Results 41 to 50 of about 580,692 (357)

Cytoplasmic p21 promotes stemness of colon cancer cells via activation of the NFκB pathway

open access: yesMolecular Oncology, EarlyView.
Cytoplasmic p21 promotes colorectal cancer stem cell (CSC) features by destabilizing the NFκB–IκB complex, activating NFκB signaling, and upregulating BCL‐xL and COX2. In contrast to nuclear p21, cytoplasmic p21 enhances spheroid formation and stemness transcription factor CD133.
Arnatchai Maiuthed   +10 more
wiley   +1 more source

Extending the in vivo Half-Life of Adalimumab Fab via Sortase A-Mediated Conjugation of Adalimumab Fab with Modified Fatty Acids

open access: yesPharmaceutical Fronts, 2020
Adalimumab, a full-length monoclonal antibody, is widely used as an anti-tumor necrosis factor-α (anti-TNF-α) agent. In this article, we aimed to prolong the in vivo half-life of adalimumab antigen-binding fragment (Fab) through Sortase A (SrtA)-mediated
Qing-Bin Zhang   +5 more
doaj   +1 more source

Dual targeting of RET and SRC synergizes in RET fusion‐positive cancer cells

open access: yesMolecular Oncology, EarlyView.
Despite the strong activity of selective RET tyrosine kinase inhibitors (TKIs), resistance of RET fusion‐positive (RET+) lung cancer and thyroid cancer frequently occurs and is mainly driven by RET‐independent bypass mechanisms. Son et al. show that SRC TKIs significantly inhibit PAK and AKT survival signaling and enhance the efficacy of RET TKIs in ...
Juhyeon Son   +13 more
wiley   +1 more source

Draft genome sequence and annotation of the enfumafungin producing fungus Hormonema carpetanum ATCC 74360

open access: yesBMC Genomic Data
Objectives Plant endophytic fungusHormonema carpetanum is the only organism known to produce enfumafungin to date. Enfumafungin is a fernane-type triterpenoid glycoside compound with broad-spectrum antifungal activity, and this leading compound has been ...
Haodong Chen   +5 more
doaj   +1 more source

Recent Advances in Novel Modulators for Cardiac Myosin Disorders

open access: yesPharmaceutical Fronts
In advanced stages of heart disease, most cases are characterized by heart failure, where the heart's systolic and diastolic functions are weakened, and then it cannot meet the body's normal oxygen demands.
Hancheng Wang   +4 more
doaj   +1 more source

Industrial-Scale Preparation of a Key Intermediate for the Manufacture of Therapeutic SGLT2 Inhibitors

open access: yesPharmaceutical Fronts, 2022
(3R,4S,5R,6R)-3,4,5-tris(benzyloxy)-6-methyltetrahydro-2H-pyran-2-one (1) is a key intermediate for the preparation of promising SGLT2 inhibitors currently undergoing clinical tests for diabetes therapy.
Lei Huang   +4 more
doaj   +1 more source

Effective therapeutic targeting of CTNNB1‐mutant hepatoblastoma with WNTinib

open access: yesMolecular Oncology, EarlyView.
WNTinib, a Wnt/CTNNB1 inhibitor, was tested in hepatoblastoma (HB) experimental models. It delayed tumor growth and improved survival in CTNNB1‐mutant in vivo models. In organoids, WNTinib outperformed cisplatin and showed enhanced efficacy in combination therapy, supporting its potential as a targeted treatment for CTNNB1‐mutated HB.
Ugne Balaseviciute   +17 more
wiley   +1 more source

Structural Characterization of Chemical Compounds Based on Their Fragmentation Rules in Sophorae Fructus by UPLC-QTOF-MS/MS

open access: yesPharmaceutical Fronts, 2022
This study aims to identify the chemical components in Sophorae Fructus, and explore the mass spectrometric cleavage rules using the UPLC-Q-TOF-MS/MS method. The main characteristic fragments of the compounds were analyzed by electrospray ionization (ESI)
Zi-Hui He   +3 more
doaj   +1 more source

Pathways Across the Valley of Death: Novel Intellectual Property Strategies for Accelerated Drug Discovery [PDF]

open access: yes, 2008
Drug discovery is stagnating. Government agencies, industry analysts, and industry scientists have all noted that, despite significant increases in pharmaceutical R&D funding, the production of fundamentally new drugs - particularly drugs that work on ...
Crossman, Colin   +3 more
core   +1 more source

Developing evidence‐based, cost‐effective P4 cancer medicine for driving innovation in prevention, therapeutics, patient care and reducing healthcare inequalities

open access: yesMolecular Oncology, EarlyView.
The cancer problem is increasing globally with projections up to the year 2050 showing unfavourable outcomes in terms of incidence and cancer‐related deaths. The main challenges are prevention, improved therapeutics resulting in increased cure rates and enhanced health‐related quality of life.
Ulrik Ringborg   +43 more
wiley   +1 more source

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