Preclinical lead optimization of a 1, 2, 4-triazole based tankyrase inhibitor

…, RGG Leenders, ST Sowa, S Alam Brinch… - Journal of Medicinal …, 2020 - ACS Publications
Tankyrases 1 and 2 are central biotargets in the WNT/β-catenin signaling and Hippo
signaling pathways. We have previously developed tankyrase inhibitors bearing a 1,2,4-triazole …

Probiotics for the chemoprotective role against the toxic effect of cancer chemotherapy

…, U Pottoo, A Ahmadi, MS Alam - Anti-Cancer Agents …, 2022 - ingentaconnect.com
Background: Chemo- and radiation therapy-based clinical management of different types of
cancers is associated with toxicity and several side effects. Therefore, there is always an …

Development of a 1, 2, 4-triazole-based lead tankyrase inhibitor: part II

RGG Leenders, SA Brinch, ST Sowa… - Journal of Medicinal …, 2021 - ACS Publications
Tankyrase 1 and 2 (TNKS1/2) catalyze post-translational modification by poly-ADP-ribosylation
of a plethora of target proteins. In this function, TNKS1/2 also impact the WNT/β-catenin …

[HTML][HTML] Tankyrase inhibition sensitizes melanoma to PD-1 immune checkpoint blockade in syngeneic mouse models

…, M Fauskanger, K Lund, SA Brinch… - Communications …, 2020 - nature.com
The development of immune checkpoint inhibitors represents a major breakthrough in
cancer therapy. Nevertheless, a substantial number of patients fail to respond to checkpoint …

[PDF][PDF] Identification of response signatures for tankyrase inhibitor treatment in tumor cell lines

L Mygland, SA Brinch, MF Strand, PA Olsen… - Iscience, 2021 - cell.com
Small-molecule tankyrase 1 and tankyrase 2 (TNKS1/2) inhibitors are effective antitumor
agents in selected tumor cell lines and mouse models. Here, we characterized the response …

Development of a 1, 2, 4-triazole-based lead tankyrase inhibitor: part II

S Krauss, RGG Leenders, SA Brinch, ST Sowa… - 2021 - oulurepo.oulu.fi
Tankyrase 1 and 2 (TNKS1/2) catalyze post-translational modification by poly-ADP-ribosylation
of a plethora of target proteins. In this function, TNKS1/2 also impact the WNT/β-catenin …

The tankyrase inhibitor OM-153 demonstrates anti-tumor effect with a therapeutic index above 10

SA Brinch, E Amundsen-Isaksen, S Espada… - Cancer Research, 2022 - AACR
The catalytic enzymes tankyrase 1 and 2 (TNKS1/2) poly-ADP-ribosylate target proteins,
including AXIN proteins, to earmark them for degradation by the ubiquitin-proteasomal system. …

The tankyrase inhibitor OM-153 demonstrates antitumor efficacy and a therapeutic window in mouse models

SA Brinch, E Amundsen-Isaksen, S Espada… - Cancer Research …, 2022 - AACR
The catalytic enzymes tankyrase 1 and 2 (TNKS1/2) alter protein turnover by poly-ADP-ribosylating
target proteins, which earmark them for degradation by the ubiquitin–proteasomal …

Influence of antidrug antibodies on plectasin efficacy and pharmacokinetics

KS Brinch, N Frimodt-Møller, N Høiby… - Antimicrobial agents …, 2009 - Am Soc Microbiol
Plectasin is a 4.4-kDa antimicrobial peptide with the potential to be a treatment of infections
caused by gram-positive bacteria. Since plectasin is a large molecule compared to …

Role of Endoscopy in Diagnosis of Adult Patients with Dysphagia

KT Al-Abachi - Annals of the College of Medicine, Mosul, 2023 - mosuljournals.com
Background: Dysphagia is an alarm gastrointestinal symptom that may be a manifestation of
serious underlying condition, which necessitate proper and timely medical intervention. …