W. H. H. W. van den Berg, W. G. van Kitel,
... for more papers by this authorW. G. van Kitel, W. G. van Kitel Department of Dermatology, Free University Hospital, de Boelelaan ... for more papers by this authorW. G. van Kitel, W. G. van Kitel Department of Dermatology, Free University Hospital, de Boelelaan ...
Tópico(s): Eicosanoids and Hypertension Pharmacology
1983 - Wiley | Contact Dermatitis
Tara Kang-Pettinger, Kayleigh Walker, R. H. Brown, Richard Cowan, Helena Wright, Roberta Baravalle, Lorna C. Waters, Frederick W. Muskett, Matthew W. Bowler, Kovilen Sawmynaden, P.J. Coombs, Mark D. Carr, Gareth Hall,
... like domain (PD-L1 D2) (6Zak K.M. Kitel R. Przetocka S. Golik P. Guzik K. Musielak ... Protein Data Bank [PDB]:5C3T (6Zak K.M. Kitel R. Przetocka S. Golik P. Guzik K. Musielak ... shown in pink (PDB: 4ZQK (6Zak K.M. Kitel R. Przetocka S. Golik P. Guzik K. Musielak ...
Tópico(s): Immune Cell Function and Interaction
2022 - Elsevier BV | Journal of Biological Chemistry
Krzysztof M. Zak, Radosław Kitel, Sara Przetocka, Przemysław Golik, Katarzyna Guzik, Bogdan Musielak, Alexander Dömlingꝉ, Grzegorz Dubin, Tad A. Holak,
Summary Targeting the PD-1/PD-L1 immunologic checkpoint with monoclonal antibodies has recently provided breakthrough progress in the treatment of melanoma, non-small cell lung cancer, and other types of cancer. Small-molecule drugs interfering with this pathway are highly awaited, but their development is hindered by insufficient structural information. This study reveals the molecular details of the human PD-1/PD-L1 interaction based on an X-ray structure of the complex. First, it is shown that the ligand ...
Tópico(s): Immune Cell Function and Interaction
2015 - Elsevier BV | Structure
Pottayil G. Sasikumar, Murali Ramachandra,
... 2008).Crossref, Medline, CAS, Google Scholar16 Zak KM, Kitel R, Przetocka S et al. Structure of the ...
Tópico(s): CAR-T cell therapy research
2017 - Future Science Ltd | Future Medicinal Chemistry
Anna Byczek-Wyrostek, Radosław Kitel, Klaudia Rumak, Magdalena Skonieczna, Anna Kasprzycka, Krzysztof Walczak,
A series of 5-alkoxy derivatives of 3,4-dichloro-5-hydroxyfuran-2-(5H)-one (mucochloric acid, MCA) were obtained and subsequently subjected to modification in the C-4 position of 2(5H)-furanone ring. The cytotoxicity of newly synthesized compounds was evaluated in MTT assay against non-small cell lung cancer (A549) and healthy lung epithelial cell line (BEAS-2B). The derivatives containing a branched alkoxy substituent in the C-5 position demonstrated the highest anticancer properties, whereas modification ...
Tópico(s): Carbohydrate Chemistry and Synthesis
2018 - Elsevier BV | European Journal of Medicinal Chemistry
Tamim Alsuliman, Caroline Kitel, Rémy Duléry, Thierry Guillaume, Fabrice Larosa, Jérôme Cornillon, Hélène Labussière‐Wallet, Clémence Médiavilla, Stéphanie Belaiche, Jérémy Delage, Sophie Alain, Ibrahim Yakoub‐Agha,
Cytomegalovirus is one of the main contributing factors to high mortality rates in patients undergoing allogeneic hematopoietic cell transplantation (allo-HCT). The main factors of treatment failure are both drug resistance and intolerance. In some cases, Cytotect®CP CMV-hyperimmune globulin is used as salvage therapy. This study aims to investigate the safety and efficacy of Cytotect®CP as a salvage therapy in patients with CMV infection after allo-HCT. Twenty-three consecutive patients received ...
