Results 81 to 90 of about 3,573,509 (380)

Accessory mutations balance the marginal stability of the HIV-1 protease in drug resistance

, 2020
The HIV-1 protease is a major target of inhibitor drugs in AIDS therapies. The therapies are impaired by mutations of the HIV-1 protease that can lead to resistance to protease inhibitors.
Hemmateenejad, B., Weikl, T.
core   +1 more source

Personalizing HIV therapy, mission impossible? [PDF]

, 2012
Sustained HIV suppression depends on a number of factors including therapy adherence, management of side effects, viral resistance and individual characteristics of patients and therapeutic settings.
Hentig, Nils von
core   +1 more source

Cyclic nucleotide signaling as a drug target in retinitis pigmentosa

FEBS Letters, EarlyView.
Disruptions in cGMP and cAMP signaling can contribute to retinal dysfunction and photoreceptor loss in retinitis pigmentosa. This perspective examines the mechanisms and evaluates emerging evidence on targeting these pathways as a potential therapeutic strategy to slow or prevent retinal degeneration.
Katri Vainionpää, Ahmed B. Montaser, Henri Leinonen   +2 more
wiley   +1 more source

Commentary on the role of treatment-related HIV compensatory mutations on increasing virulence: new discoveries twenty years since the clinical testing of protease inhibitors to block HIV-1 replication

BMC Medicine, 2012
Approximately 20 years has passed since the first human trial with HIV-1 protease inhibitors. Protease inhibitors set the stage for combination therapy in the mid-1990s but are now rarely used in first-line combination therapy and reserved for salvage ...
Arts Eric J
doaj   +1 more source

Inhibition of a viral enzyme by a small-molecule dimer disruptor. [PDF]

, 2009
We identified small-molecule dimer disruptors that inhibit an essential dimeric protease of human Kaposi's sarcoma-associated herpesvirus (KSHV) by screening an alpha-helical mimetic library.
Arnold, Leggy A, Craik, Charles S, Guy, R Kiplin, Lazic, Ana, Lee, Gregory M, Roels, Christina M, Shahian, Tina, Velusamy, Priya   +7 more
core  

The purification and characterisation of novel dipeptidyl peptidase IV-like activity from bovine serum [PDF]

, 2004
The discovery of a potentially novel proline-specific peptidase from bovine serum is presented which is capable of cleaving the dipeptidyl peptidase IV (DPIV) substrate Gly-Pro-MCA.
Abbott, Birney, Cunningham, De Meester, De Meester, Duke-Cohan, Duke-Cohan, Duke-Cohan, Durinx, Gilmartin, Hegen, Hopsu-Havu, Huang, Iwaki-Egawa, Kin, Laemmli, Malik, Mentlein, Mentlein, Ohkubo, Ohnishi, Pineiro-Sanchez, Scanlan, Schon, Sedo, Sedo, Shibuya-Saruta, Smith, Stockel-Maschek, Underwood, Yaron, Yoshimoto   +31 more
core   +1 more source

MET variants with activating N‐lobe mutations identified in hereditary papillary renal cell carcinomas still require ligand stimulation

Molecular Oncology, EarlyView.
MET variants in the N‐lobe of the kinase domain, found in hereditary papillary renal cell carcinoma, require ligand stimulation to promote cell transformation, in contrast to other RTK variants. This suggests that HGF expression in the microenvironment is important for tumor growth in such patients. Their sensitivity to MET inhibitors opens the way for
Célia Guérin, Audrey Vinchent, Marie Fernandes, Isabelle Damour, Agathe Laratte, Rémi Tellier, Gabriella O. Estevam, Jean‐Pascal Meneboo, Céline Villenet, Clotilde Descarpentries, James S. Fraser, Martin Figeac, Alexis B. Cortot, Etienne Rouleau, David Tulasne   +14 more
wiley   +1 more source

TOMM20 as a driver of cancer aggressiveness via oxidative phosphorylation, maintenance of a reduced state, and resistance to apoptosis

Molecular Oncology, EarlyView.
TOMM20 increases cancer aggressiveness by maintaining a reduced state with increased NADH and NADPH levels, oxidative phosphorylation (OXPHOS), and apoptosis resistance while reducing reactive oxygen species (ROS) levels. Conversely, CRISPR‐Cas9 knockdown of TOMM20 alters these cancer‐aggressive traits.
Ranakul Islam, Megan E. Roche, Zhao Lin, Diana Whitaker‐Menezes, Victor Diaz‐Barros, Eurico Serrano, Maria Paula Martinez Cantarin, Nancy J. Philp, Atrayee Basu Mallick, Ubaldo Martinez‐Outschoorn   +9 more
wiley   +1 more source

Juggling jobs: roles and mechanisms of multifunctional protease inhibitors in plants.

New Phytologist, 2016
Multifunctional protease inhibitors juggle jobs by targeting different enzymes and thereby often controlling more than one biological process. Here, we discuss the biological functions, mechanisms and evolution of three types of multifunctional protease ...
F. Grosse-Holz, R. V. D. van der Hoorn
semanticscholar   +1 more source

Feline coronavirus drug inhibits the main protease of SARS-CoV-2 and blocks virus replication

Nature Communications, 2020
The main protease, Mpro (or 3CLpro) in SARS-CoV-2 is a viable drug target because of its essential role in the cleavage of the virus polypeptide. Feline infectious peritonitis, a fatal coronavirus infection in cats, was successfully treated previously ...
Wayne Vuong, Muhammad Bashir Khan, Conrad Fischer, E. Arutyunova, Tess Lamer, Justin A Shields, H. Saffran, R. McKay, M. J. van Belkum, M. Joyce, H. Young, D. Tyrrell, J. Vederas, M. J. Lemieux   +13 more
semanticscholar   +1 more source