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Biology subjects

Lewis, J. S.

Publications and source records attributed to Lewis, J. S..

At least 19 recordsLinked to original sources

Structural basis of the nucleotide incorporation cycle of bacterial DNA polymerase III

Bacterial DNA polymerase III (PolIII) is the primary replicative polymerase responsible for faithful genome duplication, yet high-resolution structural snapshots of the enzyme during DNA synthesis and proofreading have remained elusive. Here we determine cryo-EM structures of the Escherichia coli PolIII core-clamp-DNA binary, ternary and proofreading complexes at 2.4-2.7 [A] resolution, revealing the structural basis of nucleotide selection, incorporation and proofreading. Binding of an incoming nucleotide expels the single-stranded template overhang from the polymerase central channel and induces a large rotation of the polymerase index finger, which closes around the incoming nucleotide to form a compact nascent base-pair-binding pocket. A conserved tyrosine on the finger stacks against the incoming nucleotide to impose stringent steric constraints that promote nucleotide selection, whereas a conserved histidine acts as a steric gate to exclude ribonucleotides. The proofreading structures capture key intermediates that reveal how PolIII transfers a mismatched primer terminus to the 3'-5' exonuclease active site and excises the misincorporated nucleotide while avoiding unnecessary degradation of correctly paired DNA. Together, these findings define the molecular mechanism by which the bacterial replicative polymerase couples rapid and processive DNA synthesis with exceptional replication fidelity.

biochemistry↗

Direct visualisation of post-replication gap formation at the bacterial RRS

Replication risk sequences (RRS) are recently discovered genomic structural elements that trigger post-replication gap formation during replisome passage. In E. coli, the two RRS elements are nearly perfect 222-bp G-quadruplex-containing repeats that flank the terminal domain and are highly conserved in both sequence and genomic position across enterobacteria. We report here the first direct visualisation of RRS function in vitro using single-molecule methods. When the G4 strand of the RRS element is positioned on the lagging-strand template, gaps are formed essentially every time a replisome encounters it. An increase in ssDNA in the synthesised DNA is readily seen using ssGAP-seq methods. When the G-quadruplex strand of the RRS is positioned on the leading-strand template, gaps are formed, albeit at lower frequency. However, the continued DNA synthesis in a rolling-circle assay indicates that the gaps are still formed on the lagging strand, indicating that the RRS complementary strand has a significant but reduced capacity to form a structure that triggers lesion skipping. The results document the potency of the RRS as a trigger for gap formation, suggesting a possible function for at least some eukaryotic G-quadruplexes.

biophysics↗

Structure of the Pre-Initiation Complex Explains CMGE Biogenesis

Summary paragraphWhen cells enter S phase, bidirectional DNA replication is initiated through the kinase-regulated recruitment of three activators (Cdc45, GINS and Pol epsilon) to a duplex DNA-loaded double hexamer of MCM ATPases. Together these proteins form two CMGE helicases that establish divergent replication forks as they become separated1. To understand CMGE biogenesis, we reconstituted the pre-Initiation Complex with purified yeast proteins. The cryo-EM structure shows a set of firing factors caught in the act of assembling two symmetric CMGEs. We show how stepwise complex formation reshapes MCM in preparation for DNA opening and we explain how ATP promotes firing-factor ejection and CMGE maturation. While we find that Sld2 promotes GINS recruitment to MCM as expected, it also aids efficient separation of the CMGE dimer, and it is essential for lagging strand ejection from MCM. These findings have direct implications for our understanding of the metazoan Sld2 ortholog, RECQL4, pointing to a replication-fork establishment mechanism conserved across eukaryotes.

biochemistry↗

Exploring the Neural Correlates of Body Perception Disturbance with a Visual Hand Morph Illusion in Complex Regional Pain Syndrome: An fMRI study

