Peter Johnström
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View article: PET imaging of mitochondrial complex-I in the adenine-induced tubulointerstitial nephropathy mouse model using [18F]BCPP-BF
PET imaging of mitochondrial complex-I in the adenine-induced tubulointerstitial nephropathy mouse model using [18F]BCPP-BF Open
Background Chronic kidney disease (CKD) poses a significant global health burden with limited effective treatments for its prevention, progression, and associated complications. Mitochondrial dysfunction is recognized as a pivotal factor i…
View article: AZ14289671 is a highly selective and blood-brain barrier penetrant irreversible TKI that targets EGFRExon20 insertions
AZ14289671 is a highly selective and blood-brain barrier penetrant irreversible TKI that targets EGFRExon20 insertions Open
Current clinical therapeutics against non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion (EGFRExon20Ins) mutations yield limited responses particularly against brain metastases; therefore, the…
View article: Radiolabeling and Preliminary In Vivo Evaluation of the Candidate CCR2 Targeting PET Radioligand [11C]AZD2423
Radiolabeling and Preliminary In Vivo Evaluation of the Candidate CCR2 Targeting PET Radioligand [11C]AZD2423 Open
Background: AZD2423 is a high-affinity and selective negative allosteric modulator of the chemokine receptor type 2 (CCR2). This receptor plays important roles in the extravasation and transmigration of monocytes under inflammatory conditi…
View article: Radiosynthesis and Evaluation of 11C-Labeled Isoindolone-Based Positive Allosteric Modulators for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor 2
Radiosynthesis and Evaluation of 11C-Labeled Isoindolone-Based Positive Allosteric Modulators for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor 2 Open
The metabotropic glutamate receptor 2 (mGluR2) has emerged as a potential therapeutic target for the treatment of various neurological diseases, prompting substantial interest in the development of mGluR2-targeted drug candidates. As part …
View article: Data from Preclinical Characterization of AZD9574, a Blood–Brain Barrier Penetrant Inhibitor of PARP1
Data from Preclinical Characterization of AZD9574, a Blood–Brain Barrier Penetrant Inhibitor of PARP1 Open
Purpose:We evaluated the properties and activity of AZD9574, a blood–brain barrier (BBB) penetrant selective inhibitor of PARP1, and assessed its efficacy and safety alone and in combination with temozolomide (TMZ) in preclinical models.Ex…
View article: Supplementary Data 1 from Preclinical Characterization of AZD9574, a Blood–Brain Barrier Penetrant Inhibitor of PARP1
Supplementary Data 1 from Preclinical Characterization of AZD9574, a Blood–Brain Barrier Penetrant Inhibitor of PARP1 Open
Supplementary methods, figures, tables
View article: Supplementary Data 1 from Preclinical Characterization of AZD9574, a Blood–Brain Barrier Penetrant Inhibitor of PARP1
Supplementary Data 1 from Preclinical Characterization of AZD9574, a Blood–Brain Barrier Penetrant Inhibitor of PARP1 Open
Supplementary methods, figures, tables
View article: Data from Preclinical Characterization of AZD9574, a Blood–Brain Barrier Penetrant Inhibitor of PARP1
Data from Preclinical Characterization of AZD9574, a Blood–Brain Barrier Penetrant Inhibitor of PARP1 Open
Purpose:We evaluated the properties and activity of AZD9574, a blood–brain barrier (BBB) penetrant selective inhibitor of PARP1, and assessed its efficacy and safety alone and in combination with temozolomide (TMZ) in preclinical models.Ex…
View article: Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood–Brain Barrier: The Discovery of AZD1390
Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood–Brain Barrier: The Discovery of AZD1390 Open
The inhibition of ataxia-telangiectasia mutated (ATM) has been shown to chemo- and radio-sensitize human glioma cells in vitro and therefore might provide an exciting new paradigm in the treatment of glioblastoma multiforme (GBM). The effe…
View article: P014 First-time-in-human visualisation of CCR9 expression in the gut by positron emission tomography
P014 First-time-in-human visualisation of CCR9 expression in the gut by positron emission tomography Open
Background CCR9/CCL25 is the key axis for recruiting lymphocytes to the small intestine and represents a potential treatment target in Crohn’s disease (CD). AZD7798 is a first-in-class monoclonal antibody for CD that depletes CCR9+ lymphoc…
View article: Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRAS<sup>G12C</sup> with Demonstrable CNS Penetration
Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRAS<sup>G12C</sup> with Demonstrable CNS Penetration Open
The glycine to cysteine mutation at codon 12 of Kirsten rat sarcoma (KRAS) represents an Achilles heel that has now rendered this important GTPase druggable. Herein, we report our structure-based drug design approach that led to the identi…
View article: Supplementary Data from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs
Supplementary Data from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs Open
Supplementary Data
View article: Figure S1 from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs
Figure S1 from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs Open
Supplementary Figure S1 - Structure and position of label for compounds assessed for BBB penetrance in non human primates (NHP). Majority of compounds were labelled with carbon-11 except afatinib which was labelled with fluorine-18. (*) In…
View article: Supplementary Data from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs
Supplementary Data from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs Open
Supplementary Data
View article: Figure S1 from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs
Figure S1 from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs Open
