In particular, she is interested in identifying the structure-activity relationships of these analogs. (wikipedia.org)
Cell4
These proteins can be present in a cell as single molecules (monomers) or as a group of several chaperone molecules (oligomers). (elifesciences.org)
propose that BiP oligomers act as reservoirs to store BiP molecules when they aren't needed by the cell. (elifesciences.org)
The term "oncotarget" encompasses all molecules, pathways, cellular functions, cell types, and even tissues that can be viewed as targets relevant to cancer as well as other diseases. (oncotarget.com)
L-767,827, an inactive structural analog of the insulin mimetic, had no effect on β-cell [Ca 2+ ] i . (diabetesjournals.org)
Solid-Phase Syn1
Solid-phase synthesis protocols were developed for preparation of three already validated prodrugs of thapsigargin: one prodrug cleavable by human kallikrein 2, one prodrug cleavable by prostate-specific antigen, and one prodrug cleavable by prostate-specific membrane antigen. (ku.dk)
Mipsagargin3
2. Thapsigargin--from Thapsia L. to mipsagargin. (nih.gov)
7. Mipsagargin: The Beginning-Not the End-of Thapsigargin Prodrug-Based Cancer Therapeutics. (nih.gov)
13. Mipsagargin, a novel thapsigargin-based PSMA-activated prodrug: results of a first-in-man phase I clinical trial in patients with refractory, advanced or metastatic solid tumours. (nih.gov)
In the case of thapsigargin, selectivity for tumor-associated cells is achieved by conjugating the drug to a peptide that is only cleaved in the vicinity of tumors to release the cytotoxic drug or an analog with retained activity. (ku.dk)
Cytotoxic1
6. Cytotoxic phenylpropanoids and an additional thapsigargin analogue isolated from Thapsia garganica. (nih.gov)
Inhibitors3
17. The effects of the phenylalanine 256 to valine mutation on the sensitivity of sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) Ca2+ pump isoforms 1, 2, and 3 to thapsigargin and other inhibitors. (nih.gov)
Her interests consider cycloaddition reactions that can realise molecules and natural products for organic photovoltaics and targeted covalent inhibitors. (wikipedia.org)
She works on the design, synthesis, and characterization of guaianolide analog covalent inhibitors with muted reactivity to thiols. (wikipedia.org)
Structure-Activity Rela1
In particular, she is interested in identifying the structure-activity relationships of these analogs. (wikipedia.org)
Transcriptional3
Here, we report that topical application of PY-60, a small-molecule activator of the transcriptional coactivator Yes-associated protein (YAP), promotes regenerative repair of cutaneous wounds in pig and human models. (bvsalud.org)
Here, we employed a screening approach that included complementary arm-specific UPR reporters and medium-throughput transcriptional profiling to identify non-toxic small molecules that phenocopy the ATF6-mediated reprogramming of the ER proteostasis environment. (elifesciences.org)
These results show that small molecule-dependent ER reprogramming, achieved through preferential activation of the ATF6 transcriptional program, is a promising strategy to ameliorate imbalances in ER function associated with degenerative protein aggregation diseases. (elifesciences.org)
Approach2
One approach to overcome this problem involves attempts at developing drugs based on general cytotoxins, like calicheamicin and thapsigargin, which kill cells at all phases of the cell cycle. (ku.dk)
used a new approach to screen over 600,000 small molecules and identified a small number that could activate ATF6-regulated genes without inducing global endoplasmic reticulum stress. (elifesciences.org)
Release4
In the study, these lupane-type triterpenes were evaluated for their inhibitory effect on histamine release from basophilic leukemia (RBL-2H3) cell line, a tumor analog of mast cells. (ijtpr.com)
The release of histamine from this mast cell was immunologically and non-immunologically stimulated by DNP 24 -BSA and thapsigargin, respectively. (ijtpr.com)
However, these compounds did not alter the histamine release from mast cells induced by thapsigargin. (ijtpr.com)
One of the small molecules tested effectively reduced the release of these proteins and prevented harmful deposits of the proteins forming in the spaces surrounding cells. (elifesciences.org)
Groups1
Now, two groups of researchers have independently identified small molecules that specifically target ATF6. (elifesciences.org)