Complex regional pain syndrome (CRPS) is a debilitating chronic pain condition whose causal mechanisms remain poorly understood. Individuals with CRPS often experience distorted perceptions of their affected limb in terms of size and shape, accompanied by feelings of dislike and disownership-- collectively referred to as body perception disturbances (BPD). Evidence that both BPD and pain can rapidly reduce following a visual hand morph illusion suggests modulation of central body representations. To elucidate the neural correlates underlying these rapid perceptual changes, we investigated brain activity during the hand morph illusion using functional magnetic resonance imaging (fMRI). Forty-four participants (22 with upper limb CRPS, 22 pain-free controls) completed the hand morph illusion task during fMRI and provided trial-by-trial ratings of ownership, likeability, and pain of their affected hand. People with CRPS showed greater activation of the left premotor cortex (PMC) during the illusion compared with controls. Functional connectivity between the left PMC and right extrastriate body area (EBA) was also revealed in CRPS during the illusion. No main effects of the illusion, relative to a sham condition, were found on pain intensity, limb ownership, or likeability ratings. These findings provide the first identification of neural correlates of body perception disturbance in CRPS, implicating PMC-EBA networks in altered body representation. Further neuroimaging research is required to define the neural signature underlying this disturbance.

neuroscience↗

Anillin-dependent actin assembly at PML NBs protects genome stability

Nuclear filamentous actin (F-actin) is emerging as a key regulator of genome stability1-6. During replication stress, transient bursts of nuclear actin assembly in S-phase promote fork remodelling and repair3,4, but how these bursts are initiated, regulated, and whether nuclear F-actin also act on DNA lesions inherited across cell cycles, remains unknown. Here, we show that replication stress induces nuclear actin assembly at liquid-liquid phase-separated (LLPS) promyelocytic leukaemia nuclear bodies (PML NBs), driven by the actin-binding protein Anillin. Although best known as a cytokinesis factor, Anillin localises to PML NBs in interphase, where it concentrates monomeric actin (G-actin) and establishes a favourable environment for spontaneous actin assembly. Filament growth within these condensates remodels PML NB morphology and composition, releasing sequestered AKT into the nucleoplasm. AKT is subsequently phosphorylated and activated, and this nuclear AKT activity is required to regulate 53BP1 nuclear bodies in G1. These protective LLPS compartments shield under-replicated DNA inherited from the stressed S-phase until the following S-phase. This prevents premature engagement by aberrant repair pathways that would otherwise generate toxic intermediates and culminate in mitotic failure. Together, these findings define a condensate-to-filament pathway in which nuclear F-actin dynamically reorganises phase-separated compartments to safeguard genome stability across cell cycles.

cell biology↗

Single-cell, Spatially-Resolved TCR Profiling Links T Cell Phenotype and Clonality in Human Tumors

Despite remarkable success in melanoma and other cancers, immune checkpoint blockade has shown limited efficacy in head and neck squamous cell carcinoma (HNSCC), with durable responses in only [~]10% of patients. This is paradoxical given the abundant infiltration of CD8 T cells in HNSCC, suggesting that current T cell profiling methods fail to fully capture functional anti-tumor immunity and that key immunosuppressive mechanisms remain poorly understood. To uncover mechanisms regulating T cell function in situ, we developed a multimodal profiling framework integrating high-dimensional flow cytometry, single-cell RNA- and TCR-sequencing, and spatial transcriptomics, including spatially-resolved TCR profiling at single-cell resolution. Applying this approach to paired blood and tumor samples from 27 HNSCC patients enabled single-cell resolution mapping of T cell clonality, transcriptional state, and spatial localization within intact tumors. Tumors with similar clinical features and immune profiles by flow cytometry and scRNA-seq exhibited markedly different spatial immune architectures. Within the T cell compartment, stem- and memory-like T cells localized within immune-rich niches, while exhausted cells were broadly dispersed in tumor-rich regions. Targeted spatial TCR mapping revealed that tumor-enriched TCR clones were distributed throughout the tumor yet adopted distinct, location-dependent phenotypes, indicating that both antigen specificity and spatial cues shape T cell differentiation and function in human tumors. These findings reveal fundamental principles of T cell organization in solid tumors and establish a versatile platform for spatially-resolved, antigen-specific T cell profiling.

immunology↗

Generalizing animal movement predictions across landscapes: a scalable framework grounded in empirical telemetry data