Supplementary Figure S1 - Structure and position of label for compounds assessed for BBB penetrance in non human primates (NHP). Majority of compounds were labelled with carbon-11 except afatinib which was labelled with fluorine-18. (*) In…
Data from Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity Open
Purpose: Approximately one-third of patients with non–small cell lung cancer (NSCLC) harboring tumors with EGFR-tyrosine kinase inhibitor (TKI)-sensitizing mutations (EGFRm) experience disease progression during treatment due to brain meta…
Supplementary Methods, Supplementary References, Supplementary Tables 1-2, Supplementary Figures 1-3 from Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity Open
Supplementary Table S1. Osimertinib, rociletinib, and afatinib permeability across Caco2 cell Monolayers; Supplementary Table S2. Strain information; Supplementary Figure S1. Structures of osimertinib (6), its plasma metabolites AZ5104 and…
View article: Data from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs
Data from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs Open
Purpose:Osimertinib is a potent and selective EGFR tyrosine kinase inhibitor (EGFR-TKI) of both sensitizing and T790M resistance mutations. To treat metastatic brain disease, blood–brain barrier (BBB) permeability is considered desirable f…
Supplementary Methods, Supplementary References, Supplementary Tables 1-2, Supplementary Figures 1-3 from Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity Open
Supplementary Table S1. Osimertinib, rociletinib, and afatinib permeability across Caco2 cell Monolayers; Supplementary Table S2. Strain information; Supplementary Figure S1. Structures of osimertinib (6), its plasma metabolites AZ5104 and…
Data from Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity Open
Purpose: Approximately one-third of patients with non–small cell lung cancer (NSCLC) harboring tumors with EGFR-tyrosine kinase inhibitor (TKI)-sensitizing mutations (EGFRm) experience disease progression during treatment due to brain meta…
View article: Data from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs
Data from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs Open
Purpose:Osimertinib is a potent and selective EGFR tyrosine kinase inhibitor (EGFR-TKI) of both sensitizing and T790M resistance mutations. To treat metastatic brain disease, blood–brain barrier (BBB) permeability is considered desirable f…
View article: Brain exposure of osimertinib in patients with epidermal growth factor receptor mutation non‐small cell lung cancer and brain metastases: A positron emission tomography and magnetic resonance imaging study
Brain exposure of osimertinib in patients with epidermal growth factor receptor mutation non‐small cell lung cancer and brain metastases: A positron emission tomography and magnetic resonance imaging study Open
Brain metastases (BMs) are associated with poor prognosis in epidermal growth factor receptor mutation‐positive (EGFRm) non‐small cell lung cancer (NSCLC). Osimertinib is a third‐generation, irreversible, EGFR‐tyrosine kinase inhibitor tha…
View article: Proof of lung muscarinic receptor occupancy by tiotropium: Translational Positron Emission Tomography studies in non-human primates and humans
Proof of lung muscarinic receptor occupancy by tiotropium: Translational Positron Emission Tomography studies in non-human primates and humans Open
Introduction Molecular imaging has not been used to support the development of drugs for the treatment of pulmonary disorders. The aim of the present translational study was to advance quantitative pulmonary PET imaging by demonstrating oc…
View article: Lung muscarinic receptor occupancy by tiotropium: translational Positron Emission Tomography studies in non-human primates and humans
Lung muscarinic receptor occupancy by tiotropium: translational Positron Emission Tomography studies in non-human primates and humans Open
Purpose Molecular imaging has not been used to support the development of drugs for the treatment of pulmonary disorders. The aim of the present translational study was to advance quantitative pulmonary PET imaging by demonstrating occupan…
View article: Lung muscarinic receptor occupancy by tiotropium: translational PET studies in non-human primates and humans
Lung muscarinic receptor occupancy by tiotropium: translational PET studies in non-human primates and humans Open
Background The aim of the present translational PET study was to estimate occupancy of tiotropium at muscarinic acetylcholine receptors (mAChR) in the lungs in vivo . The relationship between the tiotropium exposure and receptor occupancy …
Glia Imaging Differentiates Multiple System Atrophy from Parkinson's Disease: A Positron Emission Tomography Study with [<span><sup>11</sup>C</span>]<span>PBR28</span> and Machine Learning Analysis Open
Background The clinical diagnosis of multiple system atrophy (MSA) is challenged by overlapping features with Parkinson's disease (PD) and late‐onset ataxias. Additional biomarkers are needed to confirm MSA and to advance the understanding…
Brain exposure of the ATM inhibitor AZD1390 in humans—a positron emission tomography study Open
Background The protein kinase ataxia telangiectasia mutated (ATM) mediates cellular response to DNA damage induced by radiation. ATM inhibition decreases DNA damage repair in tumor cells and affects tumor growth. AZD1390 is a novel, highly…
Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs Open
Purpose: Osimertinib is a potent and selective EGFR tyrosine kinase inhibitor (EGFR-TKI) of both sensitizing and T790M resistance mutations. To treat metastatic brain disease, blood–brain barrier (BBB) permeability is considered desirable …
Effects of sevoflurane anaesthesia on radioligand binding to monoamine oxidase-B in vivo Open
Sevoflurane anaesthesia inhibited radioligand binding to MAO-B in the primate brain. The observation of lower MAO-B binding at clinically relevant concentrations of sevoflurane warrants further exploration of the potential role of MAO-B re…