Sfoglia per Soggetto "drug targeting"
Items 1-12 di 12
-
The architecture of hydrogen and sulfur σ-hole interactions explain differences in the inhibitory potency of C-β-D-glucopyranosyl thiazoles, imidazoles and an N-β-D glucopyranosyl tetrazole for human liver glycogen phosphorylase and offer new insights to structure-based design
(2020)C-Glucopyranosyl imidazoles, thiazoles, and an N-glucopyranosyl tetrazole were assessed in vitro and ex vivo for their inhibitory efficiency against isoforms of glycogen phosphorylase (GP; a validated pharmacological target ... -
Conformational properties of HIV-1 gp120/V3 immunogenic domains
(2005)Infection of target host cells by the human immunodeficiency virus-1 (HIV-1) is a multi-step process involving a series of conformational changes in the viral gp120 and gp41 proteins. Gp120 binding to the main cell receptor, ... -
Differential contributions of serotonergic and dopaminergic functional connectivity to the phenomenology of LSD
(2022)Rationale: LSD is the prototypical psychedelic. Despite a clear central role of the 5HT2a receptor in its mechanism of action, the contributions of additional receptors for which it shows affinity and agonist activity ... -
Discovery of Small-Molecule Inhibitors of Receptor Activator of Nuclear Factor-κB Ligand with a Superior Therapeutic Index
(2020)Receptor activator of nuclear factor-κB ligand (RANKL) constitutes the master mediator of osteoclastogenesis, while its pharmaceutical inhibition by a monoclonal antibody has been approved for the treatment of postmenopausal ... -
Functional characterization and anti-cancer action of the clinical phase II cardiac Na+/K+ ATPase inhibitor istaroxime: In vitro and in vivo properties and cross talk with the membrane androgen receptor
(2016)Sodium potassium pump (Na+/K+ ATPase) is a validated pharmacological target for the treatment of various cardiac conditions. Recent published data with Na+/K+ ATPase inhibitors suggest a potent anti-cancer action of these ... -
MYCing and YAPing the escape of tumor cell growth arrest after chronic PI3K/mTOR inhibition
(2017)[No abstract available] -
PD-1 and PD-L1 as immunotherapy targets and biomarkers in non-small cell lung cancer
(2019)The integration of immunotherapeutic agents in the treatment of non-small cell lung cancer (NSCLC) has revolutionized the approach of the prevalent type of lung cancer. Although PD-1 and its ligands (PD-L1 and PD-L2) are ... -
RNase P: A promising molecular target for the development of new drugs
(2004)RNase P is an ubiquitous and essential endonuclease in tRNA biogenesis, which generates the mature 5′-termini of tRNAs. RNase P activities have been identified in all three kingdoms of life (Bacteria, Archaea, Eukarya). ... -
Silencing of caveolin-1 in fibroblasts as opposed to epithelial tumor cells results in increased tumor growth rate and chemoresistance in a human pancreatic cancer model
(2019)Caveolin-1 (Cav-1) expression has been shown to be associated with tumor growth and resistance to chemotherapy in pancreatic cancer. The primary aim of this study was to explore the significance of Cav-1 expression in ... -
Systemic sclerosis: From pathogenesis towards targeted immunotherapies
(2012)Systemic sclerosis (SSc), a chronic disease with widespread collagen deposition, has three pathogenetic facets: immune activation, microvasculopathy and fibroblast activation. Immune activation and microvasculopathy occur ... -
Toward fully exploiting the therapeutic potential of marketed pharmaceuticals: The use of octreotide and chloroquine in oncology
(2019)Pleiotropy in biological systems and their targeting allows many pharmaceuticals to be used for multiple therapeutic purposes. Fully exploiting the therapeutic properties of drugs that are already marketed would be highly ...