Results 21 to 30 of about 423,855 (249)

LC–MS/MS Estimation of Rociletinib Levels in Human Liver Microsomes: Application to Metabolic Stability Estimation

Drug Design, Development and Therapy, 2021
Mohamed W Attwa, Ali S Abdelhameed, Adnan A Kadi Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi ArabiaCorrespondence: Ali S Abdelhameed Tel +966 1146 98314Fax +966 1146 76 220Email asaber@ksu.edu ...
Attwa MW, Abdelhameed AS, Kadi AA
doaj  

Antibody-Based In Vivo Imaging of Central Nervous System Targets—Evaluation of a Pretargeting Approach Utilizing a TCO-Conjugated Brain Shuttle Antibody and Radiolabeled Tetrazines

Pharmaceuticals, 2022
Bioorthogonal pretargeted imaging using the inverse-electron-demand Diels–Alder (IEDDA) reaction between a tetrazine (Tz) and a trans-cyclooctene (TCO) represents an attractive strategy for molecular imaging via antibodies.
Christoph Bredack, Martin R. Edelmann, Edilio Borroni, Luca C. Gobbi, Michael Honer   +4 more
doaj   +1 more source

Metabolic stability and its role in the discovery of new chemical entities

Acta Pharmaceutica, 2019
Determination of metabolic profiles of new chemical entities is a key step in the process of drug discovery, since it influences pharmacokinetic characteristics of therapeutic compounds.
Słoczyńska Karolina, Gunia-Krzyżak Agnieszka, Koczurkiewicz Paulina, Wójcik-Pszczoła Katarzyna, Żelaszczyk Dorota, Popiół Justyna, Pękala Elżbieta   +6 more
doaj   +1 more source

Predicting the protein half-life in tissue from its cellular properties. [PDF]

PLoS ONE, 2017
Protein half-life is an important feature of protein homeostasis (proteostasis). The increasing number of in vivo and in vitro studies using high throughput proteomics provide estimates of the protein half-lives in tissues and cells.
Mahbubur Rahman, Rovshan G Sadygov
doaj   +1 more source

Chemical Modification of Cysteine with 3-Arylpropriolonitrile Improves the In Vivo Stability of Albumin-Conjugated Urate Oxidase Therapeutic Protein

Biomedicines, 2021
3-arylpropiolonitriles (APN) are promising alternatives to maleimide for chemo-selective thiol conjugation, because the reaction product has a remarkably hydrolytic stability compared with that of thiol-maleimide reactions in vitro.
Byungseop Yang, Inchan Kwon
doaj   +1 more source

An Ultra-Fast Validated Green UPLC-MS/MS Approach for Assessing Revumenib in Human Liver Microsomes: In Vitro Absorption, Distribution, Metabolism, and Excretion and Metabolic Stability Evaluation

Medicina
Background and Objectives: Revumenib (SNDX-5613) is a powerful and specific inhibitor of the menin–KMT2A binding interaction. It is a small molecule that is currently being researched to treat KMT2A-rearranged (KMT2Ar) acute leukemias.
Mohamed W. Attwa, Ali S. Abdelhameed, Adnan A. Kadi   +2 more
doaj   +1 more source

Thein Vitroprocoagulant Effects of Standard and Extended Half-Life Recombinant Factor IX Concentrates in Patients on Prophylaxis with Emicizumab

Blood, 2020
Introduction: Emicizumab is a humanized, monoclonal, bispecific antibody that binds factor (F) FX and FIXa allowing thrombin generation in the absence of FVIII, which is used for routine treatment of patients with Hemophilia A (HA) with and without inhibitors.
Elena G Arias-Salgado, Ihosvany Fernandez-Bello, Elena Monzón Manzano, Paula Acuña, Sara García Barcenilla, María Teresa Alvarez Román, Mónica Martín, María Isabel Rivas Pollmar, Tamara Cebanu, Elena González Zorrilla, Miguel A Canales, Nora V. Butta, Victor Jimenez-Yuste   +12 more
openaire   +1 more source

Improved Biodistribution and Extended Serum Half-Life of a Bacteriophage Endolysin by Albumin Binding Domain Fusion

Frontiers in Microbiology, 2018
The increasing number of multidrug-resistant bacteria intensifies the need to develop new antimicrobial agents. Endolysins are bacteriophage-derived enzymes that degrade the bacterial cell wall and hold promise as a new class of highly specific and ...
Johan Seijsing, Anna M. Sobieraj, Nadia Keller, Yang Shen, Annelies S. Zinkernagel, Martin J. Loessner, Mathias Schmelcher   +6 more
doaj   +1 more source

Recombinant Peptide Production Platform Coupled with Site-Specific Albumin Conjugation Enables a Convenient Production of Long-Acting Therapeutic Peptide

Pharmaceutics, 2020
The number of therapeutic peptides for human treatment is growing rapidly. However, their development faces two major issues: the poor yield of large peptides from conventional solid-phase synthesis, and the intrinsically short serum half-life of ...
Mijeong Bak, Junyong Park, Kiyoon Min, Jinhwan Cho, Jihyoun Seong, Young S. Hahn, Giyoong Tae, Inchan Kwon   +7 more
doaj   +1 more source

LC-MS/MS Estimation of the Anti-Cancer Agent Tandutinib Levels in Human Liver Microsomes: Metabolic Stability Evaluation Assay

Drug Design, Development and Therapy, 2020
Mohamed W Attwa, Ali S Abdelhameed, Nasser S Al-Shakliah, Adnan A Kadi 1 Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi ArabiaCorrespondence: Ali S AbdelhameedDepartment of Pharmaceutical Chemistry ...
Attwa MW, Abdelhameed AS, Al-Shakliah NS, Kadi AA   +3 more
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