Tópico(s): Neonatal Health and Biochemistry
2018 - Springer Nature | Bone Marrow Transplantation
Natalia Stach, Magdalena Kalińska, Michal Zdzalik, Radosław Kitel, A. Karim, Karol Serwin, Wioletta Rut, Katrine S. Larsen, Abeer Jabaiah, Magdalena Firlej, Benedykt Władyka, Patrick S. Daugherty, Henning R. Stennicke, Marcin Drąg, Jan Potempa, Grzegorz Dubin,
Staphylococcus aureus is a dangerous human pathogen characterized by alarmingly increasing antibiotic resistance. Accumulating evidence suggests the role of Spl proteases in staphylococcal virulence. Spl proteases have restricted, non-overlapping substrate specificity, suggesting that they may constitute a first example of a proteolytic system in bacteria. SplA, SplB, and SplD were previously characterized in terms of substrate specificity and structural determinants thereof. Here we analyze the ...
Tópico(s): Bacterial Genetics and Biotechnology
2018 - Elsevier BV | Structure
Till Siebenmorgen, Filipe Menezes, Sabrina Benassou, Erinç Merdivan, Kieran Didi, André Mourão, Radosław Kitel, Píetro Lió, Stefan Kesselheim, Marie Piraud, Fabian J. Theis, Michael Sattler, Grzegorz M. Popowicz,
Large language models have greatly enhanced our ability to understand biology and chemistry, yet robust methods for structure-based drug discovery, quantum chemistry and structural biology are still sparse. Precise biomolecule-ligand interaction datasets are urgently needed for large language models. To address this, we present MISATO, a dataset that combines quantum mechanical properties of small molecules and associated molecular dynamics simulations of ~20,000 experimental protein-ligand complexes ...
Tópico(s): Protein Structure and Dynamics
2024 - Nature Portfolio | Nature Computational Science
Damian Muszak, Ewa Surmiak, Jacek Plewka, Katarzyna Magiera‐Mularz, Justyna Kocik, Bogdan Musielak, Dominik Sala, Radosław Kitel, Małgorzata Stec, Kazimierz Węglarczyk, Maciej Siedlar, Alexander Dömlingꝉ, Łukasz Skalniak, Tad A. Holak,
We describe a new class of potent PD-L1/PD-1 inhibitors based on a terphenyl scaffold that is derived from the rigidified biphenyl-inspired structure. Using in silico docking, we designed and then experimentally demonstrated the effectiveness of the terphenyl-based scaffolds in inhibiting PD-1/PD-L1 complex formation using various biophysical and biochemical techniques. We also present a high-resolution structure of the complex of PD-L1 with one of our most potent inhibitors to identify key PD-L1/ ...
Tópico(s): Pharmacological Receptor Mechanisms and Effects
2021 - American Chemical Society | Journal of Medicinal Chemistry
Ewa Surmiak, Katarzyna Magiera‐Mularz, Bogdan Musielak, Damian Muszak, Justyna Kocik, Radosław Kitel, Jacek Plewka, Tad A. Holak, Łukasz Skalniak,
Targeting the programmed cell death protein 1/programmed cell death 1 ligand 1 (PD-1/PD-L1) interaction has become an established strategy for cancer immunotherapy. Although hundreds of small-molecule, peptide, and peptidomimetic inhibitors have been proposed in recent years, only a limited number of drug candidates show good PD-1/PD-L1 blocking activity in cell-based assays. In this article, we compare representative molecules from different classes in terms of their PD-1/PD-L1 dissociation capacity ...
Tópico(s): Immunotherapy and Immune Responses
2021 - Multidisciplinary Digital Publishing Institute | International Journal of Molecular Sciences
Roberto Butera, Marta A. Ważyńska, Katarzyna Magiera‐Mularz, Jacek Plewka, Bogdan Musielak, Ewa Surmiak, Dominik Sala, Radosław Kitel, Marco de Bruyn, Hans W. Nijman, Philip H. Elsinga, Tad A. Holak, Alexander Dömlingꝉ,
The PD-1/PD-L1 axis has proven to be a highly efficacious target for cancer immune checkpoint therapy with several approved antibodies. Also, small molecules based on a biphenyl core can antagonize PD-1/PD-L1, leading to the in vitro formation of PD-L1 dimers. However, their development remains challenging, as we do not yet fully understand their mode of action. In this work, we designed a new scaffold based on our previously solved high-resolution structures of low-molecular-weight inhibitors bound ...
