Vandana V. Gupta

Neuro-inflammatory Biomarkers

Jyoti Pandey, Vandana V. Gupta

This narrative review explores Parkinson's disease (PD), a progressive neurodegenerative condition that significantly affects motor function and is associated with significant neuroinflammatory processes. Activated microglia and astrocytes, along with the release of inflammatory mediators, trigger neuroinflammation, a crucial factor in the onset …

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Parallel Paths, Uneven Progress: Health Care Provider and Patient Perspectives on Anti‐Amyloid Therapies for Early AD

Vandana V. Gupta, Carole Drexel, Nathaniel A. Chin, Scott Kaiser et autres

BACKGROUND: The management landscape for Alzheimer Disease (AD) is changing with the recent regulatory approvals of two anti- amyloid targeted agents for early AD in the United States, and additional agents are in the pipeline. We sought to characterize the current level …

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Discovery of a Chiral 2,4-Substituted Pyrrolo[2,3-d]pyrimidine as a Potent, Selective, and Orally Bioavailable LRRK2 Inhibitor

Omar Moukha‐Chafiq, Tuyana Malankhanova, Jacob Valiyaveettil, Vandana V. Gupta et autres

Inhibition of leucine-rich repeat kinase (LRRK2) activity with small molecules has emerged as a potential novel therapeutic target for Parkinson’s disease (PD). We have previously reported the identification of SRI-29132 as a potent LRRK2 inhibitor, but the presence of a 6-thioether moiety, …

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Novel Compound Inhibitors of HIV-1NL4-3 Vpu

Carolyn Robinson, Terri D. Lyddon, Hwi Min Gil, David T. Evans et autres

HIV-1 Vpu targets the host cell proteins CD4 and BST-2/Tetherin for degradation, ultimately resulting in enhanced virus spread and host immune evasion. The discovery and characterization of small molecules that antagonize Vpu would further elucidate the contribution of Vpu to pathogenesis and …

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Novel compound inhibitors of HIV-1 NL4-3 Vpu

Carolyn Robinson, Terri D. Lyddon, Hwi Min Gil, David T. Evans et autres

ABSTRACT HIV-1 Vpu targets the host cell proteins CD4 and BST-2/Tetherin for degradation, ultimately resulting in enhanced virus spread and host immune evasion. The discovery and characterization of small molecules that antagonize Vpu would further elucidate the contribution of Vpu to pathogenesis …

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Identification of Inhibitors of Thrombospondin 1 Activation of TGF-β

Mark J. Suto, Vandana V. Gupta, Bini Mathew, Wei Zhang et autres

TGF-β has been a target of interest for the treatment of fibrotic diseases and certain cancers. Approaches to target TGF-β include antagonists of the active ligand or TGF-β receptor kinase activity. These approaches have failed in clinical trials due to a lack …

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Discovery of a novel inhibitor of kinesin-like protein KIFC1

Wei Zhang, Ling Zhai, Yimin Wang, Rebecca J. Boohaker et autres

Historically, drugs used in the treatment of cancers also tend to cause damage to healthy cells while affecting cancer cells. Therefore, the identification of novel agents that act specifically against cancer cells remains a high priority in the search for new therapies. …

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Abstract 1746: Discovery and evaluation of a small molecule KIFC1 inhibitor for breast cancer treatment

Wei Zhang, Ling Zhai, Wenyan Lü, Yimin Wang et autres

Abstract Historically, drugs used in the treatment of certain cancers may cause damage to healthy cells while affecting cancer cells. Therefore, finding compounds that are specific toward cancer cells only is still a high priority in the search for new therapies. In …

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Unique Functional and Structural Properties of the LRRK2 Protein ATP-binding Pocket

Zhiyong Liu, Robert A. Galemmo, Kyle Fraser, Mark S. Moehle et autres

Pathogenic mutations in the LRRK2 gene can cause late-onset Parkinson disease. The most common mutation, G2019S, resides in the kinase domain and enhances activity. LRRK2 possesses the unique property of cis-autophosphorylation of its own GTPase domain. Because high-resolution structures of the human …

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Abstract P1-04-05: Subpopulation heterogeneity demonstrated in circulating tumor cells isolated from breast cancer patients using ApoStream™, an antibody-independent cancer cell recovery device

K. Anderes, VO Melnikova, Vandana V. Gupta, DK Hasegawa et autres

Abstract Background: Current established methods of circulating tumor cell (CTC) isolation and identification rely on antibodies against epithelial specific markers such as epithelial cell adhesion molecule (EpCAM) and cytokeratin (CK). The classical phenotypic definition of a CTC is a CK positive, CD45 …

The C-type Lectin Receptor CLECSF8 (CLEC4D) Is Expressed by Myeloid Cells and Triggers Cellular Activation through Syk Kinase

Lisa M. Graham, Vandana V. Gupta, Georgia Schäfer, Delyth M. Reid et autres

CLECSF8 is a poorly characterized member of the "Dectin-2 cluster" of C-type lectin receptors and was originally thought to be expressed exclusively by macrophages. We show here that CLECSF8 is primarily expressed by peripheral blood neutrophils and monocytes and weakly by several …

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