Insight into the Development of PET Radiopharmaceuticals for Oncology

J Lau, E Rousseau, D Kwon, KS Lin, F Bénard, X Chen - Cancers, 2020 - mdpi.com
While the development of positron emission tomography (PET) radiopharmaceuticals
closely follows that of traditional drug development, there are several key considerations in …

Up-to-date expert opinion on the safety of recently developed antipsychotics

L Orsolini, D De Berardis, U Volpe - Expert Opinion on Drug Safety, 2020 - Taylor & Francis
Introduction There are several new and emerging antipsychotic medication strategies
recently marketed or under clinical development for the treatment of several mental …

Determining target engagement in living systems

GM Simon, MJ Niphakis, BF Cravatt - Nature chemical biology, 2013 - nature.com
Chemical probes are critical tools for elucidating the biological functions of proteins and can
lead to new medicines for treating disease. The pharmacological validation of protein …

Antipsychotic drug-induced somnolence: incidence, mechanisms, and management

F Fang, H Sun, Z Wang, M Ren, JR Calabrese, K Gao - CNS drugs, 2016 - Springer
Somnolence is a common side effect of antipsychotics. To assess the incidence of this side
effect, we performed a MEDLINE search for randomized, double-blinded, placebo-or active …

Quantifying the interactions between biomolecules: guidelines for assay design and data analysis

PJ Tonge - ACS infectious diseases, 2019 - ACS Publications
The accurate and precise determination of binding interactions plays a central role in fields
such as drug discovery where structure–activity relationships guide the selection and …

Novel agonists of benzodiazepine receptors: design, synthesis, binding assay and pharmacological evaluation of 1, 2, 4-triazolo [1, 5-a] pyrimidinone and 3-amino-1 …

M Faizi, S Dabirian, H Tajali, F Ahmadi… - Bioorganic & medicinal …, 2015 - Elsevier
Agonists of benzodiazepine (BZD) binding site in GABA receptors are widely used in clinical
practice. In spite of their benefits they have several side effects, so synthesis of new agonists …

Is metabotropic glutamate receptor 5 upregulated in prefrontal cortex in fragile X syndrome?

TG Lohith, EK Osterweil, M Fujita, KJ Jenko, MF Bear… - Molecular autism, 2013 - Springer
Abstract Background Fragile X syndrome (FXS) is a common inherited form of intellectual
disability caused by loss of function of the fragile X mental retardation protein. Recent animal …

Chemical tools for studying lipid-binding class AG protein–coupled receptors

A Cooper, S Singh, S Hook, JDA Tyndall… - Pharmacological …, 2017 - Elsevier
Cannabinoid, free fatty acid, lysophosphatidic acid, sphingosine 1-phosphate, prostanoid,
leukotriene, bile acid, and platelet-activating factor receptor families are class AG protein …

Tactics for preclinical validation of receptor-binding radiotracers

SZ Lever, KH Fan, JR Lever - Nuclear medicine and biology, 2017 - Elsevier
Introduction Aspects of radiopharmaceutical development are illustrated through preclinical
studies of [125 I]-(E)-1-(2-(2, 3-dihydrobenzofuran-5-yl) ethyl)-4-(iodoallyl) piperazine ([125 I] …

Molecular imaging of prostate cancer

KM Emonds, JV Swinnen, L Mortelmans, FM Mottaghy - Methods, 2009 - Elsevier
Prostate carcinoma is the most common non-cutaneous malignancy in males. Imaging of
prostatic lesions is of great importance and aids in oncologic management and monitoring of …