#inhibitors — Public Fediverse posts

Next-generation #inhibitors of #SARS-CoV-2 #Mpro overcome the deficiencies of #Paxlovid, https://etidiohnew.blogspot.com/2026/04/next-generation-inhibitors-of-sars-cov.html

https://www.europesays.com/ch/39562/ Excellergy to be acquired by Novartis for up to USD 2 billion to advance potentially first-in-class trifunctional effector cell response inhibitors #2 #acquired #advance #be #billion #by #Cell #effector #Excellergy #FirstInClass #for #inhibitors #Novartis #potentially #response #to #trifunctional #Up #usd

#Oseltamivir aziridines are potent #influenza #neuraminidase #inhibitors and imaging agents, https://etidiohnew.blogspot.com/2026/03/oseltamivir-aziridines-are-potent.html

#Oseltamivir aziridines are potent #influenza #neuraminidase #inhibitors and imaging agents, https://etidiohnew.blogspot.com/2026/03/oseltamivir-aziridines-are-potent.html

#Oseltamivir aziridines are potent #influenza #neuraminidase #inhibitors and imaging agents, https://etidiohnew.blogspot.com/2026/03/oseltamivir-aziridines-are-potent.html

#Oseltamivir aziridines are potent #influenza #neuraminidase #inhibitors and imaging agents, https://etidiohnew.blogspot.com/2026/03/oseltamivir-aziridines-are-potent.html

#Oseltamivir aziridines are potent #influenza #neuraminidase #inhibitors and imaging agents, https://etidiohnew.blogspot.com/2026/03/oseltamivir-aziridines-are-potent.html

When the immune system detects a protein from a pathogen,
it’s supposed to dispatch killer T cells to eliminate the invader.

Some cancers can interfere with this process by hijacking the checkpoint proteins that keep our immune system from revving out of control
and using them to turn T cells off.

Starting in the mid-1990s, several research teams found success by treating mice with #checkpoint #inhibitors,
-- then a new class of drugs designed to keep tumor cells from concealing their identity and signaling, effectively, “nothing to see here.”

Thirty years on, checkpoint inhibitors have become a transformative tool in cancer treatment, especially for melanoma.

The research that went into developing checkpoint inhibitors showed conclusively that immune cells detect cancer much in the same way they identify other pathogens:

through differences in protein structure determined by DNA
—a crucial insight.

But as revolutionary as checkpoint inhibitors have been for immunotherapy, they don’t work for everyone
—far from it.

Some 80 percent of patients do not respond to this class of drugs.

Researchers are still trying to understand all the mechanisms that play a role in determining who does respond,
but one key factor is whether the immune system is able to recognize tumor cells on the basis of their mutations.

This is where mRNA vaccines come in.

#Jason #Luke, a melanoma researcher who now serves as chief medical officer of mRNA-medicine start-up #Strand #Therapeutics,
helped to design several ongoing clinical trials of mRNA vaccines for cancer.

He explains that both checkpoint inhibitors and mRNA vaccines build on our deep evolutionary adaptation for fighting pathogens
by identifying the proteins they shed in our bodies.

But checkpoint inhibitors are effective only if the patient’s immune system recognizes the cancer as a threat.

In contrast, mRNA vaccines have the potential to work even in patients whose cancers haven’t spurred much immune response.

The trick, Luke says, is using computational tools to decipher which of a given tumor’s mutations are most likely to be found by the immune system.

#MichaelMemoli
#WilliamColey #immunotherapy #stroma #MHC

#Global #update on susceptibilities of #influenza viruses to #neuraminidase #inhibitors and the cap-dependent endonuclease inhibitor #baloxavir, 2020–2023, https://etidiohnew.blogspot.com/2025/06/global-update-on-susceptibilities-of.html

Effects of #JAK #inhibitors in adults admitted to #hospital due to #COVID19: a systematic review and individual participant data meta-analysis of randomised clinical trials, https://etidiohnew.blogspot.com/2025/05/effects-of-jak-inhibitors-in-adults.html

Great keynote lecture by Marta Artola of the @LED3hub at #Lunteren. She talked about the importance of glycosidases in various diseases and her great work on conformationally locked #covalent and non-covalent #inhibitors and #probes.
#chemistry #ChemBio
https://pubs.acs.org/doi/10.1021/jacs.2c05666

