Results 51 to 60 of about 11,632,967 (345)

Cell wall target fragment discovery using a low‐cost, minimal fragment library

FEBS Letters, EarlyView.
LoCoFrag100 is a fragment library made up of 100 different compounds. Similarity between the fragments is minimized and 10 different fragments are mixed into a single cocktail, which is soaked to protein crystals. These crystals are analysed by X‐ray crystallography, revealing the binding modes of the bound fragment ligands.
Kaizhou Yan, Mathew Stanley, Olawale Raimi, Andrew T. Ferenbach, Helge C Dorfmueller, Daan M. F. van Aalten   +5 more
wiley   +1 more source

Theoretical Analysis of Drug Dissolution: I. Solubility and Intrinsic Dissolution Rate [PDF]

Journal of Pharmaceutical Sciences, 2016
The first-principles approach presented in this work combines surface kinetics and convective diffusion modeling applied to compounds with pH-dependent solubility and in different dissolution media. This analysis is based on experimental data available for approximately 100 compounds of pharmaceutical interest.
Boris, Shekunov, Eda Ross, Montgomery
openaire   +2 more sources

PARP inhibitors elicit distinct transcriptional programs in homologous recombination competent castration‐resistant prostate cancer

Molecular Oncology, EarlyView.
PARP inhibitors are used to treat a small subset of prostate cancer patients. These studies reveal that PARP1 activity and expression are different between European American and African American prostate cancer tissue samples. Additionally, different PARP inhibitors cause unique and overlapping transcriptional changes, notably, p53 pathway upregulation.
Moriah L. Cunningham, Jasibel Vasquez‐Gonzalez, Samantha M. Barnada, Salome Tchotorlishvili, Latese Jones, Ryan Maguire, Genevieve Lewis, Kinza Rizwan, Jenny Deng, Salma Koachar, Drithi Patel, Hailey Shankle, Tessa Mulders, Namra Ajmal, Charalambos Solomides, Emad S. Alnemri, Teresa F. Alnemri, Ayesha A. Shafi, Leonard G. Gomella, Wm Kevin Kelly, Steven B. McMahon, Matthew J. Schiewer   +21 more
wiley   +1 more source

Measurement of the pure dissolution rate constant of a mineral in water

, 2008
We present here a methodology, using holographic interferometry, enabling to measure the pure surface reaction rate constant of the dissolution of a mineral in water, unambiguously free from the influence of mass transport.
Colombani, Jean
core   +2 more sources

Silodosin oral films: Development, physico-mechanical properties and in vitro dissolution studies in simulated saliva [PDF]

, 2019
Sublingual film dosage forms for drugs used for fast symptomatic treatment have promise because they allow a rapid onset of action. The aim of this study was to prepare films of silodosin intended for sublingual administration for the symptomatic ...
Adair, Alhayali, Allam, Alonzo, Boateng, Brady, Brouwers, Campisi, Chapple, Curatolo, De Caro, El-Setouhy, ElMeshad, Gao, Garsuch, Gittings, Guo, Hanif, Hobbs, Huang, Humphrey, Jug, Kalia, Kapoor, Kim, Koland, Korhonen, Li, Liew, Madhav, Mashru, Matsubara, Miller-Chou, Montorsi, Nagy, Patel, Prabhu, Prasad, Preis, Preis, Preis, Radebaugh, Repka, Rossi, Runja, Sharma, Singh, Singh, Singh, Singh, Slavkova, Tanno, Vila, Visser, Vuddanda, Vuddanda, Yang, Zhang   +57 more
core   +2 more sources

PYCR1 inhibition in bone marrow stromal cells enhances bortezomib sensitivity in multiple myeloma cells by altering their metabolism

Molecular Oncology, EarlyView.
This study investigated how PYCR1 inhibition in bone marrow stromal cells (BMSCs) indirectly affects multiple myeloma (MM) cell metabolism and viability. Culturing MM cells in conditioned medium from PYCR1‐silenced BMSCs impaired oxidative phosphorylation and increased sensitivity to bortezomib.
Inge Oudaert, Lauren van den Broecke, Osman Aksoy, Judith Lind, Sonia Vallet, Arne Van der Vreken, Gamze Ates, Ann Massie, Ken Maes, Kim De Veirman, Elke De Bruyne, Karin Vanderkerken, Klaus Podar, Eline Menu   +13 more
wiley   +1 more source

A synthetic benzoxazine dimer derivative targets c‐Myc to inhibit colorectal cancer progression

Molecular Oncology, EarlyView.
Benzoxazine dimer derivatives bind to the bHLH‐LZ region of c‐Myc, disrupting c‐Myc/MAX complexes, which are evaluated from SAR analysis. This increases ubiquitination and reduces cellular c‐Myc. Impairing DNA repair mechanisms is shown through proteomic analysis.
Nicharat Sriratanasak, Bodee Nutho, Worawat Wattanathana, Narumon Phaonakrop, Bunnatut Panasawatwong, Katharina Erlenbach‐Wuensch, Sittiruk Roytrakul, Regine Schneider‐Stock, Pithi Chanvorachote   +8 more
wiley   +1 more source

Enhancement of Dissolution Rate of Olmesartan Medoxomil Using Urea as Carrier by Different Solid Dispersion Techniques [PDF]

, 2018
The poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T fluid often leads to insufficient bioavailability. As per Biopharmaceutical Classification System (BCS), Olmesartan belongs to the class-II category having ...
Gomathi, M. (M), Sangameswaran, B. (B)
core  

Predictors of response and rational combinations for the novel MCL‐1 inhibitor MIK665 in acute myeloid leukemia

Molecular Oncology, EarlyView.
This study characterizes the responses of primary acute myeloid leukemia (AML) patient samples to the MCL‐1 inhibitor MIK665. The results revealed that monocytic differentiation is associated with MIK665 sensitivity. Conversely, elevated ABCB1 expression is a potential biomarker of resistance to the treatment, which can be overcome by the combination ...
Joseph Saad, Rhiannon Newman, Elmira Khabusheva, Sofia Aakko, Eric Durand, Mahesh Tambe, Heikki Kuusanmäki, Alun Parsons, Juho J. Miettinen, Komal Kumar Javarappa, Ezgi June Olgac, Nemo Ikonen, Mika Kontro, Kimmo Porkka, Heiko Maacke, Janghee Woo, Ensar Halilovic, Caroline A. Heckman   +17 more
wiley   +1 more source

Dissolution of CaO in SiO₂-CaO-Al₂O₃ Slag in Si Production

Metals
This work investigates the dissolution of CaO into three different compositions of SiO2-CaO-Al2O3 slag similar to those found in industrial Si furnaces. It was found that CaO dissolution into the slag is fast.
Marit Buhaug Folstad, Kristian Etienne Einarsrud, Merete Tangstad   +2 more
doaj   +1 more source