Results 31 to 40 of about 30,899 (248)

A novel in vitro serum stability assay for antibody therapeutics incorporating internal standards

mAbs
Antibody-based therapeutics have demonstrated remarkable therapeutic benefit, but their susceptibility to biotransformation and degradation in the body can affect their safety, efficacy, and pharmacokinetic/pharmacodynamic (PK/PD) profiles.
Yihan Li, Rosendo Villafuerte-Vega, Vikram M. Shenoy, Heidi M. Jackson, Yuting Wang, Karen E. Parrish, Gary J. Jenkins, Hetal Sarvaiya   +7 more
doaj   +1 more source

Suggested Improvements for Measurement of Equilibrium Solubility-pH of Ionizable Drugs

ADMET and DMPK, 2015
The accurate prediction of solubility of drug-like molecules is difficult, and perhaps a satisfactory general model is not yet available. The most cited challenge to good prediction has been the lack of enough high-quality and drug-relevant solubility ...
Alex Avdeef
doaj   +1 more source

Chemically Regulated STING‐Activating Prodrugs of Deoxyribose Cyclic Dinucleotides Elicit Robust Immune Activation and Durable Antitumor Immunity

Angewandte Chemie, EarlyView.
All three diastereoisomers of an esterase‐sensitive phosphotriester dCDN prodrug demonstrate improved activity. The (Rp,Rp) diastereoisomer shows the highest activity with an EC50 of 1.7 nM in STING activation and displays the most pronounced antitumor activity via intravenous administration, significantly suppressing tumor proliferation, extending the
Zhiqiang Xie, Huimin Liu, Yuchen Yang, Xiaohan Sun, Jingwen Wang, Tianxiang Liu, Baifan Wang, Wenrui Qiu, Yiwen Sun, Yuting Bai, Yao Zhang, Dejun Ma, Rong Xiang, Shibo Li, Zhen Xi   +14 more
wiley   +2 more sources

In silico exploration for identifying structure-activity relationship of MEK inhibition and oral bioavailability for isothiazole derivatives

, 2010
In this study, quantitative structure–activity ⁄prop-erty models are developed for modeling and pre-dicting both MEK inhibitory activity and oral bioavailability of novel isothiazole-4-carboxami-dines.
Melagraki, G, Fleming, A, Sarimveis, H, Panayiotis A. Koutentis, Igglessi-Markopoulou, O, Georgia Melagraki, Antreas Afantitis, Afantitis, A, Olga Igglessi-Markopoulou, Koutentis, P, George Kollias, Igglessi-markopoulou Panayiotis A, Kollias, G, Koutentis, PA, Haralambos Sarimveis Olga, Haralambos Sarimveis   +15 more
core   +1 more source

G2-manifolds and the ADM formalism [PDF]

Differential Geometry and its Applications, 2019
In this paper we study a Hamiltonian function on the cotangent bundle of the space of Riemannian metrics on a 3-manifold $M$ and prove the orbits of the constrained Hamiltonian dynamical system correspond to $G_2$-manifolds foliated by hypersurfaces diffeomorphic to $M\times \mathrm{SO}(3)$.
openaire   +3 more sources

adm kurikulum

, 2019
Abstrak— the term curriculum administration emphasizes efforts to direct the curriculum so that the curriculum can be implemented appropriately in various educational activities. As is known, the curriculum contains planned activities that will be carried out during the teaching and learning process.
openaire   +5 more sources

Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1-yl)Acetophenone

Journal of the Turkish Chemical Society, Section A: Chemistry, 2023
In this study, the synthesis of chalcone compounds (1-11) derived from 4-(imidazol-1-yl)acetophenone and the structure determination of these compounds by various spectroscopic methods were carried out.
Bedriye Seda KURŞUN AKTAR, Abdulraheem Mustafa ALKARABASH , Ayşe ŞAHİN YAĞLIOĞLU, Emine Elçin ORUÇ-EMRE   +3 more
doaj   +1 more source

ADME profiling.

, 2016
ADME profiling.
Swagatika Dash (472730), Monalisa Ray (2817634), Dattatreya Kar (2817637), Shikha Singh (22657), Tammanna R. Sahrawat (2817631), Sajad Shahbazi (2817628)   +5 more
core   +1 more source

Application of drug-induced growth rate inhibition and intracellular drug exposures for comprehensive evaluation of cellular drug sensitivity

Scientific Reports
In vitro cellular assays are indispensable tools for preclinical understanding of therapeutic candidates. Herein, we have outlined methods for robust determination of cellular sensitivities by adapting drug-induced growth-rate inhibition analysis ...
Dolonchampa Maji, Malerie Wolke, Shamim Khaja, John P. Savaryn, John C. Kalvass, Gary J. Jenkins   +5 more
doaj   +1 more source

Covalent Inhibition of SHMT2 by Gambogic Acid Induces Ferroptosis Through Mitochondrial Collapse in Triple‐Negative Breast Cancer

Advanced Science, EarlyView.
In this study, chemoproteomics combined with genetic and functional analyses was integrated to identify SHMT2 as a covalent and functional target of gambogic acid (GA) in triple‐negative breast cancer (TNBC). Further validation demonstrated that GA selectively modifies the Cys241 site of SHMT2, triggering mitochondrial dysfunction, activating the Nrf2 ...
Tong Yang, Chong Qiu, Yulei Li, Ying Zhang, Chen Wang, Jie Zhou, Zheng Chu, Ang Ma, Ling Huang, Yin Kwan Wong, Junzhe Zhang, Peng Gao, Cui Liu, Junhua Zhang, Huan Tang, Jigang Wang   +15 more
wiley   +1 more source