Tópico(s): Click Chemistry and Applications
2021 - American Chemical Society | ACS Medicinal Chemistry Letters
Radosław Kitel, Anna Byczek-Wyrostek, Katarzyna Hopko, Anna Kasprzycka, Krzysztof Walczak,
The pharmacological effects of carbon to silicon bioisosteric replacements have been widely explored in drug design and medicinal chemistry. Here, we present a systematic investigation of the impact of different silyl groups on the anticancer activity of mucobromic acid (MBA) bearing furan-2(5H)-one core. We describe a comprehensive characterization of obtained compounds with respect to their anticancer potency and selectivity towards cancer cells. All four novel compounds exert stronger antiproliferative ...
Tópico(s): Synthesis and biological activity
2021 - Multidisciplinary Digital Publishing Institute | Pharmaceuticals
Radosław Kitel, Ismael Rodríguez, Xabier del Corte, Jack Atmaj, Magdalena Żarnik, Ewa Surmiak, Damian Muszak, Katarzyna Magiera‐Mularz, Grzegorz M. Popowicz, Tad A. Holak, Bogdan Musielak,
Development of small molecules targeting the PD-L1/PD-1 interface is advancing both in industry and academia, but only a few have reached early-stage clinical trials. Here, we take a closer look at the general druggability of PD-L1 using in silico hot spot mapping and nuclear magnetic resonance (NMR)-based characterization. We found that the conformational elasticity of the PD-L1 surface strongly influences the formation of hot spots. We deconstructed several generations of known inhibitors into ...
Tópico(s): CAR-T cell therapy research
2022 - American Chemical Society | ACS Chemical Biology
Wiesław Szeja, Grzegorz Grynkiewicz, Tadeusz Bieg, Piotr Świerk, Anna Byczek-Wyrostek, Katarzyna Papaj, Radosław Kitel, Aleksandra Rusin,
A series of glycoconjugates, derivatives of genistein containing a C-glycosylated carbohydrate moiety, were synthesized and their anticancer activity was tested in vitro in the human cell lines HCT 116 and DU 145. The target compounds 15–17 were synthesized by treating ω-bromoalkyl C-glycosides derived from L-rhamnal (1) with a tetrabutylammonium salt of genistein. The new, metabolically stable analogs of previously studied O-glycosidic genistein derivatives inhibited proliferation of cancer cell ...
Tópico(s): Probiotics and Fermented Foods
2014 - Multidisciplinary Digital Publishing Institute | Molecules
Mesfin Haile Kahissay, Teferi Gedif Fenta,
... traditional healers in the study communities were identified: Kitel Betash or Herbalists, ‘Awalaj’ or traditional birth ... of the study community considers traditional healing by Kitel Betash, Awalaj and Wogesha as a health care ...
Tópico(s): Global Maternal and Child Health
2015 - African Journals OnLine | Ethiopian Journal of Health Development
Natalia Stach, A. Karim, Przemysław Golik, Radosław Kitel, Katarzyna Pustelny, Natalia Gruba, Katarzyna Groborz, Urszula Jankowska, Sylwia Kędracka‐Krok, Benedykt Władyka, Marcin Drąg, Adam Lesner, Grzegorz Dubin,
Accumulating evidence suggests that six proteases encoded in the spl operon of a dangerous human pathogen, Staphylococcus aureus, may play a role in virulence. Interestingly, SplA, B, D, and E have complementary substrate specificities while SplF remains to be characterized in this regard. Here, we describe the prerequisites of a heterologous expression system for active SplF protease and characterize the enzyme in terms of substrate specificity and its structural determinants. Substrate specificity ...
