Results 71 to 80 of about 112,243 (300)

Phosphatidylinositol 4‐kinase as a target of pathogens—friend or foe?

FEBS Letters, EarlyView.
This graphical summary illustrates the roles of phosphatidylinositol 4‐kinases (PI4Ks). PI4Ks regulate key cellular processes and can be hijacked by pathogens, such as viruses, bacteria and parasites, to support their intracellular replication. Their dual role as essential host enzymes and pathogen cofactors makes them promising drug targets.
Ana C. Mendes, Guilherme M. Azevedo, Amanda P. Barcellos, Diana Bahia   +3 more
wiley   +1 more source

Thalidomide decreases gelatinase production by malignant B lymphoid cell lines through disruption of multiple integrin-mediated signaling pathways

Haematologica, 2010
Background Thalidomide and its analogs are effective agents in the treatment of multiple myeloma. Since gelatinases (matrix metalloproteinases-2 and -9) play a crucial role in tumor progression, we explored the effect of thalidomide on gelatinase ...
Marta Segarra, Ester Lozano, Marc Corbera-Bellalta, Carme Vilardell, Maria-Teresa Cibeira, Jordi Esparza, Nora Izco, Joan Bladé, Maria C. Cid   +8 more
doaj   +1 more source

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. [PDF]

, 2008
The clinical success of multitargeted kinase inhibitors has stimulated efforts to identify promiscuous drugs with optimal selectivity profiles. It remains unclear to what extent such drugs can be rationally designed, particularly for combinations of ...
Aizenstein, Brian, Apsel, Beth, Blair, Jimmy A, Feldman, Morri E, Gonzalez, Beatriz, Hoffman, Randy, Knight, Zachary A, Nazif, Tamim M, Shokat, Kevan M, Williams, Roger L   +9 more
core  

Biology of advanced uveal melanoma and next steps for clinical therapeutics [PDF]

, 2014
Uveal melanoma is the most common intraocular malignancy although it is a rare subset of all melanomas. Uveal melanoma has distinct biology relative to cutaneous melanoma, with widely divergent patient outcomes.
Bastian, BC, Bowcock, AM, Carvajal, RD, Flaherty, KT, Gershenwald, JE, Gutkind, JS, Luke, JJ, McKenna, KC, Patel, PM, Sato, T, Selig, S, Sossman, JA, Streicher, HZ, Sznol, M, Thurin, M, Triozzi, PL, Van Meir, EG, Welch, J   +17 more
core   +1 more source

Repurposing inhibitors of phosphoinositide 3-kinase as adjuvant therapeutics for bacterial infections

Frontiers in Antibiotics, 2023
The rise in antimicrobial resistance and the decline in new antibiotics has created a great need for novel approaches to treat drug resistant bacterial infections. Increasing the burden of antimicrobial resistance, bacterial virulence factors allow for survival within the host, where they can evade host killing and antimicrobial therapy within their ...
openaire   +2 more sources

Inhibiting stearoyl‐CoA desaturase suppresses bone metastatic prostate cancer by modulating cellular stress, mTOR signaling, and DNA damage response

FEBS Letters, EarlyView.
Bone metastasis in prostate cancer (PCa) patients is a clinical hurdle due to the poor understanding of the supportive bone microenvironment. Here, we identify stearoyl‐CoA desaturase (SCD) as a tumor‐promoting enzyme and potential therapeutic target in bone metastatic PCa.
Alexis Wilson, Mackenzie K Herroon, Shane Mecca, Laimar C Garmo, Jacob Lindquist, Shrila Rajendran, Steve M. Patrick, Izabela Podgorski   +7 more
wiley   +1 more source

First-in-Human Phase I Study to Evaluate the Brain-Penetrant PI3K/mTOR Inhibitor GDC-0084 in Patients with Progressive or Recurrent High-Grade Glioma. [PDF]

, 2020
PurposeGDC-0084 is an oral, brain-penetrant small-molecule inhibitor of PI3K and mTOR. A first-in-human, phase I study was conducted in patients with recurrent high-grade glioma.Patients and methodsGDC-0084 was administered orally, once daily, to ...
Cloughesy, Timothy F, Coimbra, Alexandre F, Ellingson, Benjamin M, Gerstner, Elizabeth, Lee, Eudocia Q, Lu, Xuyang, Morrissey, Kari M, Mueller, Lars U, Olivero, Alan G, Rodon, Jordi, Wen, Patrick Y, Wilson, Timothy R   +11 more
core  

Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase [PDF]

, 2014
The Vps34 (vacuolar protein sorting 34) class III PI3K (phosphoinositide 3-kinase) phosphorylates PtdIns (phosphatidylinositol) at endosomal membranes to generate PtdIns(3)P that regulates membrane trafficking processes via its ability to recruit a ...
Alessi, Dario R., Bago, Ruzica, Cross, Darren, Davies, Paul, Ganley, Ian G., Malik, Nazma, Munson, Michael J., Prescott, Alan R., Shpiro, Natalia, Sommer, Eeva, Ward, Richard   +10 more
core   +3 more sources

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

Molecular 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, Kerstin Huebner, Katharina Erlenbach‐Wuensch, Chuanpit Hampel, Daniela Thalheim, Adriana Vial‐Roehe, Bodee Nutho, Susanne Merkel, Arndt Hartmann, Pithi Chanvorachote, Regine Schneider‐Stock   +10 more
wiley   +1 more source

Novel agents in the treatment of multiple myeloma: a review about the future

Journal of Hematology & Oncology, 2016
Multiple myeloma (MM) is a disease that affects plasma cells and can lead to devastating clinical features such as anemia, lytic bone lesions, hypercalcemia, and renal disease.
Leonard Naymagon, Maher Abdul-Hay
doaj   +1 more source