BackgroundUnderstanding animal movement across broad ecological contexts is essential for guiding management decisions in natural resource and animal disease management. However, most movement studies collect data over small spatial extents, which challenges using the data for landscape-scale management applications. MethodsWe collated relocation data from 564 wild pigs spanning 25 studies across 10 states in the United States. We derived net and daily displacement distributions for individuals in each of 4 seasons. We fit gamma distributions to displacement distributions and derived mean and dispersion parameters as metrics of displacement magnitude and variation. We modeled mean and dispersion variables using gradient-boosted regression, including landscape and weather predictors, and predicted daily and net displacement distributions across the species range. We used integrated step selection analysis to estimate habitat selection for wild pig groups sharing a common composition of habitat availability across the studied populations. ResultsFemale average ({+/-} 95% confidence interval) net displacement means varied by season, peaking in Jul-Sept at 1,152 {+/-} 140 m along with daily displacement mean distances of 650 {+/-} 41 m. Average net displacement means for males peaked in Oct.-Dec. at 1,651 {+/-} 160 m with daily displacement mean distances of 1,092 {+/-} 95 m. Extreme net displacement values ranged up to 9,649 m and 4,080 m for male and female, respectively, and extreme daily displacement distribution means of 6,616 m for males, and 3,855 m for females. Almost half of the individuals included a similar composition of habitat availability, regardless of study site location. Herbaceous wetland was the most consistently favored land type and was available for more than 70% of all individual pigs across all studies. Preference for other land types depended strongly on habitat availability. ConclusionsBy comparing movement and habitat selection across a large geographic extent, our work provides new insights about the environmental drivers and limits of wild pig movement behavior. Our workflow digests variation wild pig movement distributions and habitat selection into parameters that can be used to predict movement on heterogeneous landscapes for downstream applications such as invasive species elimination campaigns or disease management.

ecology↗

Targeted Alpha Therapy with Ac-Macropa-Isatuximab for CD38-positive Hematological Malignancies

BackgroundHematological malignancies include diverse cancers related to immune system cells and blood-forming tissue. Treatment resistance and relapse are common despite the introduction of novel therapeutics. Following the development of the PET probe [89Zr]Zr-DFO-isatuximab, targeting the overexpressed CD38 receptor, we developed [225Ac]Ac-Macropa-isatuximab for targeted alpha therapy in murine models of human multiple myeloma (MM) and lymphoma. MethodsIn vitro studies were performed using the CD38 expressing MM1.S (human MM) and Daudi (human lymphoma). Radiopharmaceutical therapy studies were performed in female NSG mice, and the disseminated disease models were established by intravenous injection of luciferase-transfected cells. Mice were randomized (n = 10 mice per cohort) and received a high activity (5.5 kBq) or low activity (2.7 kBq) of [225Ac]Ac-Macropa-Isatuximab in single or multiple cycles. Controls receiving untargeted [225Ac]Ac-Macropa-IgG or saline were included. Tumor burden was measured by bioluminescence imaging (BLI). Weight loss greater than 20% or leg paralysis were used as endpoints. Results[225Ac]Ac-Macropa-Isatuximab was obtained with high radiochemical yield and purity (>95%). It displayed high immunoreactivity and excellent stability in human serum over 10 days. The therapeutic effect of [225Ac]Ac-mcp-Isatuximab was significant for all the treatment cohorts compared to the saline control after administration of the first cycle. Low activities were better tolerated in general, resulting in extended median survivals. The most successful regimen in the MM model was the dual cycle of low activity, with a median survival of 60 days (P < 0.001). In the lymphoma model, the single high activity of 5.5 kBq and four low activity of 2.7 kBq resulted in similar median survivals of 143 days (P < 0.0001) and 147 days (P < 0.0001). These regimens resulted in complete responses with no detectable cancer cells in some cases. Remarkably, no significant kidney damage was observed in any of the models. Conclusion[225Ac]Ac-Macropa-Isatuximab selectively targets CD38, reducing tumor growth and, in some cases, tumor eradication, especially when applied in multiple cycles. Importantly, it has not been associated with significant toxicities at levels of administered activity required for therapeutic benefit, indicating its promise as a therapeutic option.

