Results 161 to 170 of about 1,411,950 (341)

Improving PARP inhibitor efficacy in bladder cancer without genetic BRCAness by combination with PLX51107

Molecular Oncology, EarlyView.
Clinical trials on PARP inhibitors in urothelial carcinoma (UC) showed limited efficacy and a lack of predictive biomarkers. We propose SLFN5, SLFN11, and OAS1 as UC‐specific response predictors. We suggest Talazoparib as the better PARP inhibitor for UC than Olaparib.
Jutta Schmitz, Anna L. Bartkowiak, Michael Rose, Nora Kolks, Patrick Petzsch, Vandana Solanki, Anne Stoffel, Bianca Faßbender, Leandra Lepping, Julka Volkamer, Karl Köhrer, Marc Seifert, Tokameh Mahmoudi, Tahlita C. M. Zuiverloon, Günter Niegisch, Michèle J. Hoffmann   +15 more
wiley   +1 more source

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

Deep representation learning of chemical-induced transcriptional profile for phenotype-based drug discovery [PDF]

Xiaochu Tong, Ning Qu, Xiangtai Kong, Shengkun Ni, Jingyi Zhou, Kun Wang, Lehan Zhang, Yiming Wen, Jiangshan Shi, Sulin Zhang, Xutong Li, Mingyue Zheng   +11 more
openalex   +1 more source

Class IIa HDACs forced degradation allows resensitization of oxaliplatin‐resistant FBXW7‐mutated colorectal cancer

Molecular Oncology, EarlyView.
HDAC4 is degraded by the E3 ligase FBXW7. In colorectal cancer, FBXW7 mutations prevent HDAC4 degradation, leading to oxaliplatin resistance. Forced degradation of HDAC4 using a PROTAC compound restores drug sensitivity by resetting the super‐enhancer landscape, reprogramming the epigenetic state of FBXW7‐mutated cells to resemble oxaliplatin ...
Vanessa Tolotto, Nicolò Gualandi, Ylenia Cortolezzis, Raffaella Picco, Monica Colitti, Francesca D'Este, Mariachiara Gani, Wayne W. Hancock, Giovanni Terrosu, Cristina Degrassi, Francesca Agostini, Claudio Brancolini, Luigi E. Xodo, Eros Di Giorgio   +13 more
wiley   +1 more source

Open Innovation for Phenotypic Drug Discovery: The PD2 Assay Panel [PDF]

, 2011
Jonathan A. Lee, Shaoyou Chu, Francis S. Willard, Karen L. Cox, Rachelle J. Sells Galvin, Robert B. Peery, Sarah E. Oliver, Jennifer Oler, Tamika D. Meredith, Steven A. Heidler, Wendy H. Gough, Saba Husain, Alan D. Palkowitz, Christopher M. Moxham   +13 more
openalex   +1 more source

Determination of Ligand-Binding Affinity (K_d) Using Transverse Relaxation Rate (R₂) in the Ligand-Observed ¹H NMR Experiment and Applications to Fragment-Based Drug Discovery

, 2023
Manjuan Liu, Amin Mirza, Craig McAndrew, Arjun Thapaliya, Olivier A. Pierrat, Mark Stubbs, Tamas Hahner, N. Chessum, Paolo Innocenti, John Caldwell, Matthew D. Cheeseman, Benjamin R. Bellenie, Rob L. M. van Montfort, Gary Newton, Rosemary Burke, Ian Collins, Swen Hoelder   +16 more
openalex   +1 more source

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

Molecular 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, Lily L. Remsing Rix, Bin Fang, Eric A. Welsh, Nicole V. Bremer, Valentina Foglizzo, Paola Roa, Nickole Sigcha‐Coello, Yi Liao, Eric B. Haura, Alexander Drilon, John M. Koomen, Emiliano Cocco, Uwe Rix   +13 more
wiley   +1 more source

Editorial: Organoids for drug discovery. [PDF]

Front Pharmacol
Shen C, You M, Wang L.
europepmc   +1 more source

Big data analytics for drug discovery [PDF]

, 2013
Keith C. C. Chan
openalex   +1 more source

B2B Infrastructures in the Process of Drug Discovery and Healthcare

In this paper we describe a demonstration of an innovative B2B infrastructure which can be used to support collaborations in the pharmaceutical industry to achieve the drug discovery goal.
Boniface, M.J., Radetzki, U., Walland, Paul. W.   +2 more
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