Results 91 to 100 of about 1,166,800 (296)

Cystatin activity–based protease profiling to select protease inhibitors useful in plant protection

, 2020
Protease inhibitors of the cystatin protein superfamily show potential in plant protection for the control of herbivorous pests. Here, we describe a cystatin activity–based profiling procedure for the selection of potent cystatin candidates, using single
Sainsbury, Frank, Michaud, Dominique, Marie-Claire Goulet, Frank Sainsbury, Michaud, D, Goulet, Marie-Claire, Dominique Michaud, Goulet, MC, Sainsbury, F   +8 more
core   +1 more source

IMPDH inhibition enhances cytarabine efficacy in SAMHD1‐expressing leukaemia cells via guanine nucleotide depletion

Molecular Oncology, EarlyView.
Cytarabine is a key therapy for acute myeloid leukaemia (AML), but its efficacy is limited by the dNTPase SAMHD1, which hydrolyses its active metabolite. Screening nucleotide biosynthesis inhibitors revealed that IMPDH inhibitors selectively sensitise SAMHD1‐proficient AML cells to cytarabine.
Miriam Yagüe‐Capilla, Christopher Dirks, Caroline Eiden, Sonja K. Fesenmayer, Femke M. Hormann, Yolande Klootsema, Ingrid Lilienthal, Si Min Zhang, Nikolas Herold, Sean G. Rudd   +9 more
wiley   +1 more source

The effects of protease inhibitors on basal and insulin-stimulated lipid metabolism, insulin binding, and signaling

Journal of Lipid Research, 2003
The objective of our research was to investigate the effects of the protease inhibitors ritonavir, saquinavir, and indinavir on triglyceride synthesis, lipolysis, insulin binding, and signaling in differentiating 3T3 L1 pre-adipocytes.
Catarina Cammalleri, Ralph J. Germinario
doaj   +1 more source

Trypsin inhibition by macrocyclic and open-chain variants of the squash inhibitor MCoTI-II [PDF]

, 2005
MCoTl-I and MCoTl-II from the seeds of Momordica cochinchinensis are inhibitors of trypsin-like proteases and the only known members of the large family of squash inhibitors that are cyclic and contain an additional loop connecting the amino- and the ...
Avrutina, Olga, Gabrijelcic-Geiger, Dusica, Le Nguyen, Dung, Schmoldt, H. U., Sommerhoff, Christian P., Kolmar, Harald, Gabrijelcic-Geiger, D., Le Nguyen, D., Schmoldt, Hans-Ulrich, Diederichsen, Ulf   +9 more
core   +1 more source

KDM7A and KDM1A inhibition suppresses tumour promoting pathways in prostate cancer

Molecular Oncology, EarlyView.
Treatment resistance is a major challenge for patients with advanced prostate cancer. This study examined an alternative approach to target the major prostate cancer‐promoting pathway by targeting epigenetic factors, whose levels are higher in tumours.
Jennie N Jeyapalan, Veronika M Metzler, Simone de Brot, Corinne L Woodcock, Anna E Harris, Jennifer Lothion‐Roy, Emeli M Nilsson, Atara Ntekim, Michael S Toss, Jenny L Persson, Francesca Khani, Brian D Robinson, Lorraine J Gudas, Emad Rakha, David M Heery, Catrin S Rutland, Nigel P Mongan   +16 more
wiley   +1 more source

Developing HIV-1 Protease Inhibitors through Stereospecific Reactions in Protein Crystals

Molecules, 2016
Protease inhibitors are key components in the chemotherapy of HIV infection. However, the appearance of viral mutants routinely compromises their clinical efficacy, creating a constant need for new and more potent inhibitors.
Folasade M. Olajuyigbe, Nicola Demitri, Rita De Zorzi, Silvano Geremia   +3 more
doaj   +1 more source

Mice lacking protease nexin-1 show delayed structural and functional recovery after sciatic nerve crush [PDF]

, 2007
Multiple molecular mechanisms influence nerve regeneration. Because serine proteases were shown to affect peripheral nerve regeneration, we performed nerve crush experiments to study synapse reinnervation in adult mice lacking the serpin protease nexin-1
Atanasoski, Suzana, Suter, Ueli, Kvajo, Mirna, Fayard, Bérengère, Moreno, Eliza, Lino, Maria Maddalena, Brenner, Hans Rudolf, Monard, Denis   +7 more
core   +1 more source

Hijacking emergency granulopoiesis: Neutrophil ontogeny and reprogramming in cancer

Molecular Oncology, EarlyView.
Neutrophils are highly plastic innate immune cells; their functions in cancer extend beyond the tumour microenvironment. This Review summarises current understanding of neutrophil maturation and heterogeneity and highlights tumour‐induced granulopoiesis as a systemic programme that expands immature, immunosuppressive neutrophils via tumour‐derived ...
Gabriela Marinescu, Yi Feng
wiley   +1 more source

Peptide inhibitors of hepatitis C virus NS3 protease

, 2003
Hepatitis C virus (HCV) is a highly prevalent virus and one of the major agents of chronic hepatitis. Since HCV NS3 protease is essential for the processing of HCV polyprotein, this protease is a target of choice to control HCV replication.
García-Delgado, M. (Marina), Vizmanos-Pérez, J.L. (José Luis), Lasarte, J.J. (Juan José), Borras-Cuesta, F. (Francisco), Gonzalez-Navarro, C.J. (Carlos Javier), Portal, S. (Sergio)   +5 more
core  

Loss of IGF‐1R impairs DNA‐PKcs recruitment to chromatin leading to defective end‐joining

Molecular Oncology, EarlyView.
IGF‐1R promotes radioresistance by facilitating DNA‐PKcs recruitment to chromatin, enabling non‐homologous end‐joining (NHEJ) repair of double‐strand breaks. Inhibition or loss of IGF‐1R disrupts this recruitment to damage sites, driving compensatory reliance on microhomology‐mediated end‐joining (MMEJ) repair.
Matthew O. Ellis, Jack V. Mills, Wojciech Niedzwiedz, Valentine M. Macaulay   +3 more
wiley   +1 more source