pharmacology and toxicology↗

Exploring the PET in vivo generator 134Ce as a theranostic match for 225Ac

PurposeThe radionuclide pair cerium-134/lanthanum-134 (134Ce/134La) was recently proposed as a suitable diagnostic counterpart for the therapeutic alpha-emitter actinium-225 (225Ac). The unique properties of 134Ce offer perspectives for developing innovative in vivo investigations not possible with 225Ac. In this work, 225Ac- and 134Ce-labeled tracers were directly compared using internalizing and slow-internalizing cancer models to evaluate their in vivo comparability, progeny meandering, and potential as a matched theranostic pair for clinical translation. Despite being an excellent chemical match, 134Ce/134La has limitations to the setting of quantitative positron emission tomography imaging. MethodsThe precursor PSMA-617 and a macropa-based tetrazine-conjugate (mcp-PEG8-Tz) were radiolabelled with 225Ac or 134Ce and compared in vitro and in vivo using standard (radio)chemical methods. Employing biodistribution studies and positron emission tomography (PET) imaging in athymic nude mice, the radiolabelled PSMA-617 tracers were evaluated in a PC3/PIP (PC3 engineered to express a high level of prostate-specific membrane antigen) prostate cancer mouse model. The 225Ac and 134Ce-labeled mcp-PEG8-Tz were investigated in a BxPC-3 pancreatic tumour model harnessing the pretargeting strategy based on a trans-cyclooctene-modified 5B1 monoclonal antibody. ResultsIn vitro and in vivo studies with both 225Ac and 134Ce-labelled tracers led to comparable results, confirming the matching pharmacokinetics of this theranostic pair. However, PET imaging of the 134Ce-labelled precursors indicated that quantification is highly dependent on tracer internalization due to the redistribution of 134Ces PET-compatible daughter 134La. Consequently, radiotracers based on internalizing vectors like PSMA-617 are suited for this theranostic pair, while slow-internalizing 225Ac-labelled tracers are not quantitatively represented by 134Ce PET imaging. ConclusionWhen employing slow-internalizing vectors, 134Ce might not be an ideal match for 225Ac due to the underestimation of tumour uptake caused by the in vivo redistribution of 134La. However, this same characteristic makes it possible to estimate the redistribution of 225Acs progeny noninvasively. In future studies, this unique PET in vivo generator will further be harnessed to study tracer internalization, trafficking of receptors, and the progression of the tumour microenvironment. TOC Graphic O_FIG O_LINKSMALLFIG WIDTH=200 HEIGHT=167 SRC="FIGDIR/small/591165v1_ufig1.gif" ALT="Figure 1"> View larger version (61K): org.highwire.dtl.DTLVardef@ca3cb6org.highwire.dtl.DTLVardef@157eac6org.highwire.dtl.DTLVardef@f6ac6dorg.highwire.dtl.DTLVardef@b24d87_HPS_FORMAT_FIGEXP M_FIG C_FIG Redistribution of progeny. Investigating the 225Ac and 134Ce decay chain. This figure was created with BioRender.

