Results 71 to 80 of about 16,709 (213)

Molecular Dynamic Simulations of Bromodomain and Extra-Terminal Protein 4 Bonded to Potent Inhibitors

Molecules, 2021
Bromodomain and extra-terminal domain (BET) subfamily is the most studied subfamily of bromodomain-containing proteins (BCPs) family which can modulate acetylation signal transduction and produce diverse physiological functions.
Siao Chen, Yi He, Yajiao Geng, Zhi Wang, Lu Han, Weiwei Han   +5 more
doaj   +1 more source

The discovery of I-BRD9, a selective cell active chemical probe for bromodomain containing protein 9 inhibition

, 2015
Acetylation of histone lysine residues is one of the most well-studied post-translational modifications of chromatin, selectively recognized by bromodomain “reader” modules.
Ka Hing Che (1357551), Andrew J. Bannister (231506), Gerard Drewes (1290381), Drewy, David H., Prinjha, Rab K., Matthew Lindon (1355946), Laurie Gordon (1357524), Tony Kouzarides, Kouzarides, Tony, Drewry, David H., Paola Grandi (1343472), Rino A. Bit, Dittmann, Antje, Molnar, Judit, Humphreys, Philip G., Nicholas C. O. Tomkinson (1357533), Rab K. Prinjha, Leveridge, Melanie, Samuel C. Robson (1357527), Melanie Leveridge (1357542), Gordon, Laurie, Philip G. Humphreys (1357530), Becher, Isabelle, Che, Ka Hing, Anne-Marie Michon (1343457), Chun-wa Chung (1343454), Judit Molnar (1357521), Isabelle Becher, Samuel C. Robson, Matthew Lindon, David H. Drewry, Bamborough, Paul, Lindon, Matthew, Antje Dittmann, Michon, Anne-Marie, Nicholas C. O. Tomkinson, Rino A. Bit (1357536), Tomkinson, Nicholas C. O., Paul Bamborough (1343466), Anne-Marie Michon, Paola Grandi, David H. Drewry (386307), Paul Bamborough, Gerard Drewes, Bit, Rino A., Philip G. Humphreys, Grandi, Paola, Theodoulou, Natalie H., Isabelle Becher (1357539), Drewes, Gerard, Melanie Leveridge, Bannister, Andrew J., Tony Kouzarides (17431), Andrew J. Bannister, Chung, Chun-wa, Natalie H. Theodoulou (1357545), Ka Hing Che, Laurie Gordon, Chun-wa Chung, Judit Molnar, Robson, Samuel C., Rab K. Prinjha (449759), Natalie H. Theodoulou, Antje Dittmann (1357548)   +63 more
core   +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

Small molecule ligands of the BET-like bromodomain, SmBRD3, affect Schistosoma mansoni survival, oviposition, and development

, 2023
Schistosomiasis is a disease affecting over 200 million people worldwide, but its treatment relies on a single agent, praziquantel. To investigate new avenues for schistosomiasis control, we have conducted the first systematic analysis of bromodomain ...
Helen, Whiteland, Karl, Hoffmann, Josephine, Forde-Thomas, Manfred, Beckmann, Stuart, Conway, Anthony, Chan, Michael, McDonough, Rosa, Cookson, Darius, McArdle, Gilda, Padalino, Matthias, Schiedel   +10 more
core   +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

Proteasomal Degradation of the Papillomavirus E2 Protein Is Inhibited by Overexpression of Bromodomain-Containing Protein 4 [PDF]

Journal of Virology, 2009
ABSTRACTThe E2 protein of human papillomavirus (HPV) binds to specific sites in the viral genome to regulate its transcription, replication, and maintenance in infected cells. Like most regulatory proteins, E2 is rapidly turned over. A high-throughput assay was developed to quantify the expression and stability of E2 in vivo, based on its fusion ...
David, Gagnon, Simon, Joubert, Hélène, Sénéchal, Amélie, Fradet-Turcotte, Sabrina, Torre, Jacques, Archambault   +5 more
openaire   +2 more sources

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

Challenges and Pitfalls to Diagnosing NUTM1‐Rearranged Neoplasia of the Pancreas by Cytology and Ancillary Studies

Diagnostic Cytopathology, EarlyView.
ABSTRACT Fine‐needle aspiration cytology specimens are frequently utilized for ancillary studies to identify diagnostic and prognostic information. This case highlights diagnostic pitfalls and challenges in diagnosing NUTM1‐rearranged neoplasia on pancreatic cytology.
Terrance J. Lynn
wiley   +1 more source

The Generation of a Library of ­Bromodomain‐Containing Protein Modulators Expedited by Continuous Flow Synthesis [PDF]

European Journal of Organic Chemistry, 2016
AbstractA continuous flow process delivering key building blocks for a series of BCP modulator libraries is reported. A dynamically mixed flow reactor emerged as a pivotal technology in both synthesis and isolation phases enabling the processing of slurries and suspensions while maintaining high productivity and reliability.
Filipponi, P., Baxendale, I. R.
openaire   +2 more sources

Systemic aging fuels heart failure: Molecular mechanisms and therapeutic avenues

ESC Heart Failure, Volume 12, Issue 2, Page 1059-1080, April 2025.
Abstract Systemic aging influences various physiological processes and contributes to structural and functional decline in cardiac tissue. These alterations include an increased incidence of left ventricular hypertrophy, a decline in left ventricular diastolic function, left atrial dilation, atrial fibrillation, myocardial fibrosis and cardiac ...
Zhuyubing Fang, Umar Raza, Jia Song, Junyan Lu, Shun Yao, Xiaohong Liu, Wei Zhang, Shujuan Li   +7 more
wiley   +1 more source