Search Results - "Pors, Klaus"

Potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the benzoisoxazole moiety: application of a bioisosteric scaffold hopping approach to flufenamic acid by Pippione, Agnese Chiara, Carnovale, Irene Maria, Bonanni, Davide, Sini, Marcella, Goyal, Parveen, Marini, Elisabetta, Pors, Klaus, Adinolfi, Salvatore, Zonari, Daniele, Festuccia, Claudio, Wahlgren, Weixiao Yuan, Friemann, Rosmarie, Bagnati, Renzo, Boschi, Donatella, Oliaro-Bosso, Simonetta, Lolli, Marco Lucio

“…The aldo-keto reductase 1C3 (AKR1C3) isoform plays a vital role in the biosynthesis of androgens and is considered an attractive target in prostate cancer…”
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Dansyl linked solid phase resins as an educational tool to teach the concepts of high throughput screening and prodrugs by Morral, Jordi, Ibrahim, Ali, Traore, Fatima, Pors, Klaus

“…High throughput screening (HTS) and combinatorial chemistry have been part of the process of drug design for nearly two decades. However, methods to teach…”
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Polysialic acid sustains cancer cell survival and migratory capacity in a hypoxic environment by Elkashef, Sara M., Allison, Simon J., Sadiq, Maria, Basheer, Haneen A., Ribeiro Morais, Goreti, Loadman, Paul M., Pors, Klaus, Falconer, Robert A.

“…Polysialic acid (polySia) is a unique carbohydrate polymer expressed on the surface of NCAM (neuronal cell adhesion molecule) in a number of cancers where it…”
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Design, Synthesis, Biological Evaluation and In Silico Study of Benzyloxybenzaldehyde Derivatives as Selective ALDH1A3 Inhibitors by Ibrahim, Ali I. M., Ikhmais, Balqis, Batlle, Elisabet, AbuHarb, Waed K., Jha, Vibhu, Jaradat, Khaled T., Jiménez, Rafael, Pequerul, Raquel, Parés, Xavier, Farrés, Jaume, Pors, Klaus

“…Aldehyde dehydrogenase 1A3 (ALDH1A3) has recently gained attention from researchers in the cancer field. Several studies have reported ALDH1A3 overexpression…”
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The Chemerin-CMKLR1 Axis is Functionally important for Central Regulation of Energy Homeostasis by Yun, Haesung, Dumbell, Rebecca, Hanna, Katie, Bowen, Junior, McLean, Samantha L., Kantamneni, Sriharsha, Pors, Klaus, Wu, Qing-Feng, Helfer, Gisela

“…Chemerin is an adipokine involved in inflammation, adipogenesis, angiogenesis and energy metabolism, and has been hypothesized as a link between obesity and…”
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Cytochrome P450 isoforms 1A1, 1B1 AND 2W1 as targets for therapeutic intervention in head and neck cancer by Presa, Daniela, Khurram, Syed A., Zubir, Amir Z. A., Smarakan, Sneha, Cooper, Patricia A., Morais, Goreti R., Sadiq, Maria, Sutherland, Mark, Loadman, Paul M., McCaul, James, Shnyder, Steven D., Patterson, Laurence H., Pors, Klaus

“…Epidemiological studies have shown that head and neck cancer (HNC) is a complex multistage process that in part involves exposure to a combination of…”
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Editorial: Chemical Biology Tools for Peptide and Protein Research by Tsai, Yu-Hsuan, Iwaï, Hideo, Pors, Klaus

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Intratumoural Cytochrome P450 Expression in Breast Cancer: Impact on Standard of Care Treatment and New Efforts to Develop Tumour-Selective Therapies by Sneha, Smarakan, Baker, Simon C, Green, Andrew, Storr, Sarah, Aiyappa, Radhika, Martin, Stewart, Pors, Klaus

“…Despite significant advances in treatment strategies over the past decade, selective treatment of breast cancer with limited side-effects still remains a great…”
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Encapsulation and Delivery of Mitoxantrone Using Zirconium-Based Metal–Organic Frameworks (MOFs) and Their Cytotoxic Potential in Breast Cancer Cells by Singhal, Mitali, Riches-Suman, Kirsten, Pors, Klaus, Addicoat, Matthew A, Ruiz, Amalia, Nayak, Sanjit, Elies, Jacobo