pharmacology and toxicology↗

Radiances of Cerenkov-Emitting Isotopes on the IVIS

Cerenkov (or Cherenkov) luminescence occurs when charged particles exceed the phase velocity of a given medium. Cerenkov has gained interest in preclinical space as well as in clinical trials for optical visualization of numerous radionuclides. However, Cerenkov intensity has to be inferred from alternative databases with energy emission spectra, or theoretical fluence estimates. Here we present the largest experimental dataset of Cerenkov emitting isotopes recorded using the IVIS optical imaging system. We report Cerenkov measurements spanning orders of magnitude normalized to the activity concentration for 21 Cerenkov emitting isotopes, covering electron, alpha, beta minus, and positron emissions. Isotopes measured include Carbon-11, Fluorine-18, Phosphorous-32, Scandium-47, Copper-64, Copper-67, Gallium-68, Arsenic-72, Bromine-76, Yttrium-86, Zirconium-89, Yttrium-90, Iodine-124, Iodine-131, Cerium-134, Lutetium-177, Lead-203, Lead-212, Radium-223, Actinium-225, and Thorium-227. We hope this updating resource will serve as a rank ordering for comparing isotopes for Cerenkov luminescence in the visible window and serve as a rule of thumb for comparing Cerenkov intensities in vitro and in vivo. MethodsAll Cerenkov emitting radionuclides were either produced at Memorial Sloan Kettering Cancer Center (Carbon-11, 11C; Fluorine-18, 18F; Iodine-124, 124I), from commercial sources such as Perkin Elmer (Phosphorous-32, 32P; Yttrium-90, 90Y), Bayer (Radium-223, 223Ra, Xofigo), 3D-Imaging (Zirconium-89, 89Zr), Nuclear Diagnostic Products (Iodine-131, 131I), or from academic collaborators at Washington University at St. Louis (Copper-64, 64Cu), University of Wisconsin (Bromine-76, 76Br), MD Anderson Cancer Center (Yttrium-86, 86Y), Brookhaven National Laboratory (Arsenic-72, 72As; Thorium-227, 227Th), or Oak Ridge National Laboratory (Cerium-134, 134Ce, Actinium-225, 225Ac), and Viewpoint Molecular Targeting (Lead-203, 203Pb; Lead 212, 212Pb). All isotopes were diluted in triplicate on a black bottomed corning 96 well plate to several activity concentrations ranging from 0.1-250 Ci in 100-200 L of Phosphate Buffered Saline. Cerenkov imaging was acquired on a single Perkin-Elmer Spectrum In-Vivo Imaging System (IVIS) at field of view c with exposures ranging up to 15 minutes or lower provided no part of the image intensity was saturated, or that the activity significantly changed during the exposure. Experimental radiances on the IVIS were calculated from regions of interest drown over each 96 well, and then normalized for the activity present in the well, and the volume the isotope was diluted into.

bioengineering↗

Preclinical shortwave infrared tumor screening and resection via pHLIP ICG under ambient lighting conditions

There is a critical need to improve optical imaging that will lead to its widespread acceptance for routine clinical procedures. Shortwave infrared (SWIR, 900-1700nm) imaging has demonstrated clear advantages over visible and near-infrared imaging (reduced autofluorescence with improved contrast, resolution, and sensitivity at tissue depth). Here we show that the previously reported compound, pH low insertion peptide (pHLIP) conjugated to indocyanine green (ICG, pHLIP ICG) currently in clinical trials, serves as an excellent candidate for SWIR imaging protocols. SWIRs increased sensitivity enabled preclinical tumor screening and resection at exposure times as low as 0.1 ms with acceptable signal-to-noise and contrast-to-noise ratios. Imaging was performed under ambient lighting conditions, and SWIRs sensitivity enabled an extended surgical resection window up to 96 hrs post injection in an orthotopic breast cancer mouse model. This work provides a direct precedent for the clinical translation of SWIR pHLIP ICG imaging for cancer resection. One Sentence SummarySWIR imaging under ambient lighting is highly sensitive to pHLIP ICG, a cancer targeting fluorescent agent currently under clinical investigation.

cancer biology↗

Vomocytosis of Cryptococcus neoformans cells from murine, bone marrow-derived dendritic cells

Cryptococcus neoformans (CN) cells survive within the acidic phagolysosome of macrophages for extended times, then escape without impacting the viability of the host cell via a phenomenon that has been coined vomocytosis. Through this mechanism, CN disseminate throughout the body, sometimes resulting in a potentially fatal condition - Cryptococcal Meningitis (CM). Justifiably, vomocytosis studies have focused primarily on macrophages, as alveolar macrophages within the lung act as first responders that ultimately expel this fungal pathogen. Herein, we hypothesize that dendritic cells (DCs), an innate immune cell with attributes that include phagocytosis and antigen presentation, can also act as vomocytes. Presciently, this report shows that vomocytosis of CN indeed occurs from DCs. Primarily through time-lapse microscopy imaging, we show that rates of vomocytosis events from DCs are comparable to those seen from macrophages and further, are independent of the presence of the CN capsule and infection ratios. Moreover, phagosome-altering drugs such as chloroquine and bafilomycin A, as well as the actin-modifying drug, cytochalasin B inhibit this phenomenon from DCs. Although DC immunophenotype does not affect the total number of vomocytic events, we observed differences in the numbers of CN per phagosome and expulsion times. Interestingly, these observations were similar in primary, murine macrophages. Understanding the vomocytic behavior of different phagocytes and their phenotypic subtypes is needed to help elucidate the full picture of the dynamic interplay between CN and the immune system. Critically, deeper insight into vomocytosis could reveal novel approaches to treat CM, as well as other immune-related conditions.

