Results 21 to 30 of about 460,394 (253)

In vitro and in vivo pharmacokinetic characterization of LMT-28 as a novel small molecular interleukin-6 inhibitor [PDF]

Asian-Australasian Journal of Animal Sciences, 2020
Objective Interleukin-6 (IL-6) is a T cell-derived B cell stimulating factor which plays an important role in inflammatory diseases. In this study, the pharmacokinetic properties of LMT-28 including physicochemical property, in vitro liver microsomal ...
Sung-Hoon Ahn, Tae-Hwe Heo, Hyun-Sik Jun, Yongseok Choi   +3 more
doaj   +1 more source

Metabolic Stability of New Mito-Protective Short-Chain Naphthoquinones

Pharmaceuticals, 2020
Short-chain quinones (SCQs) have been identified as potential drug candidates against mitochondrial dysfunction, which is largely dependent on their reversible redox characteristics of the active quinone core. We recently synthesized a SCQ library of >
Zikai Feng, Jason A. Smith, Nuri Gueven, Joselito P. Quirino   +3 more
doaj   +1 more source

A Fast LC-MS/MS Methodology for Estimating Savolitinib in Human Liver Microsomes: Assessment of Metabolic Stability Using In Vitro Metabolic Incubation and In Silico Software Analysis

Separations, 2023
Savolitinib (Orpathys®), was developed by (HUTCHMED (Shanghai, China) and, AstraZeneca (Gaithersburg, Maryland, USA), is an inhibitor of the c-Met receptor tyrosine kinase that is orally bioavailable.
Mohamed W. Attwa, Haitham AlRabiah, Ali S. Abdelhameed, Adnan A. Kadi   +3 more
doaj   +1 more source

A Rapid and Sensitive UPLC-MS/MS Method for Quantifying Capmatinib in Human Liver Microsomes: Evaluation of Metabolic Stability by In Silico and In Vitro Analysis

Separations, 2023
Capmatinib (CMB) is an orally bioavailable mesenchymal–epithelial transition (MET) inhibitor approved by the US-FDA to treat metastatic non-small cell lung cancer (NSCLC) patients, with MET exon 14 skipping mutation.
Mohamed W. Attwa, Ali S. Abdelhameed, Aishah M. Alsibaee, Adnan A. Kadi   +3 more
doaj   +1 more source

Stabilizing selection and metabolism [PDF]

Heredity, 1988
This paper attempts to provide a biochemical explanation for selection against extreme phenotypes. From current ideas on the analysis of metabolic control, it is argued that, on average, most mutations will reduce flux through metabolic pathways and change substrate pool concentrations in an arbitrary direction.
openaire   +2 more sources

A highly sensitive LC-MS/MS method to determine novel Bruton's tyrosine kinase inhibitor spebrutinib: application to metabolic stability evaluation [PDF]

Royal Society Open Science, 2019
Spebrutinib (SBT) is a Bruton's tyrosine kinase inhibitor. SBT is currently in phase II and phase I clinical trials for the management of rheumatoid arthritis and chronic lymphocytic leukaemia, respectively.
Ali S. Abdelhameed, Mohamed W. Attwa, Nasser S. Al-Shaklia, Adnan A. Kadi   +3 more
doaj   +1 more source

Development of a Fast and Sensitive UPLC–MS/MS Analytical Methodology for Fenebrutinib Estimation in Human Liver Microsomes: In Vitro and In Silico Metabolic Stability Evaluation

Separations, 2023
Fenebrutinib (GDC-0853; FNB) is an oral small molecule that was developed by Roche Pharmaceuticals to slow multiple sclerosis progression. FNB is a reversible bruton tyrosine kinase (BTK) inhibitor, which showed the maximum potency of BTK inhibitors in ...
Mohamed W. Attwa, Aishah M. Alsibaee, Haya I. Aljohar, Ali S. Abdelhameed, Adnan A. Kadi   +4 more
doaj   +1 more source

Pharmaceutical and Safety Profile Evaluation of Novel Selenocompounds with Noteworthy Anticancer Activity

Pharmaceutics, 2022
Prior studies have reported the potent and selective cytotoxic, pro-apoptotic, and chemopreventive activities of a cyclic selenoanhydride and of a series of selenoesters.
Małgorzata Anna Marć, Enrique Domínguez-Álvarez, Gniewomir Latacz, Agata Doroz-Płonka, Carmen Sanmartín, Gabriella Spengler, Jadwiga Handzlik   +6 more
doaj   +1 more source

The Stability of Metabolic Syndrome in Children and Adolescents [PDF]

The Journal of Clinical Endocrinology & Metabolism, 2009
Context: Some studies suggest the presence of metabolic syndrome before adulthood may identify those at high risk for later cardiovascular morbidity, but there are few data examining the reliability of pediatric metabolic syndrome. Objective: To examine the short- and long-term stability of pediatric metabolic syndrome ...
Jennifer K, Gustafson, Lisa B, Yanoff, Benjamin D, Easter, Sheila M, Brady, Margaret F, Keil, Mary D, Roberts, Nancy G, Sebring, Joan C, Han, Susan Z, Yanovski, Van S, Hubbard, Jack A, Yanovski   +10 more
openaire   +2 more sources

MS-BACL: enhancing metabolic stability prediction through bond graph augmentation and contrastive learning. [PDF]

Brief Bioinform
Wang T, Li Z, Zhuo L, Chen Y, Fu X, Zou Q.   +5 more
europepmc   +2 more sources