Results 31 to 40 of about 754,901 (303)

Teaching an Old Dog New Tricks: Strategies That Improve Early Recognition in Similarity-Based Virtual Screening

Frontiers in Chemistry, 2019
High throughput screening (HTS) is an important component of lead discovery, with virtual screening playing an increasingly important role. Both methods typically suffer from lack of sensitivity and specificity against their true biological targets. With
Ruifeng Liu, Ruifeng Liu, Mohamed Diwan M. AbdulHameed, Mohamed Diwan M. AbdulHameed, Anders Wallqvist   +4 more
doaj   +1 more source

A Bidirectional Permeability Assay for beyond Rule of 5 Compounds

Pharmaceutics, 2021
Bidirectional permeability measurement with cellular models grown on Transwell inserts is widely used in pharmaceutical research since it not only provides information about the passive permeability of a drug, but also about transport proteins involved ...
Yunhai Cui, Cyril Desevaux, Ines Truebenbach, Peter Sieger, Klaus Klinder, Alan Long, Achim Sauer   +6 more
doaj   +1 more source

Spirotetronate Polyketides as Leads in Drug Discovery [PDF]

Journal of Natural Products, 2014
The discovery of chlorothricin (1) defined a new family of microbial metabolites with potent antitumor antibiotic properties collectively referred to as spirotetronate polyketides. These microbial metabolites are structurally distinguished by the presence of a spirotetronate motif embedded within a macrocyclic core.
Lacoske, Michelle H., Theodorakis, Emmanuel A.   +1 more
openaire   +2 more sources

Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform

, 2022
S.346-361According to the World Health Organization, more than 1 billion people are at risk of or are affected by neglected tropical diseases. Examples of such diseases include trypanosomiasis, which causes sleeping sickness; leishmaniasis; and Chagas ...
Alunda, J.M., Uliassi, E., Dello Lacono, L., Venturelli, A., Pisa, F. di, Bertolacini, C.P., Ellinper, B., Kebede, B., Gul, S., Behrens, B., Costi, M.P., Fenske, M., Mangani, S., Muller, W., Santucci, M., Calogeropoulou, T., Corral, M.J., Freitas, L.H., Wrigley, S., Prousis, K.C., Quotadamo, A., Pozzi, C., Keminer, O., Borsari, C., Clos, J., Landi, G., Wade, R.C., Ferrari, S., Leu, J., Reinshagen, J., Kuzikov, M., Witt, G., Wolf, M., Pohner, I., Linciano, P., Karunakaran, D., Pascoalino, B.D., Santarem, N., Panecka-Hofman, J., Bolognesi, M.L., Cordeiro-da-Silva, A., Moraes, C.B.   +41 more
core   +1 more source

Integrated dataset of screening hits against multiple neglected disease pathogens. [PDF]

, 2011
New chemical entities are desperately needed that overcome the limitations of existing drugs for neglected diseases. Screening a diverse library of 10,000 drug-like compounds against 7 neglected disease pathogens resulted in an integrated dataset of 744 ...
Clive Yeates, Mansour Nuha R., Ridley, Robert, Simon Townson, Nwaka, S, Dominique Besson, Yeates, Clive, Townson, Simon, Yeates Clive, Jean-Marc Paris, Geary Timothy, Murthy P. K., Ramirez, Bernadette, Maes, Louis, Ramirez Bernadette, Besson, D, Yousif, F, Yousif Fouad, Samje, M, Solomon Nwaka, Van Voorhis Wesley C., Ramirez, B, Misra-Bhattacharya, S, Samje, Moses, An Matheeussen, Ridley, R, Murthy, PK, Suzanne Gokool, Cho-Ngwa Fidelis, Bickle, Q, P K Murthy, Timothy Geary, Bickle Quentin, Gokool, Suzanne, Bernadette Ramirez, Fidelis Cho-Ngwa, Geary, Timothy, Paris, Jean-Marc, Geary, T, Maes, L, Paris Jean-Marc, Quentin Bickle, Fakorede, Foluke, Shailja Misra-Bhattacharya, Samje Moses, Moses Samje, Van Voorhis, WC, Bickle, Quentin, Matheeussen, A, Besson, Dominique, Fouad Yousif, Gokool Suzanne, Louis Maes, Van Voorhis, Wesley C, Townson, S, Fakorede, F, Yousif, Fouad, Cho-Ngwa, F, Nwaka, Solomon, Maes Louis, Townson Simon, Nwaka Solomon, Wesley C Van Voorhis, Misra-Bhattacharya, Shailja, Ridley Robert, Cho-Ngwa, Fidelis, Robert Ridley, Matheeussen An, Fakorede Foluke, Besson Dominique, Mansour, NR, Matheeussen, An, Paris, JM, Foluke Fakorede, Nuha R Mansour, Mansour, Nuha R, Yeates, C, Gokool, S, Misra-Bhattacharya Shailja   +78 more
core   +1 more source