immunology↗

Caveolin-1 temporal modulation enhances trastuzumab and trastuzumab-drug conjugate efficacy in heterogeneous gastric cancer

Resistance mechanisms and heterogeneity in HER2-positive gastric cancers (GC) limit trastuzumab benefit in 32% of patients, and other targeted therapies have failed in clinical trials. Using genomic data from patient tissue, patient-derived xenografts (PDXs), partially humanized biological models, and HER2-targeted imaging we identified caveolin-1 (CAV1) as a complementary biomarker in GC selection for trastuzumab therapy. In retrospective analyses of samples from patients enrolled on trastuzumab trials, the CAV1-high profile was associated with low membrane HER2 density and reduced patient survival. We found a negative correlation between CAV1 tumoral protein levels - a major protein of cholesterol-rich membrane domains - and trastuzumab-drug conjugate TDM1 tumor uptake. Finally, CAV1 depletion using knockdown or pharmacologic approaches was shown to increase HER2-directed immunoPET uptake and TDM1 efficacy in GC with incomplete HER2 membranous reactivity. In support of these findings, background statin use in patients is associated with enhanced antibody efficacy. Together, this work provides mechanistic justification and clinical evidence that require prospective investigation of HER2-targeted therapies combined with statins to delay drug resistance in GC. SIGNIFICANCEThis study identifies how CAV1 protein expression and statin use relate to GC response in HER2-targeted imaging and therapeutic approaches. In addition, to support the synergy of CAV1 depletion with TDM1 observed in mouse models, we demonstrate that statin users had better clinical responses to antibody-based therapies in HER2+ GC.

cancer biology↗

The E. coli helicase does not use ATP during replication.

The replisome is responsible for replication of DNA in all domains of life, with several of its individual enzyme components relying on hydrolysis of nucleoside triphosphates to provide energy for replisome function. Half a century of biochemical studies have demonstrated a dependence on ATP as an energy source for helicases to unwind duplex DNA during replication. Through single-molecule visualization of DNA replication by the Escherichia coli replisome, we demonstrate that the DnaB helicase does not rely on hydrolysis of ATP (or any ribo-NTPs) in the context of the elongating replisome. We establish that nucleotide incorporation by the leading-strand polymerase is the main motor driving the replication process. One Sentence SummaryPolymerases provide the energy for helicase-mediated DNA unwinding during E. coli DNA replication.

biochemistry↗

DETECTION OF INCIPIENT PANCREATIC CANCER WITH NOVEL TUMOR-SPECIFIC ANTIBODIES IN MOUSE MODELS

Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal malignancy, as 90% of patients do not survive beyond five years from diagnosis. This dismal prognosis is largely due to the advanced stage of the disease at diagnosis, which precludes potentially curative surgical resection. Although early detection strategies hold significant promise for improving patient outcomes, there is still no accurate diagnostic tool to detect incipient PDAC. Here, we sought to develop antibodies for the early detection of PDAC by positron-emission tomography (PET) imaging. Accordingly, we establish a pipeline to generate novel tumor-specific monoclonal antibodies (mAbs) against cell-surface proteins of PDAC patient-derived organoids (PDOs). We identify a panel of 16 tumor organoid-binding antibodies (TOBi-bodies) that display high reactivity to human PDAC tissues but not to matched adjacent normal pancreas. We then employ biochemical, flow cytometric, mass spectrometric, and CRISPR/Cas9-mediated knockout methods to determine the cognate antigens of these TOBi-bodies. We identify two mAbs that bind to tumor-specific variants of the surface protein CEACAM6 and show minimal binding to normal tissues. PET imaging in mouse models using these TOBi-bodies enables the detection of incipient human organoid-derived PDAC tumors that are rather undetectable by palpation or high-resolution ultrasound imaging techniques. We propose that further development of these mAbs as PET radiotracers could facilitate the early detection and accurate staging of PDAC.

