iTeos has a broad pipeline focused on multiple complementary mechanisms of action including
small molecules targeting IDO1, A2A, and STING as well as antibodies directed to TIGIT and Galectin 3.
Traditional
small molecules targeting ARE - regulated gene activation (e.g., bardoxolone, dimethyl fumarate) function by alkylating numerous proteins including Keap1, the controlling protein of Nrf2.
Bicyclams were the first class of non-peptidic
small molecules targeting CXCR4.
Not exact matches
SOUTH SAN FRANCISCO, CA — July 25, 2017 — Kezar Life Sciences, a private, clinical - stage biopharmaceutical company developing novel
small molecule therapeutics
targeting the immunoproteasome and the protein secretion pathway, announced today that it has closed an oversubscribed Series B investment round of $ 50 million led by Cormorant Asset Management and Morningside Venture.
The Company focuses on discovering and developing
small molecule drugs directed against tumor and immune cell
targets that control key metabolic pathways in the tumor microenvironment.
«From a translational perspective, we are interested in developing antibodies or
small molecules to
target this protein late in life,» said Villeda.
The new research, published recently as two separate studies in ACS Central Science and the Journal of the American Chemical Society, demonstrates that a new class of drugs called
small molecule RNA inhibitors can successfully
target and kill specific types of cancer.
«When
small molecules are administered, they can stick to many different proteins in the body because their size enables them to interact with many
targets, not just the intended
target, causing more side effects.»
«The next step is to identify antibodies and
small -
molecule drugs that can successfully
target Helios or genes in the Helios pathway,» says the study's lead author, Hye - Jung Kim, PhD, of Dana - Farber.
There are already some
small -
molecule compounds that
target circadian pathways, Liu said, but the drugs need to be delivered to the site.
Initial results were discouraging: attempts to simply replace the protein therapies with
small -
molecule drugs that hit the same
targets largely failed, says Saeed Fatenejad, a rheumatologist at Pfizer who is responsible for clinical development of tasocitinib.
Nanotechnology has unlocked new pathways for
targeted drug delivery, including the use of nanocarriers, or capsules, that can transport cargoes of
small -
molecule therapeutics to specific locations in the body.
«Our ultimate goal is to reduce melanoma mortality through the discovery of effective and
targeted small molecules for melanoma treatment.
«
Small molecule inhibitor shows promise in precision cancer
targeting.»
As
target depth increases, the single - scattered signal (red) becomes negligibly
small, because it is more likely that the waves will get bounced around by other biological
molecules in their path (blue).
Moreover,
small amounts of singlet oxygen produced during metabolic reactions can act as a local signaling factor that oxidizes and modifies
target molecules, but the underlying mechanisms are poorly understood.
These are used to identify protein - protein interactions, to identify the substrates of protein kinases, or to identify the
targets of biologically active
small molecules.
Previous studies have shown that a
small molecule known as ONC201 currently in advanced cancer clinical trials,
targets self - renewing colorectal cancer stem cells.
These
small molecules, which have previously been developed by the researchers, bind to a specific
target protein.
«But at the same time, we are also developing a therapeutic antibody
targeting annexin A2, and we are looking for a
small molecule that would inhibit Sema3D.»
Basic research on cancer mechanisms has led to over 40
targeted cancer therapies currently on the market, which take the form of monoclonal antibodies,
small molecule drugs, and immunotherapies.
turned into 10 years of systematic research to identify the enzyme PLK4 as a promising therapeutic
target and develop a
small molecule inhibitor to block it,» says Dr. Mak, Director of The Campbell Family Institute for Breast Cancer Research at the Princess Margaret Cancer Centre, University Health Network.
The new method gives scientists more power not only to find new antibody - based therapies, but also to discover the biological pathways through which they work — pathways that may turn out to be more easily and cheaply
targeted by
small -
molecule drugs.
In principle, if further tests bear out the protective effects of the two antibodies, then optimized versions of them, or
small -
molecule drugs that hit the same
target, could be developed as treatments for rhinovirus infections.
It contains two essential parts, a
small RNA
molecule called a microRNA (miRNA) which guides RISC to its mRNA
target; and a much larger component into which the guide RNA fits, a protein called Argonaute, which, Joshua - Tor showed in 2004, actually performs the «slicing up» of the mRNA.
