Toward Imaging of the GABA Transporter Type 1 In Vivo: Quantitative Evaluation of 4 Novel PET Radiotracers in Nonhuman Primates.

The main inhibitory neurotransmitter in the central nervous system is γ-aminobutyric acid (GABA). GABA transporter type 1 (GAT-1) is the principal GABA transporter in the brain, and it plays a crucial role in modulating GABA signaling. Its potential role in several neuropsychiatric disorders makes it an important target to study.

Discovery of -(6-Methoxypyridin-3-yl)quinoline-2-amine Derivatives for Imaging Aggregated α-Synuclein in Parkinson's Disease with Positron Emission Tomography.

The fibrillary aggregation of α-synuclein is a hallmark of Parkinson's disease (PD) and a potential target for diagnostics and therapeutics. Although substantial effort has been devoted to the development of positron emission tomography (PET) probes for detecting α-synuclein aggregates, no clinically suitable tracer has been reported. The design and synthesis of 43 new -(6-methoxypyridin-3-yl)quinolin-2-amine derivatives and an evaluation of their α-synuclein binding affinity is reported here.

Case Report: Patient-specific three-dimensional printing and computational fluid dynamics in the planning of transcatheter aortic valve replacement for quadricuspid aortic valve.

Background: Performing transcatheter aortic valve replacement (TAVR) in patients with high-risk quadricuspid aortic valve (QAV) may be feasible, but uncertainties remain regarding the development of a comprehensive procedural plan and predicting the outcomes.

Case Summary: We report a case of a 70-year-old patient with a high-risk (EuroSCORE II: 11.2%) QAV (type B) and severe aortic regurgitation (regurgitant jet area measuring 9.

Assessment of test-retest reproducibility by [F]Bavarostat for PET imaging of HDAC6.

Background: Histone deacetylase 6 (HDAC6) is an enzyme pivotal for gene regulation, influencing cellular pathways through protein deacetylation. HDAC6 is a potential therapeutic target in diseases such as cancer and neurodegenerative disorders. Koole et al.

MiR-133b-3p attenuates angiotensin II-induced cardiac hypertrophy through the inhibition of apoptosis by targeting .

MicroRNAs (miRNAs) have emerged as essential regulators that play important roles in the development of multiple systems. Recent studies have identified significant roles for miRNAs in the progression of cardiac hypertrophy. This study aims to investigate the effects of miR-133b-3p on angiotensin II (Ang II)-induced cardiac hypertrophy and apoptosis, as well as explore its underlying mechanisms.

PET Imaging of Sphingosine-1-Phosphate Receptor 1 with [F]TZ4877 in Nonhuman Primates.

Purpose: The sphingosine-1-phosphate receptor-1 (S1PR) is involved in regulating responses to neuroimmune stimuli. There is a need for S1PR-specific radioligands with clinically suitable brain pharmcokinetic properties to complement existing radiotracers. This work evaluated a promising S1PR radiotracer, [F]TZ4877, in nonhuman primates.

Exploration of (R)-[C]YH168 as a PET tracer for imaging monoacylglycerol lipase in the brain: from mice to non-human primates.

Purpose: The monoacylglycerol lipase (MAGL) plays a pivotal role in modulating the endocannabinoid system and is considered an attractive therapeutic target for diseases in both the central nervous system and periphery. The current study aimed to develop and evaluate a suitable carbon-11 labeled tracer for imaging MAGL in preclinical studies.

Methods: (R)-YH168 was synthesized via a multi-step pathway and its half-maximal inhibitory concentration (IC) values were measured using an enzymatic assay.

PET Imaging of Sphingosine-1-Phosphate Receptor 1 with [18F]TZ4877 in Nonhuman Primates.

Purpose: The sphingosine-1-phosphate receptor-1 (S1PR) is involved in regulating responses to neuroimmune stimuli. There is a need for S1PR-specific radioligands with clinically suitable brain pharmcokinetic properties to complement existing radiotracers. This work evaluated a promising S1PR radiotracer, [F]TZ4877, in nonhuman primates.

