Results 21 to 30 of about 307,974 (304)

Computational Approaches in Preclinical Studies on Drug Discovery and Development

Frontiers in Chemistry, 2020
Because undesirable pharmacokinetics and toxicity are significant reasons for the failure of drug development in the costly late stage, it has been widely recognized that drug ADMET properties should be considered as early as possible to reduce failure ...
Fengxu Wu, Fengxu Wu, Yuquan Zhou, Yuquan Zhou, Langhui Li, Langhui Li, Xianhuan Shen, Xianhuan Shen, Ganying Chen, Ganying Chen, Xiaoqing Wang, Xiaoqing Wang, Xianyang Liang, Xianyang Liang, Mengyuan Tan, Mengyuan Tan, Zunnan Huang, Zunnan Huang, Zunnan Huang   +18 more
doaj   +1 more source

T-type Ca2+ Channels: T for Targetable [PDF]

, 2018
In the last decade TTCC have been unveiled as key regulators of cancer cells biology and thus have been proposed as chemotherapeutic targets. Indeed in vitro and in vivo studies indicate that TTCC pharmacological blockers have a negative impact on the ...
Cantí Nicolás, Carles, Crespí Sallán, Marta, Herreros Danés, Judit, Nàger Grifo, Mireia, Shaikh, Soni, Visa Pretel, Anna   +5 more
core   +2 more sources

Assessing Drug-Induced Mitochondrial Toxicity in Cardiomyocytes: Implications for Preclinical Cardiac Safety Evaluation

Pharmaceutics, 2022
Drug-induced cardiotoxicity not only leads to the attrition of drugs during development, but also contributes to the high morbidity and mortality rates of cardiovascular diseases. Comprehensive testing for proarrhythmic risks of drugs has been applied in
Xiaoli Tang, Zengwu Wang, Shengshou Hu, Bingying Zhou   +3 more
doaj   +1 more source

Preclinical Evaluation of Ureidosulfamate Carbonic Anhydrase IX/XII Inhibitors in the Treatment of Cancers [PDF]

, 2019
Carbonic anhydrases (CAs) are a family of enzymes involved in the pH regulation of metabolically active cells/tissues. Upregulation of the CAIX/XII isoforms is associated with hypoxic tumours and clinically linked with malignant progression, treatment ...
Gieling, Roben, Williams, Kaye J.
core   +2 more sources

In vitro bactericidal activities of two novel dihydropyridine derivatives against Mycobacterium tuberculosis

Journal of Infection in Developing Countries, 2017
Introduction: Introducing new and effective antitubercular agents is important in tuberculosis control programs. In this study, the in vitro antitubercular activity of two novel 1,4-dihydropyridine derivatives (F-27, Cl-33) were screened against a total
Mehdi Zandhaghighi, Farzin Hadizadeh, Saman Soleimanpour, Zahra Meshkat, Seyed Abdolrahim Rezaee, Mohammad Derakhshan, Kiarash Ghazvini   +6 more
doaj   +1 more source

Pre-Clinical Tools for Predicting Drug Efficacy in Treatment of Tuberculosis

Microorganisms, 2022
Combination therapy has, to some extent, been successful in limiting the emergence of drug-resistant tuberculosis. Drug combinations achieve this advantage by simultaneously acting on different targets and metabolic pathways.
Hasmik Margaryan, Dimitrios D. Evangelopoulos, Leticia Muraro Wildner, Timothy D. McHugh   +3 more
doaj   +1 more source

Pharmacokinetics, Safety, and Efficacy of Intravitreal Digoxin in Preclinical Models for Retinoblastoma [PDF]

, 2015
PURPOSE:To assess in vitro cytotoxic activity and antiangiogenic effect, ocular and systemic disposition, and toxicity of digoxin in rabbits after intravitreal injection as a potential candidate for retinoblastoma treatment.METHODS:A panel of two ...
Abramson, David, Arana, Eloisa, Buitrago, Emiliano, Chantada, Guillermo Luis, Croxatto, Juan Oscar, del Sole, Maria Jose, Djaballah, Hakim, Francis, Jasmine, Laurent, Viviana Eunice, Mena, Hebe Agustina, Negrotto, Soledad, Schaiquevich, Paula Susana, Sgroi, Mariana, Winter, Ursula Andrea   +13 more
core   +2 more sources

Drug delivery in overcoming the blood-brain barrier: role of nasal mucosal grafting [PDF]

, 2017
The blood–brain barrier (BBB) plays a fundamental role in protecting and maintaining the homeostasis of the brain. For this reason, drug delivery to the brain is much more difficult than that to other compartments of the body. In order to bypass or cross
Carafa, Maria, Di Marzio, Luisa, Hanieh, PATRIZIA NADIA, Marianecci, Carlotta, Paolino, Donatella, Rinaldi, Federica   +5 more
core   +1 more source

Hydrogel-Based Strategies for the Prevention and Treatment of Radiation-Induced Skin Injury: Progress and Mechanistic Insights

Biomimetics
Radiation-induced skin injury (RISI) is one of the most common complications of radiotherapy, severely compromising patients’ quality of life. However, no standardized treatment has yet been established.
Yinhui Wang, Huan Liu, Yushan He, Mei Li, Jie Gao, Zongtai Han, Jiayu Zhou, Jianguo Li   +7 more
doaj   +1 more source

Phase 1 dose escalation study of the allosteric AKT inhibitor BAY 1125976 in advanced solid cancer-Lack of association between activating AKT mutation and AKT inhibition-derived efficacy [PDF]

, 2019
This open-label, phase I first-in-human study (NCT01915576) of BAY 1125976, a highly specific and potent allosteric inhibitor of AKT1/2, aimed to evaluate the safety, pharmacokinetics, and maximum tolerated dose of BAY 1125976 in patients with advanced ...
Boix, Oliver, Hess, Dagmar, Hurvitz, Sara A, Joerger, Markus, Lagkadinou, Eleni, Ma, Cynthia, Moulder, Stacy, Ocker, Matthias, Rentzsch, Christine, Rudolph, Marion, Schneeweiss, Andreas, Thiele, Silke, Tsimberidou, Apostolia M, Varga, Andrea, Wilkinson, Gary   +14 more
core   +3 more sources