Results 41 to 50 of about 805,984 (229)

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

open access: yesActa 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   +6 more
doaj   +1 more source

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

open access: yesPLoS 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

Development of an Albumin-Based PSMA Probe With Prolonged Half-Life

open access: yesFrontiers in Molecular Biosciences, 2020
Prostate-specific membrane antigen (PSMA) is an attractive target for the diagnosis and therapy of prostate cancer as it is specifically overexpressed in prostate cancer cells.
Teli Liu   +9 more
semanticscholar   +1 more source

PolyMorphine provides extended analgesic-like effects in mice with spared nerve injury. [PDF]

open access: yes, 2017
Morphine is a well-characterized and effective analgesic commonly used to provide pain relief to patients suffering from both acute and chronic pain conditions.
Chen, Renxun   +5 more
core   +1 more source

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

open access: yesBiomedicines, 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

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

open access: yesBlood, 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   +12 more
openaire   +1 more source

Review of pyronaridine anti-malarial properties and product characteristics. [PDF]

open access: yes, 2012
Pyronaridine was synthesized in 1970 at the Institute of Chinese Parasitic Disease and has been used in China for over 30 years for the treatment of malaria.
Arbe-Barnes, Sarah J   +7 more
core   +2 more sources

17,β-estradiol inhibits hepatitis C virus mainly by interference with the release phase of its life cycle [PDF]

open access: yes, 2016
Rationale & Aim: Estrogen and estrogen-mediated signalling protect from hepatitis C virus through incompletely understood mechanisms. We aimed to ascertain which phase(s) of HCV life cycle is/are affected by estrogens.
Barbaglia, Matteo N.   +10 more
core   +2 more sources

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

open access: yesMedicina
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   +2 more
doaj   +1 more source

Targeting the CBM complex causes Treg cells to prime tumours for immune checkpoint therapy. [PDF]

open access: yes, 2019
Solid tumours are infiltrated by effector T cells with the potential to control or reject them, as well as by regulatory T (Treg) cells that restrict the function of effector T cells and thereby promote tumour growth1.
Cadilha, Bruno L   +16 more
core   +2 more sources

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