Full Text Journal Articles by
Author Jared Sivinski

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Analogs of nitrofuran antibiotics are potent GroEL/ES inhibitor pro-drugs.

Mckayla Stevens, Chris Howe, Anne-Marie Ray, Alex Washburn, Siddhi Chitre, Jared Sivinski, Yangshin Park, Quyen Q Hoang, Eli Chapman, Steven M Johnson,

In two previous studies, we identified compound 1 as a moderate GroEL/ES inhibitor with weak to moderate antibacterial activity against Gram-positive and Gram-negative bacteria including Bacillus subtilis, methicillin-resistant Staphylococcus aureus, Klebsiella pneumonia, Acinetobacter baumannii, and SM101 Escherichia coli (which has a compromised lipopolysaccharide biosynthetic pathway making bacteria more permeable to ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2020, 28(22):115710]

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Targeting dual signalling pathways in concert with immune checkpoints for the treatment of pancreatic cancer.

Erik S Knudsen, Vishnu Kumarasamy, Sejin Chung, Amanda Ruiz, Paris Vail, Stephanie Tzetzo, Jin Wu, Ram Nambiar, Jared Sivinski, Shailender S Chauhan, Mukund Seshadri, Scott I Abrams, Jianmin Wang, Agnieszka K Witkiewicz,

OBJECTIVE:This study exploits the intersection between molecular-targeted therapies and immune-checkpoint inhibition to define new means to treat pancreatic cancer. DESIGN:Patient-derived cell lines and xenograft models were used to define the response to CDK4/6 and MEK inhibition in the tumour compartment. Impacts relative to immunotherapy were performed using subcutaneous and orthotopic ... Read more >>

Gut (Gut)
[2020, :]

Cited: 0 times

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A one-step, atom economical synthesis of thieno[2,3-d]pyrimidin-4-amine derivatives via a four-component reaction.

Taoda Shi, Christopher J Zerio, Jared Sivinski, Andrew J Ambrose, Kohlson T Moore, Thomas Buckley, Lynn Kaneko, Mae Zhang, Donna D Zhang, Eli Chapman,

A Na2HPO4-catalyzed four-component reaction between a ketone, malononitrile, S8 and formamide has been realized for the first time. This reaction provides a concise approach to thieno[2,3-d]pyrimidin-4-amines, previously requiring 5 steps. The utility of this reaction was validated by preparing a multi-targeted kinase inhibitor and an inhibitor of the NRF2 pathway ... Read more >>

European J Org Chem (European journal of organic chemistry)
[2019, 20(2):3269-3272]

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A high throughput substrate binding assay reveals hexachlorophene as an inhibitor of the ER-resident HSP70 chaperone GRP78.

Andrew J Ambrose, Christopher J Zerio, Jared Sivinski, Cody J Schmidlin, Taoda Shi, Alison B Ross, Kimberly J Widrick, Steven M Johnson, Donna D Zhang, Eli Chapman,

Glucose-regulated protein 78 (GRP78) is the ER resident 70 kDa heat shock protein 70 (HSP70) and has been hypothesized to be a therapeutic target for various forms of cancer due to its role in mitigating proteotoxic stress in the ER, its elevated expression in some cancers, and the correlation between high ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2019, 29(14):1689-1693]

Cited: 0 times

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Dual-targeting GroEL/ES chaperonin and protein tyrosine phosphatase B (PtpB) inhibitors: A polypharmacology strategy for treating Mycobacterium tuberculosis infections.

Alex Washburn, Sanofar Abdeen, Yulia Ovechkina, Anne-Marie Ray, Mckayla Stevens, Siddhi Chitre, Jared Sivinski, Yangshin Park, James Johnson, Quyen Q Hoang, Eli Chapman, Tanya Parish, Steven M Johnson,

Current treatments for Mycobacterium tuberculosis infections require long and complicated regimens that can lead to patient non-compliance, increasing incidences of antibiotic-resistant strains, and lack of efficacy against latent stages of disease. Thus, new therapeutics are needed to improve tuberculosis standard of care. One strategy is to target protein homeostasis pathways ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2019, 29(13):1665-1672]

Cited: 1 time

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Cell cycle plasticity driven by MTOR signaling: integral resistance to CDK4/6 inhibition in patient-derived models of pancreatic cancer.

Erik S Knudsen, Vishnu Kumarasamy, Amanda Ruiz, Jared Sivinski, Sejin Chung, Adam Grant, Paris Vail, Shailender S Chauhan, Tun Jie, Taylor S Riall, Agnieszka K Witkiewicz,

Pancreatic ductal adenocarcinoma (PDAC), like many KRAS-driven tumors, preferentially loses CDKN2A that encodes an endogenous CDK4/6 inhibitor to bypass the RB-mediated cell cycle suppression. Analysis of a panel of patient-derived cell lines and matched xenografts indicated that many pancreatic cancers have intrinsic resistance to CDK4/6 inhibition that is not due ... Read more >>

Oncogene (Oncogene)
[2019, 38(18):3355-3370]

Cited: 5 times

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HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules.

Mckayla Stevens, Sanofar Abdeen, Nilshad Salim, Anne-Marie Ray, Alex Washburn, Siddhi Chitre, Jared Sivinski, Yangshin Park, Quyen Q Hoang, Eli Chapman, Steven M Johnson,

All living organisms contain a unique class of molecular chaperones called 60 kDa heat shock proteins (HSP60 - also known as GroEL in bacteria). While some organisms contain more than one HSP60 or GroEL isoform, at least one isoform has always proven to be essential. Because of this, we have been ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2019, 29(9):1106-1112]

Cited: 4 times

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