Tópico(s): Antimicrobial Resistance in Staphylococcus
2021 - Multidisciplinary Digital Publishing Institute | International Journal of Molecular Sciences
Karolina Juszczak, Anna Kubicka, Radosław Kitel, Grzegorz Dzido, Magdalena Łabieniec-Watała, Serafin Zawadzki, Agnieszka Marczak, Krzysztof Walczak, Karolina Matczak, Mateusz D. Tomczyk,
Hexokinase 2 (HK2), an enzyme of the sugar kinase family, plays a dual role in glucose metabolism and mediating cancer cell apoptosis, making it an attractive target for cancer therapy. While positive HK2 expression usually promotes cancer cells survival, silencing or inhibiting this enzyme has been found to improve the effectiveness of anti-cancer drugs and even result in cancer cell death. Previously, benitrobenrazide (BNBZ) was characterized as a potent HK2 inhibitor with good anti-cancer activity ...
Tópico(s): Biochemical and Molecular Research
2022 - Multidisciplinary Digital Publishing Institute | International Journal of Molecular Sciences
Giada Mondanelli, Claudia Volpi, Ciriana Orabona, Ursula Grohmann,
... 2016).Crossref, Medline, CAS, Google Scholar3 Zak KM, Kitel R, Przetocka S et al. Structure of the ...
Tópico(s): Cancer, Stress, Anesthesia, and Immune Response
2017 - Future Science Ltd | Future Medicinal Chemistry
Charlotte Uetrecht, Kristina Lorenzen, Matthäus Kitel, Johannes Heidemann, Jesse Huron Robinson Spencer, Hartmut Schlüter, Joachim Schulz,
The SPB/SFX instrument at the European XFEL provides unique conditions for single-particle imaging (SPI) experiments due to its high brilliance, nano-focus and unique pulse structure. Promising initial results provided by the international LCLS (Linac Coherent Light Source) SPI initiative highlight the potential of SPI. Current available injection methods generally have high sample consumption and do not provide any options for pulsing, selection or orientation of particles, which poses a problem ...
Tópico(s): Mass Spectrometry Techniques and Applications
2019 - Wiley | Journal of Synchrotron Radiation
Florian Nietzold, Stefan Rubner, Beata Łabuzek, Przemysław Golik, Ewa Surmiak, Xabier del Corte, Radosław Kitel, Christoph Protzel, Regina Reppich‐Sacher, Jan Stichel, Katarzyna Magiera‐Mularz, Tad A. Holak, Thorsten Berg,
Abstract Nutlin‐3a is a reversible inhibitor of the p53/MDM2 interaction. We have synthesized the derivative Nutlin‐3a‐aa bearing an additional exocyclic methylene group in the piperazinone moiety. Nutlin‐3a‐aa is more active than Nutlin‐3a against purified wild‐type MDM2, and is more effective at increasing p53 levels and releasing transcription of p53 target genes from MDM2‐induced repression. X‐ray analysis of wild‐type MDM2‐bound Nutlin‐3a‐aa indicated that the orientation of its modified piperazinone ...
Tópico(s): Ubiquitin and proteasome pathways
2023 - Wiley | ChemBioChem
Zbigniew Dauter, Alexander Wlodawer,
... et al., 2018Stach N. Kalinska M. Zdzalik M. Kitel R. Karim A. Serwin K. Rut W. Larsen ... et al., 2018Stach N. Kalinska M. Zdzalik M. Kitel R. Karim A. Serwin K. Rut W. Larsen ... et al., 2018Stach N. Kalinska M. Zdzalik M. Kitel R. Karim A. Serwin K. Rut W. Larsen ... et al., 2018Stach N. Kalinska M. Zdzalik M. Kitel R. Karim A. Serwin K. Rut W. Larsen ... et al., 2018Stach N. Kalinska M. Zdzalik M. Kitel R. Karim A. Serwin K. Rut W. Larsen ... et al., 2018Stach N. Kalinska M. Zdzalik M. Kitel R. Karim A. Serwin K. Rut W. Larsen ...
Tópico(s): Antimicrobial Peptides and Activities
2018 - Elsevier BV | Structure
Wiktor Uzar, B.Z. Kaminska, Hubert Rybka, Łukasz Skalniak, Katarzyna Magiera‐Mularz, Radosław Kitel,
PD-L1, via its interactions with PD-1, constitutes a key immune checkpoint that allows cancer cells to escape immune surveillance. Targeting PD-1/PD-L1 with monoclonal antibodies (mAbs) led to spectacular success in clinical oncology. However, the inherent limitations of mAbs and increasing findings about immune-related adverse events (iRAEs) prompted intense research in the field of small-molecule inhibitors of PD-L1.
