Results 41 to 50 of about 362,059 (246)

A novel quinazolinone insulin receptor inhibitor and its synergy with an EGFR inhibitor in glucose‐driven glioblastoma

Molecular Oncology, EarlyView.
The novel styrylquinazolinone‐based molecule W1B effectively suppresses glioblastoma by inhibiting IGF1R and EGFR. In high‐glucose microenvironments driving tumor resistance, W1B acts synergistically with the EGFR inhibitor dacomitinib. This combination safely blocks compensatory survival signaling in zebrafish xenograft models. Showcasing promising in
Patryk Rurka, Wioleta Cieślik, Wojciech Płaziński, Katarzyna Stępnik, Anna Boguszewska‐Czubara, Elżbieta Kot, Robert Musioł, Mateusz Jasica, Anna Mrozek‐Wilczkiewicz, Katarzyna Malarz   +9 more
wiley   +1 more source

The Role of PK/PD Analysis in the Development and Evaluation of Antimicrobials

Pharmaceutics, 2021
Pharmacokinetic/pharmacodynamic (PK/PD) analysis has proved to be very useful to establish rational dosage regimens of antimicrobial agents in human and veterinary medicine.
Alicia Rodríguez-Gascón, María Ángeles Solinís, Arantxa Isla   +2 more
doaj   +1 more source

Pharmacokinetic Evaluation of a Novel Transdermal Ketoprofen Formulation in Healthy Dogs [PDF]

, 2022
Dogs undergo various surgical procedures such as castration, ovariohysterectomy, and other orthopedic procedures, which are known to cause inflammation and pain. Non-steroidal anti-inflammatory drugs (NSAIDs) are very effective analgesics for alleviating
Kempster, Samantha, Ravuri, Halley Gora, Alexandra Balmanno, Jazmine Skinner, Mills, Paul C., Satake, Nana, Samantha Kempster, Balmanno, Alexandra, Skinner, Jazmine, Halley Gora Ravuri, Nana Satake, Paul C. Mills   +11 more
core   +1 more source

Partial FAK suppression promotes tumor growth, an effect reversed by macrophage p110δ PI3K inactivation

Molecular Oncology, EarlyView.
Partial inhibition of focal adhesion kinase (FAK) can paradoxically promote tumor growth, rather than simply producing a weaker antitumor effect than that observed with strong FAK suppression. In breast cancer and melanoma models, targeting p110δ PI3K, particularly in macrophages, counteracted these tumor‐promoting effects, highlighting the importance ...
Lydia Xenou, Niki Tzenaki, Anna Tsapara, Maria Tzardi, Evangelia A. Papakonstanti   +4 more
wiley   +1 more source

Evaluation of Adefovir PBPK Model to Assess Biomarker‐Informed OAT1 Drug–Drug Interaction and Effect of Chronic Kidney Disease

CPT: Pharmacometrics & Systems Pharmacology
Evaluation of transporter‐mediated drug–drug interactions (DDI) with endogenous biomarkers, coupled with physiologically‐based pharmacokinetic modeling (PBPK) is envisioned to replace or reduce dedicated DDI clinical trials with clinical probe substrates.
Shawn Pei Feng Tan, Huaying Wu, Amin Rostami‐Hodjegan, Daniel Scotcher, Aleksandra Galetin   +4 more
doaj   +1 more source

PBPK Model of Coproporphyrin I: Evaluation of the Impact of SLCO1B1 Genotype, Ethnicity, and Sex on its Inter‐Individual Variability

CPT: Pharmacometrics & Systems Pharmacology, 2021
Coproporphyrin I (CPI) is an endogenous biomarker of OATP1B activity and associated drug‐drug interactions. In this study, a minimal physiologically‐based pharmacokinetic model was developed to investigate the impact of OATP1B1 genotype (c.521T>C ...
Hiroyuki Takita, Shelby Barnett, Yueping Zhang, Karelle Ménochet, Hong Shen, Kayode Ogungbenro, Aleksandra Galetin   +6 more
doaj   +1 more source

UiO‐66 metal–organic frameworks in biomedicine: From structural tunability to bioimaging, photodiagnostics, and photodynamic cancer therapy

FEBS Open Bio, EarlyView.
UiO‐66(Zr) metal–organic frameworks are chemically stable, biocompatible, and highly tunable nanomaterials. Their modular structure enables controlled drug delivery, multimodal bioimaging, and light‐activated photodynamic therapy, supporting integrated diagnostic and therapeutic (theranostic) applications in cancer and biomedical research.
Veronika Huntošová, Grigorii Rakhalskii, Miroslav Almáši   +2 more
wiley   +1 more source

TRPML1 agonist ML‐SA5 attenuates pulmonary fibroblast activation by suppressing mTOR and restoring autophagic flux

FEBS Open Bio, EarlyView.
TGF‐β1 stimulation downregulates lysosomal channel TRPML1 in pulmonary fibroblasts. The TRPML1 agonist ML‐SA5 suppressed fibroblast‐to‐myofibroblast activation and collagen production. Mechanistically, ML‐SA5 inhibited mTOR phosphorylation, restored autophagic flux, and its effects were enhanced by rapamycin (mTOR inhibitor) and reversed by MHY1485 ...
Jiatong Yao, Xiaoting Kang, Lulu Meng, Shaoxuan Zhang, Qiujie Li, Jinyu Zhou, Mengyue Xue, Chu Li, Hua Zhu, Pengzhou Hang, Jing Zhao   +10 more
wiley   +1 more source

Genotype, Ethnicity, and Drug–Drug Interaction Modeling as Means of Verifying Transporter Biomarker PBPK Model: The Coproporphyrin‐I Story

CPT: Pharmacometrics & Systems Pharmacology
Coproporphyrin‐I (CP‐I) is a selective endogenous biomarker of organic anion‐transporting polypeptide (OATP)1B. Multiple CP‐I PBPK models with differing input parameters have been reported so far.
Yuki Ujihira, Shawn Pei Feng Tan, Daniel Scotcher, Aleksandra Galetin   +3 more
doaj   +1 more source

mRNA-Based Nanomedicinal Products to Address Corneal Inflammation by Interleukin-10 Supplementation

Pharmaceutics, 2021
The anti-inflammatory cytokine Interleukin-10 (IL-10) is considered an efficient treatment for corneal inflammation, in spite of its short half-life and poor eye bioavailability. In the present work, mRNA-based nanomedicinal products based on solid lipid
Itziar Gómez-Aguado, Julen Rodríguez-Castejón, Marina Beraza-Millor, Mónica Vicente-Pascual, Alicia Rodríguez-Gascón, Sara Garelli, Luigi Battaglia, Ana del Pozo-Rodríguez, María Ángeles Solinís   +8 more
doaj   +1 more source