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From PARP1 to TNKS2 Inhibition: A Structure-Based Approach.

ACS medicinal chemistry letters

Tomassi S, Pfahler J, Mautone N, Rovere A, Esposito C, Passeri D, Pellicciari R, Novellino E, Pannek M, Steegborn C, Paiardini A, Mai A, Rotili D.
PMID: 32435397
ACS Med Chem Lett. 2020 Feb 03;11(5):862-868. doi: 10.1021/acsmedchemlett.9b00654. eCollection 2020 May 14.

Tankyrases (TNKSs) have recently gained great consideration as potential targets in Wnt/β-catenin pathway-dependent solid tumors. Previously, we reported the 2-mercaptoquinazolin-4-one MC2050 as a micromolar PARP1 inhibitor. Here we show how the resolution of the X-ray structure of PARP1 in...

Fragmentation production of doubly heavy baryons.

Physical review. D, Particles and fields

Doncheski MA, Steegborn J, Stong ML.
PMID: 10020117
Phys Rev D Part Fields. 1996 Feb 01;53(3):1247-1252. doi: 10.1103/physrevd.53.1247.

No abstract available.

Correction: The mechanism of sirtuin 2-mediated exacerbation of alpha-synuclein toxicity in models of Parkinson disease.

PLoS biology

de Oliveira RM, Vicente Miranda H, Francelle L, Pinho R, Szegö ÉM, Martinho R, Munari F, Lázaro DF, Moniot S, Guerreiro P, Fonseca-Ornelas L, Marijanovic Z, Antas P, Gerhardt E, Enguita FJ, Fauvet B, Penque D, Pais TF, Tong Q, Becker S, Kügler S, Lashuel HA, Steegborn C, Zweckstetter M, Outeiro TF.
PMID: 28379951
PLoS Biol. 2017 Apr 05;15(4):e1002601. doi: 10.1371/journal.pbio.1002601. eCollection 2017 Apr.

[This corrects the article DOI: 10.1371/journal.pbio.2000374.].

Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.

ACS medicinal chemistry letters

You W, Steegborn C.
PMID: 33214841
ACS Med Chem Lett. 2020 Sep 24;11(11):2285-2289. doi: 10.1021/acsmedchemlett.0c00407. eCollection 2020 Nov 12.

Sirtuins are NAD

Constitutively Activating GNAS Somatic Mutation in Right Ventricular Outflow Tract Tachycardia.

Circulation. Arrhythmia and electrophysiology

Ip JE, Xu L, Dai J, Steegborn C, Jaffré F, Evans T, Cheung JW, Basson CT, Panaghie G, Krogh-Madsen T, Abbott GW, Lerman BB.
PMID: 34587755
Circ Arrhythm Electrophysiol. 2021 Oct;14(10):e010082. doi: 10.1161/CIRCEP.121.010082. Epub 2021 Sep 30.

[Figure: see text].

Effects of 3-Bromo-4,5-dihydroisoxazole Derivatives on Nrf2 Activation and Heme Oxygenase-1 Expression.

ChemistryOpen

Pinto A, El Ali Z, Moniot S, Tamborini L, Steegborn C, Foresti R, De Micheli C.
PMID: 30397576
ChemistryOpen. 2018 Oct 12;7(11):858-864. doi: 10.1002/open.201800185. eCollection 2018 Nov.

Natural and synthetic electrophilic compounds have been shown to activate the antioxidant protective Nrf2 (nuclear factor erythroid 2-related factor 2)/heme oxygenase-1 (HO-1) axis in cells and tissues. Here, we tested the ability of different isoxazoline-based electrophiles to up-regulate Nrf2/HO-1....

Sirt4: A Multifaceted Enzyme at the Crossroads of Mitochondrial Metabolism and Cancer.

Frontiers in oncology

Tomaselli D, Steegborn C, Mai A, Rotili D.
PMID: 32373514
Front Oncol. 2020 Apr 15;10:474. doi: 10.3389/fonc.2020.00474. eCollection 2020.

Sirtuins are NAD

Total Synthesis of (+)-Cornexistin.

