Results 201 to 210 of about 43,753 (252)
Replacement soaking for human tankyrase 2 enables studies on substrate analogues and inhibitors
Replacement soaking, also known as cross‐soaking, is a compelling method for solving complex structures in cases where traditional soaking and co‐crystallization approaches fail. This method is demonstrated with human tankyrase 2, and new crystal structures of complexes with nanomolar inhibitors and an analogue of the substrate NAD+ are reported ...
Johan Pääkkönen +3 more
wiley +1 more source
Recent Advances in the Molecular Mechanisms of Bacterial Anti‐Phage Defence Systems
Panoptes as an example for an antiphage system consists of OptS producing a cyclic dinucleotide that prevents activation of OptE, a transmembrane protein. Phage T4 infection introduces the sponge protein Acb2 that adsorbs the cyclic dinucleotide thus activating OptE which disrupts the cell membrane aborting phage infection.
Harald Brüssow
wiley +1 more source
The GLP‐1–Mitochondria Axis in Metabolic Aging
Glucagon‐like peptide‐1 receptor agonists engage AMPK–PGC‐1α signaling to remodel mitochondrial biogenesis, dynamics, and quality control, but downstream effects are context‐dependent and tissue‐specific rather than uniformly receptor‐proximal. Whether this proposed mitochondria‐incretin axis reflects a novel geroscience mechanism or indirect metabolic
Renin Chang +3 more
wiley +1 more source
Pancreatic Cancer—Advances in the Last 50 Years
World Journal of Surgery, Volume 50, Issue 8, Page 2106-2115, August 2026.
S. George Barreto +5 more
wiley +1 more source
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Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase
Bioorganic and Medicinal Chemistry Letters, 2008We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed with restricted conformation through intramolecular hydrogen bond formation; the compounds exhibit low nM enzyme and cellular activity
Keith A, Menear +13 more
exaly +3 more sources
Natural Inhibitors of Poly(ADP-ribose) Polymerase-1
Molecular Neurobiology, 2012Poly(ADP-ribose) polymerases (PARPs) are enzymes that catalyze the transfer of ADP-ribose units from β-nicotinamide adenine dinucleotide (NAD(+)) to acceptor proteins. PARP-1 is responsible for more than 90 % of protein poly-ADP-ribosylation in the brain and may play a role as a molecular switch for cell survival and death. The functional roles of PARP-
Robert Strosznajder, Marek Banasik
exaly +3 more sources
Comparative Analyses of Poly(ADP-Ribose) Polymerase Inhibitors
International Journal of Toxicology, 2022Poly(ADP-ribose) polymerase inhibitors (PARPi) are approved as monotherapies in BRCA1/2-mutated (m BRCA1/2) metastatic breast and ovarian cancers, and in advanced pancreatic and metastatic castration-resistant prostate cancers. Differential safety profiles across PARPi necessitate improved mechanistic understanding of inhibitor ...
Mausumee Guha +9 more
openaire +2 more sources
Poly(ADP-Ribose) Polymerase Inhibitors
Current Medicinal Chemistry, 2003Poly(ADP-ribose) polymerase-1 (PARP-1) is the principal member of the PARP enzyme family consisting of PARP-1 and several recently identified novel poly(ADP-ribosyl)ating enzymes. PARP-1 functions as a DNA damage sensor and signalling molecule. Upon binding to DNA breaks, activated PARP cleaves NAD(+) into nicotinamide and ADP-ribose and polymerizes ...
Garry J, Southan, Csaba, Szabó
openaire +2 more sources
Current Opinion in Oncology, 2019
Purpose of review In the past few years, the advent of PARP inhibitors has been a revolution in the management of ovarian cancer. Patients harboring somatic or germ line BRCA1/2 mutations exhibit different clinical and treatment response behavior.
Hélène, Vanacker +2 more
openaire +2 more sources
Purpose of review In the past few years, the advent of PARP inhibitors has been a revolution in the management of ovarian cancer. Patients harboring somatic or germ line BRCA1/2 mutations exhibit different clinical and treatment response behavior.
Hélène, Vanacker +2 more
openaire +2 more sources
Poly (ADP-ribose) Polymerase Inhibitors in Cancer Treatment
American Journal of Clinical Oncology, 2014Recent research on inhibitors of poly (ADP-ribose) polymerase (PARP) has demonstrated their potential for improving cancer therapy. They inhibit protein poly (ADP-ribosyl)ation and thus affect numerous molecular and cellular functions, including DNA repair and cell survival, that are critical for such physiological and patho-physiological states as ...
Kathryn A, Mason +5 more
openaire +2 more sources

