Výsledky vyhledávání - "Benjamin Noll"

Anti-Leukaemic activity of Rilpivirine Is mediated by Aurora A Kinase Inhibition

Autor: Saiful Islam, Muhammed H. Rahaman, Mingfeng Yu, Benjamin Noll, Jennifer H. Martin, Shudong Wang, Richard Head

Publikováno v: Cancers
Volume 15
Issue 4
Pages: 1044

Simple Summary Rilpivirine is an anti-viral drug used for treating human immunodeficiency virus (HIV) patients. In a recent study, we demonstrated that rilpivirine inhibited Aurora A, a protein kinase that mainly regulates the mitotic events of the c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::311410a16842321989575f0e519a7ae0
https://hdl.handle.net/11541.2/33139

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An orally bioavailable and highly efficacious inhibitor of CDK9/FLT3 for the treatment of acute myeloid leukemia

Autor: Abel Tesfaye Anshabo, Laychiluh Bantie, Sarah Diab, Jimma Lenjisa, Alemwork Kebede, Yi Long, Gary Heinemann, Jasmine Karanjia, Benjamin Noll, Sunita K. C. Basnet, Manjun Li, Robert Milne, Hugo Albrecht, Shudong Wang

Publikováno v: Cancers; Volume 14; Issue 5; Pages: 1113

Mutations in FMS-like tyrosine kinase 3 (FLT3) occur in approximately one-third of AML patients and are associated with a particularly poor prognosis. The most common mutation, FLT3-ITD, is a self-activating internal tandem duplication (ITD) in the F

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb76e0b4e5a2ac45bd74644f460d73c1
https://hdl.handle.net/11541.2/31432

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Discovery of N-Phenyl-4-(1H-pyrrol-3-yl)pyrimidin-2-amine Derivatives as Potent Mnk2 Inhibitors: Design, Synthesis, SAR Analysis, and Evaluation of in vitro Anti-leukaemic Activity

Autor: Shudong Wang, Mingfeng Yu, Robert W. Milne, Cobus Gerber, Benjamin Noll, Saiful Islam, Sunita K.C. Basnet, Hugo Albrecht, Jingfeng Lu, Sarah Diab, Peng Li, Ahmed Abdelaziz, Laychiluh B. Mekonnen

Publikováno v: Medicinal Chemistry. 15:602-623

Background:Aberrant expression of eukaryotic translation initiation factor 4E (eIF4E) is common in many types of cancer including acute myeloid leukaemia (AML). Phosphorylation of eIF4E by MAPK-interacting kinases (Mnks) is essential for the eIF4E-me

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78300ef209a34b429c837abbbb93df57
https://doi.org/10.2174/1573406415666181219111511

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Sulfonamide-Based Inhibitors of Biotin Protein Ligase as New Antibiotic Leads

Autor: Kwangjun Lee, Andrew D. Abell, Steven W. Polyak, Beatriz Blanco-Rodriguez, John B. Bruning, Danielle Cini, Grant W. Booker, Robert W. Milne, Benjamin Noll, Andrew J. Hayes, Andrew C Marshall, Ashleigh S. Paparella, Jiage Feng, Matthew C.J. Wilce, Jingxian Yu, William Tieu

Publikováno v: ACS Chemical Biology. 14:1990-1997

Here, we report the design, synthesis, and evaluation of a series of inhibitors of Staphylococcus aureus BPL (SaBPL), where the central acyl phosphate of the natural intermediate biotinyl-5′-AMP (1) is replaced by a sulfonamide isostere. Acylsulfam

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17972eb42541dd574d7fb900e1b5a4a3
https://doi.org/10.1021/acschembio.9b00463

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Tacrolimus dose, blood concentrations and acute nephrotoxicity, but not CYP3A5/ABCB1 genetics, are associated with allograft tacrolimus concentrations in renal transplant recipients

Autor: Rong Hu, Graeme R. Russ, Andrew A. Somogyi, Jonathan Tuke, Daniel T. Barratt, Benedetta C. Sallustio, Janet K. Coller, Benjamin Noll

Aims: Long-term use of the immunosuppressant tacrolimus is limited by nephrotoxicity. Following renal transplantation, the risk of nephrotoxicity may be determined more by allograft than by blood tacrolimus concentrations, and thus may be affected by

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f92d23f667a0cef3776f89a32945254f
https://hdl.handle.net/11541.2/147207

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Discovery and pharmacological characterization of a novel series of highly selective inhibitors of cyclin-dependent kinases 4 and 6 as anticancer agents

Autor: Laychiluh Bantie, Saiful Islam, Malika Kumarasiri, Solomon Tadesse, Benjamin Noll, Robert W. Milne, Khamis Tomusange, Ge Zhu, Nataliya Bykovska, Mingfeng Yu, Shudong Wang, Frankie Lam, Peng Li

Publikováno v: British Journal of Pharmacology. 175:2399-2413

Background and purpose Cyclin D-dependent kinases 4 and 6 (CDK4/6) are crucial regulators of the G1 to S phase transition of the cell cycle and are actively pursued as therapeutic targets in cancer. We sought to discover a novel series of orally bioa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::245a3a7d6d4fa68a532dfb0d542e63b4
https://doi.org/10.1111/bph.13974

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Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation

Autor: Muhammed H. Rahaman, Shudong Wang, Solomon Tadesse, Khamis Tomusange, Robert W. Milne, Laychiluh B. Mekonnen, Saiful Islam, Frankie Lam, Benjamin Noll, Hugo Albrecht, Sunita K.C. Basnet, Mingfeng Yu, Theodosia Teo

Publikováno v: Journal of Medicinal Chemistry. 60:1892-1915

Cyclin D dependent kinases (CDK4 and CDK6) regulate entry into S phase of the cell cycle and are validated targets for anticancer drug discovery. Herein we detail the discovery of a novel series of 4-thiazol-N-(pyridin-2-yl)pyrimidin-2-amine derivati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1648237e2f97eba5963718c7cb65e8c3
https://doi.org/10.1021/acs.jmedchem.6b01670

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Relationship between allograft cyclosporin concentrations and P‐glycoprotein expression in the 1st month following renal transplantation

Autor: Andrew A. Somogyi, Jonathan Tuke, Graeme R. Russ, Benedetta C. Sallustio, Janet K. Coller, Benjamin Noll

Publikováno v: Br J Clin Pharmacol

The immunosuppressant cyclosporin is a P‐glycoprotein (P‐gp) substrate whose impaired function has been associated with an increased risk of cyclosporin‐induced nephrotoxicity following renal transplantation. This study investigated the relatio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fe2569a21f656cb08152649f4083da0
https://europepmc.org/articles/PMC6475688/

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