#Structural and #virologic #mechanism of the emergence of #resistance to #Mpro #inhibitors in #SARS-CoV-2, PNAS: https://www.pnas.org/doi/abs/10.1073/pnas.2404175121?af=R

We generated SARS-CoV-2 variants resistant to three SARS-CoV-2 main protease (Mpro) inhibitors (#nirmatrelvir, TKB245, and 5h), by propagating the ancestral SARS-CoV-2WK521WT in VeroE6TMPRSS2 cells with increasing concentrations of each inhibitor and examined their structural and virologic profiles.

Whole- #Genome #Analysis of #Influenza #H1N1pdm09 Viruses Isolated from #ILI #Outpatients in #Myanmar & Community-Acquired #Oseltamivir - #Resistant Strains Present from 2015 to 2019 https://www.mdpi.com/1999-4915/16/8/1300

1 virus intra-subtype reassortment, collected in the '15 season. 3 viruses possessed #H275Y substitution in NA protein, appearing to be CA without prior administration of neuraminidase #inhibitors. These viruses exhibited highly reduced susceptibility to #oseltamivir & #peramivir.

#Genetic & #molecular characterization of #H9N2 avian #influenza viruses in #Yunnan Province, SW #China, Poul Sci.: https://www.sciencedirect.com/science/article/pii/S0032579124006199?via%3Dihub

Analysis of these #aminoacid sites suggests that H9N2 influenza viruses in Yunnan continue to mutate and adapt to #mammals & are sensitive to #neuraminidase #inhibitors but resistant to #adamantanes. It is necessary to strengthen surveillance of AIV H9N2 subtypes in poultry and LPMs in Yunnan to further understand their genetic diversity.

The Raf #kinase #inhibitors #Dabrafenib and #Regorafenib impair #Zika virus #replication via distinct mechanisms, J Virol.: https://journals.asm.org/doi/full/10.1128/jvi.00618-24?af=R

This study provides further insight into ZIKV-host interactions and has implications for the development of novel #antivirals against ZIKV and possibly other #flaviviruses.

Multiple #transatlantic #incursions of #HPAI clade 2.3.4.4b A(#H5N5) virus into North #America and #spillover to #mammals, Cell Rep.: https://www.cell.com/cell-reports/fulltext/S2211-1247(24)00808-8?_returnURL=https%3A%2F%2Flinkinghub.elsevier.com%2Fretrieve%2Fpii%2FS2211124724008088%3Fshowall%3Dtrue

#Seabirds likely enabled multiple incursions of A(H5N5) virus from #Europe to #Canada. Some A(H5N5) viruses possessed the mammalian #adaptation #marker #PB2-E627K. A(H5N5) viruses demonstrated rapid 100% #mortality and some transmission in #ferrets. A(H5N5) viruses preferred avian virus receptors and are sensitive to NA #inhibitors.

#Genotypic & #phenotypic susceptibility of emerging avian #influenza A viruses to
#NAIs & cap-dependent endonuclease #inhibitors, Antiviral Res.: https://www.sciencedirect.com/science/article/pii/S0166354224001682?via%3Dihub

Frequencies of markers of resistance to antivirals were low among >20,000 avian influenza A viruses studied. #H5Nx, #H7Nx, & #H9N2 viruses were susceptible to sub-nanomolar concentrations of antivirals. NA-I222M, but not NA-S246N or NA-I222V, in H5N1 confers reduced inhibition by #oseltamivir.

#Genotypic & #phenotypic susceptibility of emerging avian #influenza A viruses to
#NAIs & cap-dependent endonuclease #inhibitors, Antiviral Res.: https://www.sciencedirect.com/science/article/pii/S0166354224001682?via%3Dihub

Frequencies of markers of resistance to antivirals were low among >20,000 avian influenza A viruses studied. #H5Nx, #H7Nx, & #H9N2 viruses were susceptible to sub-nanomolar concentrations of antivirals. NA-I222M, but not NA-S246N or NA-I222V, in H5N1 confers reduced inhibition by #oseltamivir.

