Search Results - "Bingham, Matilda"

Accelerating BRPF1b hit identification with BioPhysical and Active Learning Screening (BioPALS) by Pal, Sandeep, Nare, Zandile, Rao, Vincenzo A., Smith, Brian O., Morrison, Ian, Fitzgerald, Edward A., Scott, Andrew, Bingham, Matilda J., Pesnot, Thomas

“…We report the development of BioPhysical and Active Learning Screening (BioPALS); a rapid and versatile hit identification protocol combining AI‐powered…”
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1504 Epithelial to mesenchymal transition (EMT) can be driven by macrophages through multiple signalling pathways by Turner, Darryl, Dobie, Ross, Rzepecka, Justyna, Gooding, Hayley, Bingham, Matilda

“…BackgroundEMT is the process whereby epithelial cells acquire mesenchymal characteristics. This process is highly regulated and required in development and…”
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Ring-Closing Metathesis as a Basis for the Construction of Aromatic Compounds by Donohoe, Timothy J., Orr, Allan J., Bingham, Matilda

“…The use of metathesis, especially in the context of ring‐closing metathesis (RCM) to form five‐ and six‐membered rings, is widespread in organic chemistry…”
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Flexible metathesis-based approaches to highly functionalised furans and pyrroles by Donohoe, Timothy J., Kershaw, Neil M., Orr, Allan J., Wheelhouse, Katherine M.P., Fishlock, Lisa P., Lacy, Adam R., Bingham, Matilda, Procopiou, Panayiotis A.

“…A range of differentially functionalised furans and pyrroles have been synthesised in short order by the judicious use of a ring-closing…”
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A Simple Route to Functionalized Δ1-Pyrrolenines by Z. Zard, Samir, Bingham, Matilda, Moutrille, Cécile

“…Treatment of γ-unsaturated oxime esters with cupric acetate or ferric chloride in acetic acid / t-butanol or in t-butanol alone leads to the formation of…”
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Abstract 3764: Porcupine inhibitor RXC004 enhances immune response in pre-clinical models of cancer by Bhamra, Inder, Armer, Richard, Bingham, Matilda, Eagle, Catherine, Cook, Alicia Edmenson, Phillips, Caroline, Woodcock, Simon

“…Abstract Background: RXC004, a potent and selective porcupine (PORCN) inhibitor, is being investigated in a safety and tolerability study in cancer patients…”
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Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections by Kirk, Ralph, Betson, Mark, Bingham, Matilda, Doyle, Paul, Harvey, Rebecca, Huxley, Anthony, Moat, John, Pesnot, Thomas, Tait, Michael, Hallworth, Sebastian, Nelson, Gary

“…[Display omitted] Delafloxacin, a fourth-generation anionic fluoroquinolone (FQ) was approved in 2019 for community acquired bacterial pneumonia (CARP). It has…”
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Novel porcupine (PORCN) inhibitor RXC004: Evaluation in models of RNF43 loss of function cancers by Bhamra, Inder, Adams, Nick, Armer, Richard, Bingham, Matilda, McKeever, Helen, Phillips, Caroline, Thompson, Ben, Woodcock, Simon

“…Abstract only e14094 Background: Wnt signalling initiates oncogenic pathways involved in tumour initiation, growth, differentiation and metastasis. 1 Targeting…”
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Development of an organo- and enzyme-catalysed one-pot, sequential three-component reaction by Kinnell, Angela, Harman, Thomas, Bingham, Matilda, Berry, Alan, Nelson, Adam

“…A one-pot, three-component process is described which involves both organo- and enzyme-catalysed carbon–carbon bond-forming steps. In the first step, an…”
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Abstract A199: Development of a series of novel, potent and selective inhibitors of cFMS as a potential treatment for CSF1 expressing cancers via the modulation of the tumor microenvironment and the repolarization of macrophages by Mahale, Sachin G., Belfield, Andrew, Wright, Jamie, Campbell, Mary-Ann, Bingham, Matilda, Armer, Richard

“…Abstract Redx Oncology has developed novel small molecule inhibitors of Colony Stimulating Factor 1 Receptor (CSF1R or cFMS) which have proven to be…”
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Abstract 5581: Development of 2nd generation indoleamine 2,3-dioxygenase 1 (IDO1) selective inhibitors by Pesnot, Thomas, Mahale, Sachin, MacFaul, Philip, Maclean, John, Phillips, Caroline, Bingham, Matilda, Eagle, Catherine, Kelly, James, Thippeswamy, Abhijith, Armitage, Simon, Grisin, Aleksandr, Aiken, Sheenagh, Cartwright, Lucy, Armer, Richard

“…Abstract Harnessing the immune system via immune checkpoint blockade (e.g. anti PD-1, anti PD-L1, anti CTLA4) has led to fast and long lived responses in…”
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The Wnt Pathway Inhibitor RXC004 Blocks Tumor Growth and Reverses Immune Evasion in Wnt Ligand-dependent Cancer Models by Phillips, Caroline, Bhamra, Inder, Eagle, Catherine, Flanagan, Eimear, Armer, Richard, Jones, Clifford D, Bingham, Matilda, Calcraft, Peter, Edmenson Cook, Alicia, Thompson, Ben, Woodcock, Simon A