“…Mitoxantrone (MTX) is a drug employed in breast cancer treatment, but its application is largely limited due to side effects. A controlled delivery approach…”
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Quantitative analysis of cytochrome P450 isoforms in human liver microsomes by the combination of proteomics and chemical probe-based assay by Liu, Xidong, Hu, Lianghai, Ge, Guangbo, Yang, Bo, Ning, Jing, Sun, Shixin, Yang, Ling, Pors, Klaus, Gu, Jingkai

“…Cytochrome P450 (CYP) is one of the most important drug‐metabolizing enzyme families, which participates in the biotransformation of many endogenous and…”
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Aldehyde Dehydrogenases and Prostate Cancer: Shedding Light on Isoform Distribution to Reveal Druggable Target by Quattrini, Luca, Sadiq, Maria, Petrarolo, Giovanni, Maitland, Norman J, Frame, Fiona M, Pors, Klaus, La Motta, Concettina

“…Prostate cancer represents the most common malignancy diagnosed in men, and is the second-leading cause of cancer death in this population. In spite of…”
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Chemical and biological explorations of the family of CC-1065 and the duocarmycin natural products by Ghosh, Nandita, Sheldrake, Helen M, Searcey, Mark, Pors, Klaus

“…CC-1065, the duocarmycins and yatakemycin are members of a family of ultrapotent antitumour antibiotics that have been the subject of extensive investigations…”
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DNA mismatch repair deficiency, resistance to cancer chemotherapy and the development of hypersensitive agents by Pors, Klaus, Patterson, Laurence H

“…DNA Mismatch Repair (MMR) deficiency results in resistance to platinating and alkylating agents, DNA minor groove binders, inhibitors of topoisomerases and…”
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Aldehyde dehydrogenases in cancer: an opportunity for biomarker and drug development? by Pors, Klaus, Moreb, Jan S.

“…•High ALDH expression in CSCs is associated with a worse prognosis.•ALDH isozyme expression can to some extent be cancer specific.•Rational approach to…”
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Alchemix: A Novel Alkylating Anthraquinone with Potent Activity against Anthracycline- and Cisplatin-resistant Ovarian Cancer by Pors, Klaus, Paniwnyk, Zennia, Teesdale-Spittle, Paul, Plumb, Jane A, Willmore, Elaine, Austin, Caroline A, Patterson, Laurence H

“…Chloroethylaminoanthraquinones are described with intercalating and alkylating capacity that potentially covalently cross-link topoisomerase II (topo II) to…”
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How can the potential of the duocarmycins be unlocked for cancer therapy? by Jukes, Zoë, Morais, Goreti Ribeiro, Loadman, Paul M., Pors, Klaus

“…•Duocarmycins are powerful cell-killing agents with potential to treat tumours.•The exceptional potency of the duocarmycins might also be their achilles’…”
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Abstract 2020: Investigation of CYP450 enzymes as therapeutic targets in rhabdomyosarcoma by Picher, Enric Arasanz, Pors, Klaus

“…Abstract Introduction: Rhabdomyosarcoma (RMS) is a rare soft tissue sarcoma (STS) that predominantly affects children and teenagers. It is the most frequent…”
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Structural Investigations of Prodrug Activation by Human Cytochrome P450 Enzymes by Bart, Aaron G., Pors, Klaus, Scott, Emily E.

“…Some human cytochrome P450 enzymes are selectively expressed in tumor tissues, providing an opportunity for targeted, P450‐mediated activation of cancer…”
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Cytochrome P450 Binding and Bioactivation of Tumor-Targeted Duocarmycin Agents by Bart, Aaron G., Morais, Goreti, Vangala, Venu R., Loadman, Paul M., Pors, Klaus, Scott, Emily E.

“…Not provided…”
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Deep Transfer Learning-Based Approach for Glucose Transporter-1 (GLUT1) Expression Assessment by Al Zorgani, Maisun Mohamed, Ugail, Hassan, Pors, Klaus, Dauda, Abdullahi Magaji

“…Glucose transporter-1 (GLUT-1) expression level is a biomarker of tumour hypoxia condition in immunohistochemistry (IHC)-stained images. Thus, the GLUT-1…”
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