Results 71 to 80 of about 14,786 (290)

Navigating PROTACs in Cancer Therapy: Advancements, Challenges, and Future Horizons

Food Science & Nutrition
Proteolysis Targeting Chimeras (PROTACs) have revolutionized cancer therapy by offering a selective and innovative approach to degrade key oncogenic proteins associated with various malignancies.
Saooda Ibrahim, Muhammad Umer Khan, Iqra Khurram, Raima Rehman, Abdur Rauf, Zubair Ahmad, Abdullah S. M. Aljohani, W. Al Abdulmonem, M. M. Quradha   +8 more
semanticscholar   +1 more source

Semiconducting polymer nano-PROTACs for activatable photo-immunometabolic cancer therapy

Nature Communications, 2021
Immunometabolic intervention has been applied to treat cancer via inhibition of certain enzymes associated with intratumoral metabolism. However, small-molecule inhibitors and genetic modification often suffer from insufficiency and off-target side ...
Chi Zhang, Ziling Zeng, Dong Cui, Shasha He, Yuyan Jiang, Jingchao Li, Jiaguo Huang, Kanyi Pu   +7 more
semanticscholar   +1 more source

Cell wall target fragment discovery using a low‐cost, minimal fragment library

FEBS Letters, EarlyView.
LoCoFrag100 is a fragment library made up of 100 different compounds. Similarity between the fragments is minimized and 10 different fragments are mixed into a single cocktail, which is soaked to protein crystals. These crystals are analysed by X‐ray crystallography, revealing the binding modes of the bound fragment ligands.
Kaizhou Yan, Mathew Stanley, Olawale Raimi, Andrew T. Ferenbach, Helge C Dorfmueller, Daan M. F. van Aalten   +5 more
wiley   +1 more source

PROTACs: Mechanism and Bioavailability enhancement strategies by nanotechnology, RNA viral infections (vaccine strategy) and Prodrug development

German Journal of Pharmaceuticals and Biomaterials
Proteolysis Targeting Chimera (PROTACs) are a brand-new concept of therapeutics that use the ubiquitin-proteasome system for selective degradation of disease-related proteins.
Sanaul Mustafa, Md Sabir Hussain Siddiquee   +1 more
doaj   +3 more sources

Homo-PROTACs:bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation [PDF]

, 2017
E3 ubiquitin ligases are key enzymes within the ubiquitin proteasome system which catalyze the ubiquitination of proteins, targeting them for proteasomal degradation.
A Grosfeld, A Hergovich, A Rapisarda, A Schoenfeld, AC Lai, AC Lai, AR Schoenfeld, B Vu, C Galdeano, C Galdeano, C Loenarz, CE Stebbins, CH Arrowsmith, CM Pickart, CM Robinson, D Komander, DC Swinney, DE Feldman, DL Buckley, DL Buckley, DM Spencer, DP Bondeson, E Bulatov, EF Douglass, EK Schrader, ES Fischer, ET Mack, FE Morreale, G Chessari, G Lu, G Minervini, G Nalepa, G Petzold, GE Winter, H Lebraud, H Sun, I Molle Van, IJ Frew, J Frost, J Krönke, J Lu, JR Skaar, K Raina, L Gossage, LT Vassilev, M Li, M Tanaka, M Toure, M Zengerle, MD Petroski, ME Matyskiela, MR Arkin, MS Gadd, N Ohoka, N Zheng, PH Maxwell, RE Barry, T Han, T Ito, T Kamura, T Uehara, TA Soucy, TB Durham, TG Davies, TK Oost, TW Corson, V Bangiyeva, V Wittmann, WG Kaelin, X Huang, X Lucas, X Tan, Y Itoh, Z-Y Jiang   +73 more
core   +3 more sources

Engineering of Glioblastoma‐Derived Biomimetic Vesicles and Their Structural and Molecular Features