cancer biology↗

The structural and functional connectivity neural underpinnings of body image

How we perceive our bodies is fundamental to our self-consciousness and our experience in the world. There are two types interrelated internal body representations--a subjective experience of the position of a limb in space (body schema) and the subjective experience of the shape and size of the limb (body image). Body schema has been extensively studied, but there is no evidence of the brain structure and network dynamics underpinning body image. Here, we provide the first evidence for the extrastriate body area (EBA), a multisensory brain area, as the structural and functional neural substrate for body shape and size. We performed a multisensory finger-stretch illusion that elongated the index finger. EBA volume and functional connectivity to the posterior parietal cortex are both related to the participants susceptibility to the illusion. Taken together, these data suggest that EBA structure and connectivity encode body representation and body perception disturbances.

neuroscience↗

A simple strategy to reduce the salivary gland and kidney uptake of PSMA targeting small molecule radiopharmaceuticals

The past five years have seen an increasing acceptance of peptide-based prostate-specific membrane antigen (PSMA)-targeted radionuclide therapy (TRT) agents for treatment of metastatic castration-resistant prostate cancer (mCRPC), with [177Lu]-DKFZ-PSMA-617 ([177Lu]-PSMA-617) emerging as the leading candidate. [177Lu]-PSMA-617 and other PSMA ligands have shown efficacy in reducing the tumor burden in mCRPC patients but irradiation to salivary gland and kidneys is a concern and dose limiting factor. Therefore, methods to reduce non-target organ toxicity are needed to safely treat patients and preserve their quality of life. Here, we report the effects of the addition of the cold PSMA ligand DKFZ-PSMA-11 (PSMA-11) on the uptake of [177Lu]-PSMA-617 in tumor, salivary glands and kidneys. Groups of athymic nude mice (n = 4) bearing PC3-PIP (PSMA+) tumor xenografts were administered with [177Lu]-PSMA-617 along with 0, 5, 100, 500, 1000 and 2000 pmoles of PSMA-11. Biodistribution studies 1 h post-administration revealed that [177Lu]-PSMA-617 uptake in PSMA-expressing PC3-PIP tumors was 21.71{+/-}6.13, 18.7{+/-}2.03, 26.44{+/-}2.94, 16.21{+/-}3.5, 13.52{+/-}3.68, and 12.03{+/-}1.96 %ID/g when 0, 5, 100, 500, 1000 and 2000 pmoles of PSMA-11 were added, respectively. Corresponding kidney uptake values were 123.14{+/-}52.52, 132.31{+/-}47.4, 84.29{+/-}78.25, 2.12{+/-}1.88, 1.16{+/-}0.36, 0.64{+/-}0.23 %ID/g, respectively. Corresponding salivary gland uptake values were 0.48{+/-}0.11, 0.45{+/-}0.15, 0.38{+/-}0.3, 0.08{+/-}0.03, 0.09{+/-}0.07, 0.05{+/-}0.02 % ID/g, respectively. Thus, uptake of PSMA TRT agents in salivary gland and kidney can be substantially reduced without impact on tumor uptake by adding cold PSMA-11. Our data provides proof-of-concept and we propose that similar strategy be pursued in future clinical trials to prevent xerostomia and renal toxicity arising from [177Lu]-PSMA-617.

pharmacology and toxicology↗

rapidPop: Rapid population assessments of wildlife using camera trap data in R Shiny Applications

O_SCPLOWRAPIDC_SCPLOWPO_SCPLOWOPC_SCPLOW is a new R package for implementing occupancy models for Rapid Population Assessments (RPAs) with data from camera traps. RPAs are designed to provide quick assessments of a density index so that users can identify relative changes in density associated with changes in conditions (Schlichting et al., 2020). For example, users may want to assess if there was a change in density after an effort to cull an invasive species. O_SCPLOWRAPIDC_SCPLOWPO_SCPLOWOPC_SCPLOW provides a Shiny Application for running occupancy models with the option to include the effect of parameters on occupancy (e.g., before or after a culling operation).

ecology↗