Novel Tryptophan Hydroxylase Inhibitor TPT-001 Reverses PAH, Vascular Remodeling, and Proliferative-Proinflammatory Gene Expression

Authors: Legchenko, Ekaterina ^a, Chouvarine, Philippe ^a, Qadri, Fatimunnisa ^b, Specker, Edgar ^{c, d}, Nazaré, Marc ^c, Wesolowski, Radoslaw ^{b, d}, Matthes, Susann ^b, Bader, Michael ^{b, d, e, f, g}, Hansmann, Georg ^{a, h, ∗}

Source: In JACC: Basic to Translational Science July 2024 9(7):890-902

Antagonistic control of active surface integrins by myotubularin and phosphatidylinositol 3-kinase C2β in a myotubular myopathy model

Authors: Samsó, Paula, Koch, Philipp A., Posor, York, Lo, Wen-Ting, Belabed, Hassane, Nazare, Marc, Laporte, Jocelyn, Haucke, Volker

Source: Proceedings of the National Academy of Sciences of the United States of America, 2022 Oct 01. 119(40), 1-10.

Access URL: https://www.jstor.org/stable/27208449

Discovery of tetrazolo-pyridazine-based small molecules as inhibitors of MACC1-driven cancer metastasis

Authors: Yan, Shixian, Schöpe, Paul Curtis, Lewis, Joe, Putzker, Kerstin, Uhrig, Ulrike, Specker, Edgar, von Kries, Jens Peter, Lindemann, Peter, Omran, Anahid, Sanchez-Ibarra, Hector E., Unger, Anke, Zischinsky, Mia-Lisa, Klebl, Bert, Walther, Wolfgang, Nazaré, Marc, Kobelt, Dennis, Stein, Ulrike

Source: In Biomedicine & Pharmacotherapy December 2023 168

Isoform-selective targeting of PI3K: time to consider new opportunities?

Authors: Cirillo, Davide, Diceglie, Marta, Nazaré, Marc

Source: In Trends in Pharmacological Sciences September 2023 44(9):601-621

Donor manipulation for constructing a pH sensing thermally activated delayed fluorescent probe to detect alkaliphiles

Authors: Liu, Qian, Yang, Miao, Meng, Xiangchuan, Han, Xiaowan, Nazare, Marc, Xu, Youjun, Hu, Hai-Yu, Zhang, Qingyang

Source: In Talanta 15 August 2022 246

Designed nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells

Authors: Barone, Matthias, Müller, Matthias, Chiha, Slim, Ren, Jiang, Albat, Dominik, Soicke, Arne, Dohmen, Stephan, Klein, Marco, Bruns, Judith, van Dinther, Maarten, Opitz, Robert, Lindemann, Peter, Beerbaum, Monika, Motzny, Kathrin, Roske, Yvette, Schmieder, Peter, Volkmer, Rudolf, Nazaré, Marc, Heinemann, Udo, Oschkinat, Hartmut, Dijke, Peter ten, Schmalz, Hans-Günther, Kühne, Ronald

Source: Proceedings of the National Academy of Sciences of the United States of America, 2020 Nov . 117(47), 29684-29690.

Access URL: https://www.jstor.org/stable/26970821

A pharmacological master key mechanism that unlocks the selectivity filter gate in K⁺ channels

Authors: Schewe, Marcus, Sun, Han, Mert, Ümit, Mackenzie, Alexandra, Pike, Ashley C. W., Schulz, Friederike, Constantin, Cristina, Vowinkel, Kirsty S., Conrad, Linus J., Kiper, Aytug K., Gonzalez, Wendy, Musinszki, Marianne, Tegtmeier, Marie, Pryde, David C., Belabed, Hassane, Nazare, Marc, de Groot, Bert L., Decher, Niels, Fakler, Bernd, Carpenter, Elisabeth P., Tucker, Stephen J., Baukrowitz, Thomas

Source: Science, 2019 Feb . 363(6429), 875-880.

Access URL: https://www.jstor.org/stable/26762240

EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

Authors: Brennecke, Philip, Rasina, Dace, Aubi, Oscar, Herzog, Katja, Landskron, Johannes, Cautain, Bastien, Vicente, Francisca, Quintana, Jordi, Mestres, Jordi, Stechmann, Bahne, Ellinger, Bernhard, Brea, Jose, Kolanowski, Jacek L., Pilarski, Radosław, Orzaez, Mar, Pineda-Lucena, Antonio, Laraia, Luca, Nami, Faranak, Zielenkiewicz, Piotr, Paruch, Kamil, Hansen, Espen, von Kries, Jens P., Neuenschwander, Martin, Specker, Edgar, Bartunek, Petr, Simova, Sarka, Leśnikowski, Zbigniew, Krauss, Stefan, Lehtiö, Lari, Bilitewski, Ursula, Brönstrup, Mark, Taskén, Kjetil, Jirgensons, Aigars, Lickert, Heiko, Clausen, Mads H., Andersen, Jeanette H., Vicent, Maria J., Genilloud, Olga, Martinez, Aurora, Nazaré, Marc, Fecke, Wolfgang ^**, Gribbon, Philip ^*