Advanced Healthcare Materials, EarlyView.
ABSTRACT Biomimetic nanosystems and vesicles have arisen as a novel approach to design vesicular transport systems with diverse therapeutic potential. The ‘biomimetic’ strategy involves the integration of cell membrane components into lipid bilayers, conferring them with biological properties originating from the cell of origin. Until now, most studies
Noelia Hernández‐Lobato, Hanan Abumanhal‐Masarweh, Martí de Cabo, Pablo Guerra, Marilena Hadjidemetriou, Neus Lozano, Kostas Kostarelos   +6 more
wiley   +1 more source

Potent and selective chemical probe of hypoxic signaling downstream of HIF-α hydroxylation via VHL inhibition [PDF]

, 2016
Chemical strategies to using small molecules to stimulate hypoxia inducible factors (HIFs) activity and trigger a hypoxic response under normoxic conditions, such as iron chelators and inhibitors of prolyl hydroxylase domain (PHD) enzymes, have broad ...
A Melvin, A Rapisarda, A Rentsch, A Robinson, AC Lai, AJ Majmundar, AW Schüttelkopf, B Ortmann, C Briggs, C Galdeano, C Loenarz, C Waugh, C Willam, CE Stebbins, CH Arrowsmith, CJ Schofield, CYM Okumura, D Martinez Molina, D Wu, DA Chan, DK Finlay, DL Buckley, DL Buckley, DP Bondeson, E Bulatov, E Muchnik, ER Maher, G Camurri, G Ramsay, GL Semenza, GL Semenza, GL Wang, GN Murshudov, GN Murshudov, HK Eltzschig, I Van Molle, IC Macdougall, IH Jain, J-H Min, JA Wells, JR Gnarra, JW Banks, K Valko, KKW To, L Gossage, M Bantscheff, M Ivan, M Li, M Toure, M Zengerle, MA McDonough, MC Chan, MD Winn, ME Bunnage, MH Rabinowitz, P Emsley, P Hill, P Jaakkola, PH Maxwell, PP Kapitsinou, PR Evans, R Chowdhury, R Mehta, R Provenzano, RK Bruick, S Rey, SF Ehrentraut, SS Karuppagounder, T Eckle, T Kamura, TA Soucy, VB Chen, VH Haase, W Kabsch, W-C Hon, WG Kaelin, WG Kaelin, X Huang, X Liu   +78 more
core   +7 more sources

Inhibition of bromodomain and extra-terminal (BET) proteins increases NKG2D ligand MICA expression and sensitivity to NK cell-mediated cytotoxicity in multiple myeloma cells. role of cMYC-IRF4-miR-125b interplay [PDF]

, 2016
Background: Anticancer immune responses may contribute to the control of tumors after conventional chemotherapy and different observations have indicated that chemotherapeutic agents can induce immune responses resulting in cancer cell death and immune ...
Abruzzese, MARIA PIA, Bilotta, MARIA TERESA, Borrelli, Cristiana, Cippitelli, Marco, Fionda, Cinzia, Molfetta, Rosa, Paolini, Rossella, Petrucci, MARIA TERESA, Ricciardi, Maria Rosaria, Santoni, Angela, Soriani, Alessandra, Vulpis, Elisabetta, Zingoni, Alessandra, Zitti, Beatrice   +13 more
core   +15 more sources

An Affinity-directed PROtein Missile (AdPROM) system for targeted proteolysis [PDF]

, 2016
The von Hippel-Lindau (VHL) protein serves to recruit the hypoxia inducible factor alpha (HIF1α) protein under normoxia to the CUL2 E3 ubiquitin ligase for its ubiquitylation and degradation through the proteasome.
Bozatzi, Polyxeni, Fulcher, Luke, Hornberger, Annika, Macartney, Thomas, Rojas-Fernandez, Alejandro, Sapkota, Gopal   +5 more
core   +3 more sources

PROTACs targeting epigenetic proteins

Acta Materia Medica, 2023
The field of epigenetics pertains to alterations in gene function that are inherited without changes in the DNA sequence, including histone modifications, post-translational modifications of amino acids, and covalent modifications of DNA bases. These alteration pathways modulate the transformation of genotypes into specific phenotypes.
Chao Zhang, Yuna He, Xiuyun Sun, Wenyi Wei, Yanlong Liu, Yu Rao   +5 more
openaire   +3 more sources