Angewandte Chemie (International ed. in English)

Steinborn C, Wildermuth RE, Barber DM, Magauer T.
PMID: 32558114
Angew Chem Int Ed Engl. 2020 Sep 21;59(39):17282-17285. doi: 10.1002/anie.202008158. Epub 2020 Aug 18.

Herein, we describe the first total synthesis of (+)-cornexistin as well as its 8-epi-isomer starting from malic acid. The robust and scalable route features a Nozaki-Hiyama-Kishi reaction, an auxiliary-controlled syn-Evans-aldol reaction, and a highly efficient intramolecular alkylation to form...

Metabolic Rewiring by Loss of Sirt5 Promotes Kras-Induced Pancreatic Cancer Progression.

Gastroenterology

Hu T, Shukla SK, Vernucci E, He C, Wang D, King RJ, Jha K, Siddhanta K, Mullen NJ, Attri KS, Murthy D, Chaika NV, Thakur R, Mulder SE, Pacheco CG, Fu X, High RR, Yu F, Lazenby A, Steegborn C, Lan P, Mehla K, Rotili D, Chaudhary S, Valente S, Tafani M, Mai A, Auwerx J, Verdin E, Tuveson D, Singh PK.
PMID: 34245764
Gastroenterology. 2021 Nov;161(5):1584-1600. doi: 10.1053/j.gastro.2021.06.045. Epub 2021 Jul 08.

BACKGROUND & AIMS: SIRT5 plays pleiotropic roles via post-translational modifications, serving as a tumor suppressor, or an oncogene, in different tumors. However, the role SIRT5 plays in the initiation and progression of pancreatic ductal adenocarcinoma (PDAC) remains unknown.METHODS: Published...

Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10).

ACS medicinal chemistry letters

Fushimi M, Buck H, Balbach M, Gorovyy A, Ferreira J, Rossetti T, Kaur N, Levin LR, Buck J, Quast J, van den Heuvel J, Steegborn C, Finkin-Groner E, Kargman S, Michino M, Foley MA, Miller M, Liverton NJ, Huggins DJ, Meinke PT.
PMID: 34413957
ACS Med Chem Lett. 2021 Jul 14;12(8):1283-1287. doi: 10.1021/acsmedchemlett.1c00273. eCollection 2021 Aug 12.

Soluble adenylyl cyclase (sAC) has gained attention as a potential therapeutic target given the role of this enzyme in intracellular signaling. We describe successful efforts to design improved sAC inhibitors amenable for

Metabolic Rewiring by Loss of Sirt5 Promotes Kras-Induced Pancreatic Cancer Progression.

Gastroenterology

Hu T, Shukla SK, Vernucci E, He C, Wang D, King RJ, Jha K, Siddhanta K, Mullen NJ, Attri KS, Murthy D, Chaika NV, Thakur R, Mulder SE, Pacheco CG, Fu X, High RR, Yu F, Lazenby A, Steegborn C, Lan P, Mehla K, Rotili D, Chaudhary S, Valente S, Tafani M, Mai A, Auwerx J, Verdin E, Tuveson D, Singh PK.
PMID: 34245764
Gastroenterology. 2021 Nov;161(5):1584-1600. doi: 10.1053/j.gastro.2021.06.045. Epub 2021 Jul 08.

BACKGROUND & AIMS: SIRT5 plays pleiotropic roles via post-translational modifications, serving as a tumor suppressor, or an oncogene, in different tumors. However, the role SIRT5 plays in the initiation and progression of pancreatic ductal adenocarcinoma (PDAC) remains unknown.METHODS: Published...

Constitutively Activating GNAS Somatic Mutation in Right Ventricular Outflow Tract Tachycardia.

Circulation. Arrhythmia and electrophysiology

Ip JE, Xu L, Dai J, Steegborn C, Jaffré F, Evans T, Cheung JW, Basson CT, Panaghie G, Krogh-Madsen T, Abbott GW, Lerman BB.
PMID: 34587755
Circ Arrhythm Electrophysiol. 2021 Oct;14(10):e010082. doi: 10.1161/CIRCEP.121.010082. Epub 2021 Sep 30.

[Figure: see text].

Showing 1 to 12 of 12 entries