Source: In SLAS Discovery March 2019 24(3):398-413

A New Highly Thyrotropin Receptor-Selective Small-Molecule Antagonist with Potential for the Treatment of Graves' Orbitopathy

Authors: Marcinkowski, Patrick, Hoyer, Inna, Specker, Edgar, Furkert, Jens, Rutz, Claudia, Neuenschwander, Martin, Sobottka, Sebastian, Sun, Han, Nazare, Marc, Berchner-Pfannschmidt, Utta, von Kries, Jens Peter, Eckstein, Anja, Schülein, Ralf, Krause, Gerd

Source: Thyroid. 29(1):111-123

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100083436011.0x000001&indx=1&recIds=ETOCvdc_100083436011.0x000001

Identification of a Novel Benzimidazole Pyrazolone Scaffold That Inhibits KDM4 Lysine Demethylases and Reduces Proliferation of Prostate Cancer Cells

Authors: Carter, David M., Specker, Edgar, Przygodda, Jessica, Neuenschwander, Martin, von Kries, Jens Peter, Heinemann, Udo, Nazaré, Marc ^*, Gohlke, Ulrich ^**

Source: In SLAS Discovery August 2017 22(7):801-812

DOTA‐Based Plectin‐1 Targeted Contrast Agent Enables Detection of Pancreatic Cancer in Human Tissue.

Authors: Gazzi, Thais¹, Lesina, Marina², Wang, Qinghua³, Berninger, Alexandra², Radetzki, Silke¹, Demir, Ihsan Ekin⁴, Kohlmann, Larissa², Meiser, Waldemar¹, Wilke, Sebastian¹, von Kries, Jens Peter¹, Algül, Hana², hana.alguel@tum.de, Hu, Hai‐Yu³, haiyu.hu@imm.ac.cn, Nazare, Marc¹, nazare@fmp-berlin.de

Source: Angewandte Chemie International Edition; Jun2024, Vol. 63 Issue 26, p1-8, 8p

Phosphoinositide Conversion Inactivates R‐RAS and Drives Metastases in Breast Cancer

Authors: Li, Huayi, Prever, Lorenzo, Hsu, Myriam Y., Lo, Wen‐Ting, Margaria, Jean Piero, De Santis, Maria Chiara, Zanini, Cristina, Forni, Marco, Novelli, Francesco, Pece, Salvatore, Di Fiore, Pier Paolo, Porporato, Paolo Ettore, Martini, Miriam, Belabed, Hassane, Nazare, Marc, Haucke, Volker, Gulluni, Federico, Hirsch, Emilio

Source: Advanced science. 9(9)

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100145487968.0x000001&indx=1&recIds=ETOCvdc_100145487968.0x000001

A novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging

Authors: Liu, Yun, Zhang, Leilei, Nazare, Marc, Yao, Qingqiang, Hu, Hai-Yu

Source: Acta pharmaceutica sinica B. 8(3):401-408

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100094685939.0x000001&indx=1&recIds=ETOCvdc_100094685939.0x000001

CLK2 and CLK4 are regulators of DNA damage-induced NF-κB targeted by novel small molecule inhibitors

Authors: Mucka, Patrick, Lindemann, Peter, Bosco, Bartolomeo, Willenbrock, Michael, Radetzki, Silke, Neuenschwander, Martin, Brischetto, Cristina, Peter von Kries, Jens, Nazaré, Marc, Scheidereit, Claus

Source: In Cell Chemical Biology 19 October 2023 30(10):1303-1312

DOTAM Derivatives as Active Cartilage-Targeting Drug Carriers for the Treatment of Osteoarthritis

Authors: Hu, Hai-Yu, Lim, Ngee-Han, Ding-Pfennigdorff, Danping, Saas, Joachim, Wendt, K. Ulrich, Ritzeler, Olaf, Nagase, Hideaki, Plettenburg, Oliver, Schultz, Carsten, Nazare, Marc

Source: Bioconjugate chemistry. 26(3):383-388

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCRN631131784&indx=1&recIds=ETOCRN631131784

Small molecule inhibiting microglial nitric oxide release could become a potential treatment for neuroinflammation.

Authors: Jordan, Philipp, Costa, Amanda, Specker, Edgar, Popp, Oliver, Volkamer, Andrea, Piske, Regina, Obrusnik, Tessa, Kleissle, Sabrina, Stuke, Kevin, Rex, Andre, Neuenschwander, Martin, von Kries, Jens Peter, Nazare, Marc, Mertins, Phillip, Kettenmann, Helmut, Wolf, Susanne A.

Source: PLoS ONE; 2/6/2023, Vol. 18 Issue 2, p1-33, 33p

Subject Terms: SMALL molecules, NITRIC oxide, NITRIC-oxide synthases, MASS spectrometry, MICROGLIA

Quinoline-carboxamide derivatives as P2Y12 antagonists

Process for the palladium-catalyzed coupling of terminal alkynes with aryl tosylates

Transition metal catalyzed synthesis of 2H-indazoles

Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles