Results 71 to 80 of about 27,094 (219)

A 5-Br-1-Propylisatin Derivative as a Promising BRD9 Ligand: Insights from Computational and STD NMR Investigation

Molecules
Bromodomain-containing protein 9 (BRD9) belongs to the non-canonical BAF chromatin remodeling complex and represents a relevant therapeutic target in pathologies featuring dysregulated epigenetic control.
Erica Gazzillo, Gabriel Rocha, Maria Giovanna Chini, Gianluigi Lauro, Jesús Angulo, Giuseppe Bifulco   +5 more
doaj   +1 more source

Discovery of a PCAF bromodomain chemical probe [PDF]

, 2016
The p300/CBP-associated factor (PCAF) and related GCN5 bromodomain-containing lysine acetyl transferases are members of subfamily I of the bromodomain phylogenetic tree.
Apirat Chaikuad, Mendez Johnson, Jacqui, Brennan, Paul E., Peter G. K. Clark, Yang, Hongbing, Catherine M. Rogers, TRULLI, LAURA, Mendez-Johnson, Jacqui, Dorrell, Lucy, Murphy, Emma J., Matthias T. Ehebauer, Ehebauer, Matthias T., John R. Walker, Dixon, Darren J, Daniels, Danette, Lin, Yu Hui, Dixon, Darren J., Huber, Kilian V.M., Chun‐Feng D. Hou, Dixon, Darren, Moses Moustakim, Clark, Peter G.K., Clark, Peter G. K., Hou, Chun-Feng D., Jacqui Mendez‐Johnson, Octovia P. Monteiro, Hui, Raymond, Kilian V. M. Huber, Jag Heer, Stefan Knapp, Hou, Chun Feng D., Fedorov, Oleg, Emma J. Murphy, Fuentes de Arriba, Angel L., Monteiro, Octovia, Oleg Fedorov, Heer, Jag, Laura Trulli, Knapp, Stefan, Rogers, Catherine M., Huber, Kilian, Yu‐Hui Lin, Danette Daniels, Paul E. Brennan, Lucy Dorrell, Moustakim, Moses, Darren J. Dixon, Brennan, Paul, Huber, Kilian V. M., Chaikuad, Apirat, Raymond Hui, Walker, John R., Angel L. Fuentes de Arriba, Monteiro, Octovia P., Lin, Yu-Hui, Hongbing Yang   +55 more
core   +1 more source

Structural Activity Relationship Analysis of New Diphenyl PFI-3 Analogues Targeting for the Treatment of Glioblastoma

Pharmaceuticals
Background/Objectives: Human glioblastoma (GBM) is the most aggressive brain cancer in adults and a highly treatment-refractory malignancy. The overall prognosis for the GBM is extremely poor, with a median survival of 12–14 months after initial ...
Dong-Jin Hwang, Chuanhe Yang, Yinan Wang, Hannah Kelso, Satyanarayana Pochampally, Lawrence M. Pfeffer, Duane D. Miller   +6 more
doaj   +1 more source

Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability. [PDF]

PLoS ONE, 2016
Lysine acetylation is an important epigenetic mark regulating gene transcription and chromatin structure. Acetylated lysine residues are specifically recognized by bromodomains, small protein interaction modules that read these modification in a sequence
Laura Lori, Alessandra Pasquo, Clorinda Lori, Maria Petrosino, Roberta Chiaraluce, Cynthia Tallant, Stefan Knapp, Valerio Consalvi   +7 more
doaj   +1 more source

Efficacy, safety and cost‐effectiveness of CAR‐T therapy

British Journal of Clinical Pharmacology, EarlyView.
CAR T‐cells demonstrate high efficacy in blood cancers, including ALL, MM and DLBCL. Innovations target solid tumours despite challenges such as antigen escape. Combination therapies enhance the delivery and infiltration of CAR T cells. Toxicity, cost and resistance remain major barriers to clinical use.
Emina Karahmet Sher, Amina Džidić‐Krivić, Emma Pinjic, Nejra Selak, Kanita Omerbasic, Alexandar Chupin, Andrej Belancic, Almir Fajkic   +7 more
wiley   +1 more source

Harnessing ferroptosis from multilayer defense networks to nanoplatforms for specific cancer therapy

BMEMat, EarlyView.
Nanomaterials target metabolically‐regulated ferroptosis for cancer therapy. Iron‐based or alternative nanoplatforms integrate ferroptosis with chemotherapy, immunotherapy, or radiotherapy. They enable stimulus‐responsive therapies (photothermal, photodynamic, sonodynamic) activated by near‐infrared, light, or ultrasound, achieving potent synergistic ...
Xinyue Xu, Xuejian Wang, Wenyan Jiang, Wan Hairul Anuar Kamaruddin, Chunyan Fang, Pengfei Zhang   +5 more
wiley   +1 more source

Unveiling the folding mechanism of the Bromodomains

Biochemistry and Biophysics Reports, 2017
Bromodomains (BRDs) are small protein domains often present in large multidomain proteins involved in transcriptional regulation in eukaryotic cells. They currently represent valuable targets for the development of inhibitors of aberrant transcriptional processes in a variety of human diseases.
Petrosino, Maria, Bonetti, Daniela, Pasquo, Alessandra, Lori, Laura, Chiaraluce, Roberta, Consalvi, Valerio, Travaglini-allocatelli, Carlo   +6 more
openaire   +4 more sources

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain

, 2018
The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine residues on histone proteins. The four BET bromodomainsBRD2, BRD3, BRD4, and BRDTeach contain two bromodomain modules.
Chun-wa Chung (1343454), David J. Hirst (1399282), Paul Bamborough (1343466), Emmanuel H. Demont (1399288), Matthew Lindon (1355946), Robert P. Law (2613493), Rab K. Prinjha (449759), Allan J. B. Watson (1369614), Stephen J. Atkinson (1297362), Laurie J. Gordon (1343442)   +9 more
core   +2 more sources

Humanized Candida and NanoBiT Assays Expedite Discovery of Bdf1 Bromodomain Inhibitors With Antifungal Potential

Advanced Science
The fungal Bromodomain and Extra‐Terminal (BET) protein Bdf1 is a potential antifungal target against invasive fungal infections. However, the need to selectively inhibit both Bdf1 bromodomains (BDs) over human orthologs and the lack of molecular tools ...
Kaiyao Wei, Marie Arlotto, Justin M. Overhulse, Tuan‐Anh Dinh, Yingsheng Zhou, Nathan J. Dupper, Jiayi Yang, Boris A. Kashemirov, Hasan Dawi, Cécile Garnaud, Gaëlle Bourgine, Flore Mietton, Morgane Champleboux, Amédé Larabi, Yordan Hayat, Rose‐Laure Indorato, Marjolaine Noirclerc‐Savoye, Dimitrios Skoufias, Muriel Cornet, Gwenaël Rabut, Charles E. McKenna, Carlo Petosa, Jérôme Govin   +22 more
doaj   +1 more source

Intravenous Lipopolysaccharide Challenge in Healthy Participants Reveals Pharmacodynamic Markers in Blood and Bone Marrow for Early‐Phase Oncology Drug Development

Clinical Pharmacology &Therapeutics, EarlyView.
Demonstrating pharmacological effects in early‐phase oncology clinical trials remains challenging, largely due to the lack of robust pharmacodynamic markers. Lipopolysaccharide (LPS) is used as an immune challenge agent in healthy participants to study drugs for autoimmune conditions.
Igor Radanović, Ingrid Tomljanović, Wieke H. Grievink, Diana R. Pereira, Michelle Osse, Peter van Balen, Maria J. Juachon, Marieke L. de Kam, Lisa Pagan, Manon A.A. Jansen, Matthijs Moerland, Jacobus J. Bosch   +11 more
wiley   +1 more source