#Genotypic & #phenotypic susceptibility of emerging avian #influenza A viruses to
#NAIs & cap-dependent endonuclease #inhibitors, Antiviral Res.: https://www.sciencedirect.com/science/article/pii/S0166354224001682?via%3Dihub

Frequencies of markers of resistance to antivirals were low among >20,000 avian influenza A viruses studied. #H5Nx, #H7Nx, & #H9N2 viruses were susceptible to sub-nanomolar concentrations of antivirals. NA-I222M, but not NA-S246N or NA-I222V, in H5N1 confers reduced inhibition by #oseltamivir.

#Genotypic & #phenotypic susceptibility of emerging avian #influenza A viruses to
#NAIs & cap-dependent endonuclease #inhibitors, Antiviral Res.: https://www.sciencedirect.com/science/article/pii/S0166354224001682?via%3Dihub

Frequencies of markers of resistance to antivirals were low among >20,000 avian influenza A viruses studied. #H5Nx, #H7Nx, & #H9N2 viruses were susceptible to sub-nanomolar concentrations of antivirals. NA-I222M, but not NA-S246N or NA-I222V, in H5N1 confers reduced inhibition by #oseltamivir.

#Genotypic & #phenotypic susceptibility of emerging avian #influenza A viruses to
#NAIs & cap-dependent endonuclease #inhibitors, Antiviral Res.: https://www.sciencedirect.com/science/article/pii/S0166354224001682?via%3Dihub

Frequencies of markers of resistance to antivirals were low among >20,000 avian influenza A viruses studied. #H5Nx, #H7Nx, & #H9N2 viruses were susceptible to sub-nanomolar concentrations of antivirals. NA-I222M, but not NA-S246N or NA-I222V, in H5N1 confers reduced inhibition by #oseltamivir.

#Avian #Influenza A(#H5N1) #US #Situation #Update and CDC Activities: One Virus Isolated from #Cow showed reduce #sensitivity to #neuraminidase #inhibitors, https://www.cdc.gov/flu/avianflu/spotlights/2023-2024/avian-situation-update.htm

CDC found one virus from a cow with a marker known to be associated with reduced susceptibility to the neuraminidase inhibitors (a change at NA-T438I). This change has been seen rarely in the past in H5N1 viruses isolated from wild birds and poultry.

#Structure-based #discovery of dual #pathway #inhibitors for #SARS-CoV-2 entry https://www.nature.com/articles/s41467-023-42527-5

Lindsay Hohsfield will talk about "Using #CSF1R #inhibitors to uncover #myeloid cell trafficking routes into the #CNS"

⏰ September 11th, 2023, 12 pm
📍 @dzne

#Neuroscience

My second scifi submission for Vol 14. This is also based on the writting of Alastair Reynolds, this time it is "The Last Stand of John the Revelator", from his book Inhibitor Phase.

As with the last one, a mix of Blender, C4d with Octane and Photoshop. Also used Embergen for the explosions.

#SciFi #ScienceFiction #Space #spaceship #RevelationSpace #Lighthugger #inhibitors #AlastairReynolds #ArtOnMastodon #MastoArt #illustration #ArtByAlastairTemple #3d #blender3d #Cinema4D

Identification of #SARS-CoV-2 #Mpro #inhibitors containing P1’ 4-fluorobenzothiazole moiety highly active against SARS-CoV-2 https://www.nature.com/articles/s41467-023-36729-0

A widely-used class of #antidepressants, particularly for persistent or severe cases, is selective #serotonin reuptake #inhibitors (#SSRIs). These drugs target serotonin, a #chemical that carries messages between nerve cells in the brain and has been dubbed the ‘pleasure chemical’.
#Depression #Psychiatry #Neuroscience #sflorg
https://www.sflorg.com/2023/01/psyc01232301.html

A nice overview on #PCSK9 #inhibitors and related #medchem opportunities.
https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.2c01290

As appendix to my #Introduction and catalyst for possible collaborations in the field, I would like to #boost our recent #DrugDiscovery effort in the modulation of the #CCL20/#CCR6 axis to identify new #inhibitors for #IBD and other #diseases depending on the same axis.

https://www.sciencedirect.com/science/article/abs/pii/S0223523422006055