Tópico(s): CAR-T cell therapy research
2024 - Taylor & Francis | Expert Opinion on Therapeutic Patents
A Collet, Christophe Zawadzki, Emmanuelle Jeanpierre, Caroline Kitel, Sylvain Dubucquoi, É. Hachulla, Sophie Susen, David Launay,
Systemic sclerosis (SSc) is an autoimmune disease associated with endothelial activation and fibrosis. Non-O blood group patients carry an increased risk of thrombosis, fibrosis and autoimmune diseases. The aim of our work was to evaluate the distribution of ABO groups in SSc patients and their association with the disease’s characteristics. ABO groups were determined in 504 SSc patients (with 131 completed by a genotypic analysis). The distribution of ABO groups and their diplotypes in SSc patients ...
Tópico(s): Genetic Syndromes and Imprinting
2022 - Multidisciplinary Digital Publishing Institute | Journal of Clinical Medicine
Kitel, Wilhelm, Silicate Melt Equilibria, Rutgers University Press, New Brunswick, New Jersey, x + 159 pp., 200 illustrations, ...
1955 - American Geophysical Union | Transactions American Geophysical Union
... the Much Lamented Death of Mrs. Mehite-bell Kitel.” Described as “[e]xtraordinary” and “moving,” it turns ...
Tópico(s): American Literature and Humor Studies
2017 - University of North Carolina Press | Early American literature
Alexey V. Okulov, С.А. КУНГУРЦЕВА,
... that the unworked almandine garnet came from the Kitel deposit in the northern Ladoga region. The studies ...
Tópico(s): Mineralogy and Gemology Studies
2023 - | Краткие сообщения Института археологии (КСИА)
Paweł Mirski, Alexander Yu. Ivanov, Denis Kitel, Tomasz Tumiel,
We conducted a pilot study to investigate breeding dispersal and ranging behaviour of two adult female Great Grey Owls in central Belarus. The females stayed within a few kilometres of their breeding site and ranged only 2–3 km on average and at night.
Tópico(s): Animal Ecology and Behavior Studies
2021 - Taylor & Francis | Bird Study
Produção Nacional
João Carlos Dos Reis Carneiro de Oliveira,
... assunto, utilizava-se amplamente a teoria da elasticidade (Kitel, 2006). Todavia, a proposta geométrica deu novos rumos ...
Tópico(s): Material Selection and Properties
2021 - UNIVERSIDADE ESTADUAL DE FEIRA DE SANTANA | Anais do ... Seminário de Iniciação Científica/Anais Seminário de Iniciação Científica
Maria Hoyer, Álvaro H. Crevenna, Radosław Kitel, Kherim Willems, Mirosława Czub, Grzegorz Dubin, Pol Van Dorpe, Tad A. Holak, Don C. Lamb,
Abstract Protein assembly plays an important role throughout all phyla of life, both physiologically and pathologically. In particular, aggregation and polymerization of proteins are key-strategies that regulate cellular function. In recent years, methods to experimentally study the assembly process on a single-molecule level have been developed. This progress concomitantly has triggered the question of how to analyze this type of single-filament data adequately and what experimental conditions ...
Tópico(s): Advanced Polymer Synthesis and Characterization
2022 - Nature Portfolio | Scientific Reports
Grzegorz Porębski, Alicja Dziadowiec, Hubert Rybka, Radoslaw Kitel, Mateusz Kwitniewski,
Initiation of the bradykinin generation cascade is responsible for the occurrence of attacks in some types of angioedema without wheals. Hereditary angioedema due to C1 inhibitor deficiency (HAE-C1-INH) is one such clinical entity. In this paper, we explore the existing evidence that mast cells (MCs) degranulation may contribute to the activation of the kallikrein-kinin system cascade, followed by bradykinin formation and angioedema. We present the multidirectional effects of MC-derived heparin and ...
Tópico(s): Urticaria and Related Conditions
2024 - Frontiers Media | Frontiers in Immunology