Composite diffuse large B-cell lymphoma and peripheral T-cell lymphoma: a case report with two-year follow-up and literature review.

Composite lymphoma is an uncommon type of lymphoid malignancy, and those consisting of concurrent diffuse large B-cell lymphoma (DLBCL) and peripheral T-cell lymphoma, not otherwise specified (PTCL-NOS) in the same organ are rare. Here, we report a case of a 75-year-old male patient admitted to our emergency department with intestinal obstruction presenting with abdominal pain and vomiting. He underwent partial resection of the small intestine under general anesthesia, and subsequent histopathology confirmed the mass to be composite DLBCL and PTCL-NOS.

Bortezomib-based chemotherapy for patients with Waldenström macroglobulinemia: a single-center experience.

Waldenström Macroglobulinemia (WM) is a rare type of non-Hodgkin lymphoma with no standard first-line treatment, and the disease is still incurable. This study evaluated the clinical efficacy, safety, and prognostic factors of bortezomib-based chemotherapy as initial treatment in WM patients. We retrospectively analyzed the clinical data collected from 44 newly diagnosed WM patients treated with bortezomib-based regimens at the Affiliated Hospital of Nantong University from December 2011 to June 2021.

CtBP proteins transactivate matrix metalloproteinases and proinflammatory cytokines to mediate the pathogenesis of abdominal aortic aneurysm.

Abdominal aortic aneurysm (AAA) is a life-threatening disorder that occurs in the aorta. The inflammatory thickness of the aneurysm wall and perianeurysmal fibrosis are two main causes of AAA pathogenesis; however, the molecular mechanisms involved in these two processes are still unclear. We discovered that C-terminal binding protein 1 (CtBP1) and CtBP2 were overexpressed in the aortas of AAA-model mice created by treatment with CaCl and elastase.

Efficient delivery of the Bcl-2 antisense oligonucleotide G3139 via nucleus-targeted aCD33-NKSN nanoparticles.

G3139 is an antisense oligodeoxyribonucleotide (ODN) developed as a Bcl-2 down-regulating agent for the treatment of acute myelogenous leukemia (AML). However, the clinical efficacy of G3139 has been shown to be limited due to its rapid plasma clearance and low permeability. To enhance the effective delivery of G3139, this work prepared a novel nano gene delivery vector (aCD33-NKSN) consisting of a CD33 antigbody (aCD33), a nuclear localization signal (NLS), gene fusion peptides (KALA), and stearic acid (SA) for CD33 antigen targeting and nuclear localization.

Radiosynthesis and characterization of a carbon-11 PET tracer for receptor-interacting protein kinase 1.

Introduction: Receptor-interacting protein kinase 1 (RIPK1) has emerged as a crucial regulator of necroptosis and the inflammatory response by activating a group of downstream immune receptors. It has been recognized as a pivotal contributor to cell death and inflammation in various physiological and pathological processes. RIPK1 deficiency or dysregulation in humans can cause severe immunodeficiency and neurodegenerative diseases such as multiple sclerosis and amyotrophic lateral sclerosis.

Radiosynthesis and evaluation of a fluorine-18 radiotracer [F]FS1P1 for imaging sphingosine-1-phosphate receptor 1.

Assessment of sphingosine-1-phosphate receptor 1 (S1PR1) expression could be a unique tool to determine the neuroinflammatory status for central nervous system (CNS) disorders. Our preclinical results indicate that PET imaging with [C]CS1P1 radiotracer can quantitatively measure S1PR1 expression changes in different animal models of inflammatory diseases. Here we developed a multiple step F-18 labeling strategy to synthesize the radiotracer [F]FS1P1, sharing the same structure with [C]CS1P1.

PET Study of Sphingosine-1-phosphate Receptor 1 Expression in Response to Infection.

Sphingosine-1-phosphate receptor 1 (S1PR1) plays a crucial role in infectious diseases. Targeting S1PR1 provides protection against pathogens, such as influenza viruses. This study is aimed at investigating S1PR1 in response to bacterial infection by assessing S1PR1 expression in -infected mice.