Results 241 to 250 of about 504,672 (298)

Synergistische Entwicklungsstrategien von Inhibitoren gegen humane UDP‐Galactose‐4‐Epimerase

Angewandte Chemie, EarlyView.
Die Epimerase GalE ist essenziell für die Biosynthese von krebsrelevanten O‐GalNAc Glykanen. Wir verwenden orthogonales, strukturbasiertes Screening niedermolekularer Fragmente an, um kovalente und nichtkovalente Inhibitoren gegen GalE mit nicht mehr als 22 optimierten Verbindungen zu erhalten.
William M. Browne, Jonathan Pettinger, Teresa Weckwerth, Andrew Purkiss, Sing Hei Lok, Louisa Penicaut, Roksana Ogrodowicz, Raveena Prema, Simone Kunzelmann, Chloe Roustan, Ganka Bineva‐Todd, Saskia Pieters, Francesca Zappacosta, Alfred E. Doherty, Isobel Oram, Christelle Soudy, Robert Quinlan, Joanna Redmond, Svend Kjaer, David House, Stephane Mouilleron, Jacob T. Bush, Benjamin Schumann   +22 more
wiley   +1 more source

RaPID Selection of Backbone Macrocyclic Peptides Targeting Akt2

Angewandte Chemie, EarlyView.
Backbone macrocyclic peptide library (BMP) library was screened against Akt2 via RaPID to discover potent BMPPakti‐3 (IC50 = 34 nM). ABSTRACT Backbone‐cyclic peptides (BMPs) are an attractive class of molecules appeared in diverse natural bioactive products. However, mRNA display technology coupled with ribosomal synthesis is intrinsically inapplicable
Koki Shinbara, Ekishin Yanagi, Ayaka Aizawa, Takayuki Katoh, Hiroaki Suga   +4 more
wiley   +2 more sources

Concentration-Dependent Anticancer Effects of Melittin-Functionalized Nanomaterials. [PDF]

Materials (Basel)
Câmpian A, Florea A.
europepmc   +1 more source

Antileishmanial Activity of <i>Schinus terebinthifolia</i> Essential Oil: Chemistry, In Vitro and Mechanistic Studies. [PDF]

Molecules
Monzote L, Betancourt L, Scull R, Satyal P, Gil L, Gille L, Setzer WN.   +6 more
europepmc   +1 more source

The effects of Palbociclib and Ferulic acid combination on cellular processes in breast cancer. [PDF]

Discov Oncol
Bayav I, Tokgun PE, Ergezgin H, Tomatir AG.   +3 more
europepmc   +1 more source

Phenolic Profile and Antioxidant Capacity of Extracts from Papache (<i>Randia echinocarpa</i> Moc. & Sessé Ex DC), a Plant Used in Traditional Mexican Medicine. [PDF]

Plants (Basel)
Lugo-Gamboa RR, Muñoz-Sevilla NP, Apún-Molina JP, Fierro-Coronado JA, Cruz-Mendívil A, Espinoza-Ortiz M, Valdez-Morales M, Santamaria-Miranda A.   +7 more
europepmc   +1 more source

A Synergistic Inhibitor Development Strategy Against Human UDP‐Galactose‐4‐Epimerase

Angewandte Chemie International Edition, EarlyView.
The epimerase GalE is crucial for the biosynthesis of cancer‐relevant O‐GalNAc glycans. Here, we employ orthogonal, structurally enabled small molecule fragment screens to yield both covalent and non‐covalent inhibitors against GalE within no more than 22 elaborated compounds.
William M. Browne, Jonathan Pettinger, Teresa Weckwerth, Andrew Purkiss, Sing Hei Lok, Louisa Penicaut, Roksana Ogrodowicz, Raveena Prema, Simone Kunzelmann, Chloe Roustan, Ganka Bineva‐Todd, Saskia Pieters, Francesca Zappacosta, Alfred E. Doherty, Isobel Oram, Christelle Soudy, Robert Quinlan, Joanna Redmond, Svend Kjaer, David House, Stephane Mouilleron, Jacob T. Bush, Benjamin Schumann   +22 more
wiley   +1 more source

Tetrahydrocarbazole as a Versatile Scaffold in Drug Discovery: A Cross-Target SAR Analysis and Design Paradigms. [PDF]

Molecules
Ma M, Luo S, An S, Nie Z, Wei Z, Zong J, Li X, Wang C, Tang Y, Yao L.   +9 more
europepmc   +1 more source