King believes that venom - based peptides — short chains of amino acids — are better at being selective than
small molecules because the venom peptides don't
target the pore; they
target a specific sodium channel switch.
Certain ligases, like Fbxl3, can be
targeted with
small molecules.
A new class of experimental drug - like
small molecules is showing great promise in
targeting a brain enzyme to prevent early memory loss in Alzheimer's disease, according to Northwestern Medicine ® research.
However, some
small molecule drugs can cross this barrier and form the basis of
targeted therapies.
«Together, our findings indicate that these molecular regulators, TRIP - Br2 and GATA3, could be viable
targets for
small drug
molecules that could serve as potential therapeutic agents against obesity,» Liew said.
«Traditionally, scientists have theorized fairly narrow limits on which proteins can be
targeted with
small -
molecule ligands, but our results suggest that those boundaries are much wider,» said Cravatt.
Today in PLOS Pathogens, scientists report that they've designed
small molecules to
target a particularly vulnerable region of hemagglutinin, one of the two proteins that jut from the viral surface like a flower.
His lab is designing
small peptides that
target the seeds and mimic regions of «chaperone»
molecules, which usually bind to proteins and help them to fold correctly.
The
target is a
small molecule called homocysteine.
The novel thyroid and parathyroid contrast agents differ significantly from most current NIR contrast agents, which are composed of two separate
molecules linked together: a
molecule that emits a fluorescent signal, called the fluorophore, and an antibody or
small molecule that
targets the tissue of interest.
Through the combination of CRISPRs and RNA - guided endonucleases, such as Cas9, («Cas» stands for CRISPR - associated), bacteria are able to utilize
small customized crRNA
molecules (for CRISPR RNA) to guide the
targeting and degradation of matching DNA sequences in invading viruses and plasmids to prevent them from replicating.
The process of drug discovery has been dominated in recent years by the screening of large libraries of structurally diverse
small molecules for effects on
target proteins associated with disease.
By focusing the light, researchers can
target the release of their caged
molecule in a very
small volume — roughly a cubic micron.
Small molecule MYC inhibitor conjugated to integrin -
targeted nanoparticles extends survival in a mouse model of disseminated multiple myeloma.
One of the gene's molecular
targets, for example, is a microRNA (a
small noncoding RNA
molecule) called let7, which in turn regulates hundreds of other genes, so the effects of Lin28a can set off a complex array of regulatory interactions.
It's still early days, but researchers report that they've discovered a new
small molecule that binds selectively to a long -
targeted enzyme, halting its role in pain and addiction while not interfering with enzymes critical to healthy cell function.
In the current, sixth, blind test, there were five
targets, including a
small semi-rigid
molecule, a medium sized flexible
molecule with five known polymorphs, a hydrated Chloride salt, a co-crystal and a large flexible
molecule.
Ideally, an approach to
target CXCR4 would complement CCR5 - specific therapy, but the broad expression pattern of CXCR4 has made systemic inhibition of this coreceptor by
small molecules problematic [10], [11].
Target - based strategies typically employ in vitro high - throughput screening methods to identify
small molecules that alter the activity of an identified candidate protein implicated in a disease process.
Moreover, protein - protein interactions can be directly
targeted with
small molecules.
Arguably, the most economical and efficient strategy for development of
small molecules with regenerative medicine applications is to use non-mammalian animal models for both
target - and phenotype - based drug discovery.
PTC and Roche are old friends and signed an agreement in September 2009 to develop orally bioavailable
small molecules using PTC's GEMS technology, focusing initially on four CNS disease
targets.
SOUTH PLAINFIELD, NJ — December 6, 2007 — PTC Therapeutics, Inc. (PTC), a biopharmaceutical company focused on the discovery, development, and commercialization of
small -
molecule drugs
targeting post-transcriptional control mechanisms, today announced an expanded research collaboration with the Spinal Muscular Atrophy (SMA) Foundation.
We also develop in silico chemogenomic approaches to analyze jointly the chemical space of
small molecules and biological space of protein
targets, leading in particular to efficacy profile and secondary effect prediction.
Second is the lack of understanding of the detailed molecular mechanisms of regeneration and thus the lack of identified proteins that can be
targeted with
small molecules.