Discover and read the best of Twitter Threads about #smallmolecule
Most recents (4)
1/ $PVCT’s Modernized #SmallMolecule #RoseBengal: A #DrugSubstance, and #ActivePharmaceuticalIngredient for 21st Century #DrugDevelopment. A THREAD.
2/ “Everyone” seems to know or understand #RoseBengal, but do they (you) really?
3/ #RoseBengal is a small molecule (i.e., <1,000 Daltons*), but a “heavy” one at 973.67 Da or g/mol. It is heavy because of its four iodides, which comprise 52% of its molecular weight.
885 of all small molecule drugs pass the rule-of-five test; of these, 619 (70%) are actually dosed orally, whereas 159 (20%) of orally dosed drugs fail at least one of the rule-of-five parameters
-John P Overington, Bissan Al-Lazikani and Andrew L Hopkins
nature.com/articles/nrd21…
-John P Overington, Bissan Al-Lazikani and Andrew L Hopkins
nature.com/articles/nrd21…
@johnpoverington et al determine that all current drugs with a known mode-of-action act through 324 distinct molecular drug targets. 266 are human-genome-derived proteins, and the remainder are bacterial, viral, fungal or other pathogenic organism targets
readcube.com/articles/10.10…
readcube.com/articles/10.10…
Small molecule drugs modulate 248 proteins, of which 207 are targets encoded by the human genome. Oral #smallmolecule drugs target 227 molecular targets, of which 186 are human
-@johnpoverington, Bissan Al-Lazikani, Andrew Hopkins
nature.com/articles/nrd21…
-@johnpoverington, Bissan Al-Lazikani, Andrew Hopkins
nature.com/articles/nrd21…
Congrats to Hayley Zullow of @kadochlab @HarvardMITmdphd @BBS_Harvard programs and our team, including @akshaysci, @JunQiLab, @ar_davino, and many others, on this exciting new study out today in @MolecularCell @CellPressNews ! Tweetorial below: (1/7) cell.com/molecular-cell…
Here, we explore the impact of the #fusion oncoprotein hallmark to #myxoidliposarcoma, FUS-DDIT3, and its impact on #BAF #SWISNF complex-mediated #chromatin remodeling activities genome wide. (2/7)
We previously showed that fusions such as SS18-SSX and EWS-FLI1, in #synovialsarcoma and #Ewingsarcoma, respectively, interact with BAF complexes and direct their genomic occupancy in a cancer-specific, gain-of-function manner. (3/7)
Time to catch up on some #Senescence papers, starting with beautiful work by @corina_amor_MD, Judith Freucht & @JosefLeibold. They used #CART #CellTherapy to clear #Senescent cells, and you'll never guess what happened next! nature.com/articles/s4158…
Just kidding, you guessed it: disease model mice got better. Props to the authors for A) inducing #Senescence in 3 different ways, B) using 2 models of #NASH/liver #Fibrosis, and C) validating their senescence observations in human samples of #Cancer and #Atherosclerosis.
The linchpin of the paper was identifying a specific membrane marker on #Senescent cells, uPAR. They used bulk #Transcriptomics to identify candidates, then narrowed down with #Proteomic data. Go #Omics!
They didn't explore whether uPAR is causative for the #Senescent phenotype.
They didn't explore whether uPAR is causative for the #Senescent phenotype.
