Results 81 to 90 of about 504,672 (298)
How Desirable Are Your IC50s?: A Way to Enhance Screening-Based Decision Making [PDF]
SLAS Discovery, 2010 Dose-response curves, resulting in estimates of endpoints such as the IC(50), are fundamental to drug discovery. However, some estimates are more reliable than others. It is important to know just how reliable an estimate is if we want to base decisions on it or use it in further modeling.
Gaia V, Paolini +2 more
openaire +2 more sources
FEBS Open Bio, EarlyView.Chemoresistance in bladder cancer: Macrophage recruitment associated with CXCL1, CXCL5 and CXCL8 expression is characteristic of Gemcitabine/Cisplatin (Gem/Cis) Non‐Responder tumors (right side) while Responder tumors did not show substantial tumor‐stromal crosstalk (left side). All biological icons are attributed to Bioicons: carcinoma, cancerous‐cell‐
Sophie Leypold +11 more
wiley +1 more source
Inhibitors of Bacterial \u3cem\u3eN\u3c/em\u3e-succinyl-L,L-diaminopimelic Acid Desuccinylase (DapE) and Demonstration of in vitro Antimicrobial Activity [PDF]
, 2009 The dapE-encoded N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) is a critical bacterial enzyme for the construction of the bacterial cell wall. A screen biased toward compounds containing zinc-binding groups (ZBG’s) including thiols, carboxylic ...
Armoush, Nicola +3 more
core +1 more source
The contrasting activity of iodido versus chlorido ruthenium and osmium arene azo- and imino-pyridine anticancer complexes : control of cell selectivity, cross-resistance, p53 dependence, and apoptosis pathway [PDF]
, 2013 Organometallic half-sandwich complexes [M(p-cymene)(azo/imino-pyridine)X]+ where M = RuII or OsII and X ═ Cl or I, exhibit potent antiproliferative activity toward a range of cancer cells.
Romero-Canelón, Isolda +2 more
core +1 more source
PARP inhibitors induce a senescence phenotype in non‐small cell lung carcinoma cell lines
FEBS Open Bio, EarlyView.Talazoparib is the most potent inducer of senescence among different PARP1 inhibitors in human NSCLC cells. In the absence of PARP, no senescence phenotype was observed, demonstrating that PARP1 is necessary for the induction of senescence by this inhibitor.
Camille Huart +7 more
wiley +1 more source
1,2,6-thiadiazinones as novel narrow spectrum calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) inhibitors [PDF]
, 1983 We demonstrate for the first time that 4H-1,2,6-thiadiazin-4-one (TDZ) can function as a chemotype for the design of ATP-competitive kinase inhibitors. Using insights from a co-crystal structure of a 3,5-bis(arylamino)-4H-1,2,6-thiadiazin-4-one bound to ...
Asquith, Christopher R.M. +11 more
core +3 more sources
Nonspecific, Reversible Inhibition of Voltage-Gated Calcium Channels by CaMKII Inhibitor CK59 [PDF]
, 2013 Investigation of kinase-related processes often uses pharmacological inhibition to reveal pathways in which kinases are involved. However, one concern about using such kinase inhibitors is their potential lack of specificity.
Kahrls, Andrew S., Mynlieff, Michelle
core +2 more sources
FEBS Open Bio, EarlyView.This study investigated a novel WST‐8‐based assay for evaluating d‐Amino acid oxidase (DAO) inhibitors. We confirmed its effectiveness using known inhibitors and found that uremic toxins possess relatively weak inhibitory activity compared to existing drugs.
Kahoko Miyake +4 more
wiley +1 more source
Tạp chí Khoa học và Công nghệThis study investigated the extraction of total phenolic compounds from Perilla frutescens (L.) Britt leaves collected in Tuy Loan, Danang City, Vietnam.
Minh Nguyet Thi NGUYEN +4 more
doaj +1 more source
FEBS Open Bio, EarlyView.Pharmacological inhibition of PERK in a DEN‐induced mouse model of liver cancer does not reduce tumor burden but alters cellular stress signaling. Despite blocking PERK activity, downstream stress responses, including CHOP expression, remain active, suggesting compensatory mechanisms within the unfolded protein response that may influence tumor ...
Ada Lerma‐Clavero +5 more
wiley +1 more source