“…Wnt signaling is implicated in the etiology of gastrointestinal tract cancers. Targeting Wnt signaling is challenging due to on-target toxicity concerns and…”
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Abstract 5160: Development of REDX05358, a novel highly selective and potent pan RAF inhibitor and a potential therapeutic for BRAF and RAS mutant tumors by Mason, Helen, Scrace, Simon, Testar, Richard, Rainard, Julie, Talab, Fatima, Poonawala, Ryaka, Smith, Philippa, Brooke, Harriet, Frith, Sarah, Ahmet, Jonathan, Hall, Jonathan, Sorrell, David, Moore, Jon, Phillips, Caroline, France, Dennis, Bingham, Matilda, Armer, Richard

“…Abstract REDX05358 has been identified as a novel, highly selective and potent next generation pan RAF inhibitor with improved therapeutic potential and…”
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Abstract 4795: Development of novel, selective, reversible inhibitors equipotent against wild-type and C481S Bruton's tyrosine kinase (BTK) by Guisot, Nicolas E S, Walker, Victoria, Best, Stuart A., Abet, Valentina, Chappell, Rose, Emmerich, Juliette, Ho, Kelvin, Kelly, James R., Lyons, Kristina, Müller, Melanie, Refuerzo, Julienne, Sargent, Louise, Talab, Fatima, Waldron, Madelene, Bingham, Matilda, Campbell, Mary-Ann, Phillips, Caroline, Armer, Richard

“…Abstract Redx Oncology has developed novel, differentiated, reversible small molecule inhibitors of BTK, combining current best-in-class potency with improved…”
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Eating, sleeping and rewarding: orexin receptors and their antagonists by Bingham, Matilda J, Cai, Jiaqiang, Deehan, Maureen R

“…The orexin system plays a key role in the control of eating, sleeping and rewarding. This review summarizes the latest developments in the identification of…”
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Abstract 419: The development of BRPF1 degraders as a potential treatment for acute myeloid leukemia by Glynn, Daniel Joseph, Crampton, Rosie, Pesnot, Thomas, Scott, Andrew, Nassoy, Anne-Chloe, Kirk, Ralph, Narducci, Daniele, Nelson, Gary, Ongiri, Lynette, Begum, Habiba, Rao, Vincent, Bingham, Matilda, McPherson, Rhoanne, Turner, Darryl

“…Abstract Acetylation of histones and additional nuclear proteins is a key mechanism in the regulation of gene expression. Aberrant acetylation has been linked…”
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Development of REDX05194, a Novel, Potent and Selective Inhibitor of Bruton's Tyrosine Kinase (BTK) As a Potential Treatment for B-Cell Malignancies by Walker, Victoria, Guisot, Nicolas E S, Best, Stuart, Talab, Fatima, Lucas, Catherine L, Refuerzo, Julienne, Calder, Mathew, Proctor, Lauren, Muller, Melanie, Ho, Kelvin, Chappell, Rose, Emmerich, Juliette, Harmon, Shona, Bingham, Matilda, Campbell, Mary-Ann, Armer, Richard

“…The B-cell receptor (BCR) signaling pathway is required for the survival, activation, proliferation and differentiation of B-cells. Bruton's Tyrosine Kinase…”
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REDX08608, a Novel, Potent and Selective, Reversible BTK Inhibitor with Efficacy and Equivalent Potency Against Wild-Type and Mutant C481S BTK by Guisot, Nicolas E.S., Best, Stuart A., Wright, Victoria, Thomason, Andrew, Woyach, Jennifer A., Mantel, Rose, McClanahan, Fabienne, Abet, Valentina, Castagna, Diana, Cousin, Peggy, Emmerich, Juliette, Ho, Kelvin, Kelly, James Russell, King-Tours, James, Lyons, Kristina, Muller, Melanie, Refuerzo, Julienne, Sargent, Louise, Talab, Fatima, Bingham, Matilda, Phillips, Caroline, Armer, Richard

“…Here we report the preclinical profile of REDX08608 our novel, potent and selective, reversible BTK inhibitor that is equipotent against wild-type and mutant…”
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A Metathesis Approach to Aromatic Heterocycles by Donohoe, Timothy J., Orr, Allan J., Gosby, Katherine, Bingham, Matilda

“…The ring closing metathesis (RCM) reaction can be used to prepare substituted furans and pyrroles. By utilising a Pd‐catalysed coupling reaction with…”
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The identification, and optimisation of hERG selectivity, of a mixed NET/SERT re-uptake inhibitor for the treatment of pain by Angus, Derek, Bingham, Matilda, Buchanan, Dawn, Dunbar, Neil, Gibson, Linsday, Goodwin, Richard, Haunsø, Anders, Houghton, Andrea, Huggett, Margaret, Morphy, Richard, Napier, Susan, Nimz, Olaf, Passmore, Joanna, Walker, Glenn

“…Hit compound 1, a selective noradrenaline re-uptake transporter (NET) inhibitor was optimised to build in potency at the serotonin re-uptake transporter (SERT)…”
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