Tumor cell‐specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase

EMBO Molecular Medicine, 2014
Deregulated expression of MYC is a driver of colorectal carcinogenesis, necessitating novel strategies to inhibit MYC function. The ubiquitin ligase HUWE1 (HECTH9, ARF‐BP1, MULE) associates with both MYC and the MYC‐associated protein MIZ1.
Stefanie Peter, Jennyfer Bultinck, Kevin Myant, Laura A Jaenicke, Susanne Walz, Judith Müller, Michael Gmachl, Matthias Treu, Guido Boehmelt, Carsten P Ade, Werner Schmitz, Armin Wiegering, Christoph Otto, Nikita Popov, Owen Sansom, Norbert Kraut, Martin Eilers   +16 more
doaj   +1 more source

Space medicine: gut microbiome of hardy species is a potential source to counter disorders during space travel

Future Science OA, 2023
Tweetable abstract It is proposed that gut microbiome of species like cockroaches may offer a potential source of novel mechanisms/molecules that can be translated into humans to safeguard astronauts against stressors of the space environment during deep
Ruqaiyyah Siddiqui, Adel B Elmoselhi, Naveed Ahmed Khan   +2 more
doaj   +1 more source

Clinical and Biological Features of Response in Resistant Neuroblastoma to 131I‐Metaiodobenzylguanidine Radiotherapy in the Anti‐GD2 Immunotherapy Era

Pediatric Blood &Cancer, EarlyView.
ABSTRACT Background 131I‐metaiodobenzylguanidine (131I‐MIBG) radiotherapy is a key treatment for relapsed and refractory (R/R) neuroblastoma (NB). Patients with R/R disease treated in the modern era are increasingly exposed to anti‐GD2 immunotherapy, which exerts selective pressure and may modify both tumor cell state and microenvironment.
Benjamin J. Lerman, Katherine K. Matthay, Fabienne Hollinger, Catriona Black, Ann A. Lazar, Miguel Pampaloni, Steven G. DuBois, Kieuhoa T. Vo   +7 more
wiley   +1 more source

Evaluating Triazole-Substituted Pyrrolopyrimidines as CSF1R Inhibitors

Molecules
6-Aryl-7H-pyrrolo[2,3-d]pyrimidin-4-amines have promising properties as colony-stimulating factor 1 receptor (CSF1R) inhibitors. Inspired by these antagonists, two series of 1,2,3-triazole analogues (28 compounds) were synthesized and evaluated as CSF1R ...
Srinivasulu Cherukupalli, Jan Eickhoff, Carsten Degenhart, Peter Habenberger, Anke Unger, Bård Helge Hoff, Eirik Sundby   +6 more
doaj   +1 more source

Hospitalization Through Families’ Eyes: Comparing Inpatient Care Quality for Children With Sickle Cell Disease and Cystic Fibrosis in Canada

Pediatric Blood &Cancer, EarlyView.
ABSTRACT Background Sickle cell disease (SCD) is a chronic, inherited hemoglobinopathy that requires frequent hospitalization for disease‐related complications. Canadian data on inpatient care is limited. This study compared caregiver‐reported hospital experiences of children with SCD to those with cystic fibrosis (CF), a chronic, autosomal recessive ...
Hailey M. Zwicker, Kyle Kemp, Perri Tutelman, Sharon H. J. Hou, Paul Fairie, Maria Santana, Gregory M. T. Guilcher, Taryn Fay‐McClymont, Glenda Bendiak, Wendy Pelletier, Nicola Wright, Fiona Schulte   +11 more
wiley   +1 more source