growing to retain or alter the selectivity of anchored kinase hinge-binding fragments
(ROYAL SOC CHEMISTRY, 2014-01-01)<p>The selectivity patterns of kinase hinge-binding fragments can be retained during fragment growing, suggesting a new way to control poly-pharmacology.</p> -
MicroRNA-135b promotes cancer progression by acting as a downstream effector of oncogenic pathways in colon cancer.
(CELL PRESS, 2014-04-14)MicroRNA deregulation is frequent in human colorectal cancers (CRCs), but little is known as to whether it represents a bystander event or actually drives tumor progression in vivo. We show that miR-135b overexpression is ... -
Intrinsic susceptibility MRI identifies tumors with ALKF1174L mutation in genetically-engineered murine models of high-risk neuroblastoma.
(PUBLIC LIBRARY SCIENCE, 2014-03-25)The early identification of children presenting ALK(F1174L)-mutated neuroblastoma, which are associated with resistance to the promising ALK inhibitor crizotinib and a marked poorer prognosis, has become a clinical priority. ... -
Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A.
(AMER CHEMICAL SOC, 2014-03-27)Stapled helix peptides can serve as useful tools for inhibiting protein-protein interactions but can be difficult to optimize for affinity. Here we describe the discovery and optimization of a stapled helix peptide that ... -
Subclonal reconstruction of tumors by using machine learning and population genetics.
(NATURE PUBLISHING GROUP, 2020-09-01)Most cancer genomic data are generated from bulk samples composed of mixtures of cancer subpopulations, as well as normal cells. Subclonal reconstruction methods based on machine learning aim to separate those subpopulations ... -
Allergen Delivery Inhibitors: A Rationale for Targeting Sentinel Innate Immune Signaling of Group 1 House Dust Mite Allergens through Structure-Based Protease Inhibitor Design.
(AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS, 2018-09-01)Diverse evidence from epidemiologic surveys and investigations into the molecular basis of allergenicity have revealed that a small cadre of "initiator" allergens promote the development of allergic diseases, such as asthma, ...