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Showing results 1 to 6 of 6

Journal article

Combining cancer chemotherapeutics with bacterial DNA repair inhibitors to develop novel antimicrobials

Authors : Bernacchia, Lorenzo (2023)

Cancer chemotherapeutics kill rapidly dividing cells, which includes cells of the immune system. The 12 resulting neutropenia predisposes patients to infection, which delays treatment and is a major cause 13 of morbidity and mortality. Here we have exploited the cytotoxicity of the anti-cancer compound 14 cisplatin to screen for FDA-approved drugs that impair bacterial nucleotide excision DNA repair (NER), 15 the primary mechanism bacteria use to repair ...

Journal article

Conserved Structure Modules within the lncRNA SChLAP1 Mediate Protein Recognition Implicated in Aggressive Prostate Cancer

Authors : McFadden, Emily J. (2023)

The lncRNA Second Chromosome Locus Associated with Prostate 1 (SChLAP1) was previously identified as a predictive biomarker and potential driver of aggressive prostate cancer. Recent work suggests that SChLAP1 may bind the SWI/SNF chromatin remodeling complex to promote prostate cancer metastasis, though the exact role of SWI/SNF recognition is debated. To date, there are no detailed biochemical studies of apo SChLAP1 or SChLAP1:protein com...

Journal article

Design of a mucin-selective protease for targeted degradation of cancer-associated mucins

Authors : Pedram, Kayvon (2023)

Targeted protein degradation is an emerging strategy for the elimination of classically undruggable proteins. Here, to expand the landscape of substrates that can be selectively degraded, we designed degraders which are dependent on both peptide sequence and glycosylation status of the target protein. We applied this approach to mucins, O-glycosylated proteins that drive cancer progression through biophysical and immunological mechanisms. Engineering of&...

Journal Article

Identification of putative druggable pockets in PRL3, a significant oncology target, using in silico analysis

Authors : Bennett, Grace M. (2023)

Aberrant cellular phosphorylation is a hallmark of several diseases including inflammation and cancers (1–3). Protein phosphorylation is a post-translational modification that can act as a switch to regulate biochemical pathways and is regulated by the concerted action of two classes of enzymes: kinases and phosphatases. As such, kinases and phosphatases present as significant potential clinical molecular targets. To date, several kinase inhibitors have&#...

Ebooks (Sách điện tử)

Oatmeal and wheat flour as the sources of thyroid peroxidase (TPO), lipoxygenase (LOX) and xanthine oxidase (XO) modulators potentially applicable in the prevention of inflammatory

Authors : Kowalska, Ewa Habza (2023)

Despite the widespread potential pro-health effects of ferulic acid (FA), their interference in the 10 progression of thyroid dysfunction has mainly remained unresolved. Here, we combined in vitro enzyme 11 studies with the in vitro cellular approach to investigate the potential of main dietary sources of FA - the 12 oatmeal (OM) and wheat flour (WF) compounds for the prophylactics of inflammatory thyroid diseases. 13 Potentially bioaccessible OM an...

Journal article

PH Domain-Mediated Autoinhibition and Oncogenic Activation of Akt

Authors : Bae, Hwan (2023)

Previously, we reported that the conformation of autoinhibited Akt, a Ser/Thr protein kinase that plays a central role in metabolism and cancer, may be shifted by small molecule allosteric inhibitors limiting the mechanistic insights from existing X-ray structures that have relied on such compounds (Chu, Viennet, et al, 2020). Here we discover unexpectedly that a single mutation, R86A, in Akt’s PH domain exhibits intensified autoinhibitory&...