Results 181 to 190 of about 754,901 (303)

Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites. [PDF]

ACS Med Chem Lett, 2017
Devine W, Thomas SM, Erath J, Bachovchin KA, Lee PJ, Leed SE, Rodriguez A, Sciotti RJ, Mensa-Wilmot K, Pollastri MP.   +9 more
europepmc   +1 more source

Transcriptional profiling of circulating extracellular vesicles from prebiopsy prostate cancer patients

Molecular Oncology, EarlyView.
RNA profiling of circulating extracellular vesicles (EVs) from blood samples of men undergoing prostate biopsy identifies transcripts associated with clinically significant prostate cancer. Integrative analysis with public tumor datasets links EV‐derived gene signatures to tumor stage and progression‐free survival, highlighting CASP3, XRCC2, and RIT1 ...
Stefan Werner, Pierre Tennstedt, Randi C. Pose, Christian Müller, Katharina Besler, Svenja Schneegans, Malik Alawi, Marie C. Roesch, Sven Peine, Desiree Bonci, Joanna Budna‐Tukan, Evi Lianidou, Catherine Alix‐Panabières, Derya Tilki, Klaus Pantel   +14 more
wiley   +1 more source

Differential <i>ex vivo</i> susceptibility of <i>Plasmodium malariae</i> and <i>Plasmodium falciparum</i> clinical isolates from Ghana and Mali to current and lead discovery candidate antimalarial drugs. [PDF]

Microbiol Spectr
Soulama A, Sogore F, Ansah F, Diakite O, Chirawurah JD, Maiga FO, Maiga M, Danwonno HA, Campo B, Djimde AA, Awandare GA, Amenga-Etego LN, Dembele L, Aniweh Y.   +13 more
europepmc   +1 more source

An Automated Microscale Thermophoresis Screening Approach for Fragment-Based Lead Discovery. [PDF]

J Biomol Screen, 2016
Linke P, Amaning K, Maschberger M, Vallee F, Steier V, Baaske P, Duhr S, Breitsprecher D, Rak A.   +8 more
europepmc   +1 more source

Interaction of HS1BP3 with cortactin modulates TKS5 localisation, cell secretion and cancer malignancy

Molecular Oncology, EarlyView.
Here, we demonstrate that HS1BP3 interacts with Cortactin through a proline‐rich region (PRR3.1) and show that this interaction, and HS1BP3 itself, promote cancer cell proliferation and invasion. Inhibition of this interaction leads to build‐up of TKS5 in multivesicular endosomes and altered secretion of CD63 and CD9, providing an explanation for the ...
Arja Arnesen Løchen, Kristiane Søreng, Chiara Veroni, Laura Trachsel‐Moncho, Nagham Asp, Robin Gaupset, Lars Gustav Lyckander, Helene Knævelsrud, Lars Eftang, Anne Simonsen   +9 more
wiley   +1 more source

Mass Spectrometry Instrumentation for Therapeutic Lead Discovery

Mass Spectrometry Instrumentation for Therapeutic Lead Discovery. Drug discovery is reliant on the application of basic research and advanced technologies to obtain solutions to human suffering caused by diseases.

core  

Successes and challenges in phenotype-based lead discovery for prion diseases. [PDF]

J Med Chem, 2014
Ghaemmaghami S, Russo M, Renslo AR.
europepmc   +1 more source

Interpreting the effects of DNA polymerase variants at the structural level

Molecular Oncology, EarlyView.
Using MAVISp and molecular dynamics simulations, we analyzed over 60 000 missense variants in POLE and POLD1 from ClinVar, COSMIC, cBioPortal, and saturation mutagenesis. Identified mechanistic indicators, including stability, binding, and long‐range, enable structural interpretation, providing ACMG‐like evidence for possible reclassification of VUS ...
Matteo Arnaudi, Karolina Krzesińska, Ludovica Beltrame, Pablo Sánchez‐Izquierdo Besora, Matteo Tiberti, Mef Nilbert, Anna Rohlin, Elena Papaleo   +7 more
wiley   +1 more source

NMR-based platform for fragment-based lead discovery used in screening BRD4-targeted compounds. [PDF]

Acta Pharmacol Sin, 2016
Yu JL, Chen TT, Zhou C, Lian FL, Tang XL, Wen Y, Shen JK, Xu YC, Xiong B, Zhang NX.   +9 more
europepmc   +1 more source

Metastasis on pause: How dormant tumor cells stay hidden within the tumor microenvironment and evade immune surveillance

Molecular Oncology, EarlyView.
Dormant cancer cells can hide in distant organs for years, evading treatment and the immune system. This review highlights how signals from the surrounding tissue and immune environment keep these cells inactive or trigger their reawakening. Understanding these mechanisms may help develop therapies to eliminate or control dormant cells and prevent ...
Kanishka Tiwary, Jose Javier Bravo‐Cordero   +1 more
wiley   +1 more source