One possibility is to cut off bacteria's nutrient supply by blocking essential metabolic pathways
with a small molecule inhibitor, essentially starving the bacteria to death.
Moreover, reducing tau acetylation
with a small molecule inhibitor leads to depletion of pathogenic phosphorylated - tau in neurons.
Not exact matches
«Our research and development team has made tremendous progress
with our portfolio of novel,
small molecule Naᵥ1.7
inhibitors for the treatment of acute and chronic pain,» said Stan Abel, President and Chief Executive Officer of SiteOne Therapeutics.
The authors also found that a novel
small molecule inhibitor of the salvage pathway enzyme deoxycytidine kinase blocked leukemia growth in mice in combination
with thymidine (to inhibit the de novo pathway).
Therefore, a novel therapeutic approach in inflammatory breast cancer could involve a combination of conventional chemotherapy
with small -
molecule inhibitors of the Cdk2 cell cycle kinase.
To do so, they treated melanoma cells
with a panel of
small molecules and identified JNJ - 7706621 (JNJ) as the best
inhibitor of cyclinB1 / cdk1.
Coincidentally, co-author Lawrence Shapiro, PhD, at Columbia, was building a crystal structure of cadherin - 11 and is now working
with Byers and Brenner to show how the
molecule binds to Celebrex and other
small molecule drug cadherin - 11
inhibitors.
Scanning electron micrograph of the coronary microvasculature of a mouse that has been treated
with a
small molecule tyrosine kinase
inhibitor of platelet - derived growth factor receptor beta.
Hu and his collaborator Juan R. Del Valle at the University of South Florida are developing novel
small molecule inhibitors against IRE - 1 to combat cancers associated
with high numbers of MDSCs.
This lab, in collaboration
with the lab of Ruben Shaw at the Salk Institute, recently identified SBI - 0206965, the first potent and selective
small molecule inhibitor of ULK1, a serine / threonine kinase that is a critical regulator of autophagy.
iTeos is now developing EOS200271 which is a synthetic,
small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1), which has demonstrated the same anti-tumour activity in multiple preclinical tumour models in combination
with immune checkpoint
inhibitors as competitors, but also has demonstrated superior brain penetration.
Application of high - throughput screening to identify a novel αIIb - specific
small -
molecule inhibitor of αIIbβ3 - mediated platelet interaction
with fibrinogen.
She remained in Sheffield to complete a PhD and short post-doc in the lab of Professor Beining Chen, primarily working to screen and characterise
small molecule inhibitors of anthrax toxins as part of a collaboration
with the Health Protection Agency at Porton Down.
UNC569, a novel
small molecule Mer
inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo.
Our group has 3 major goals: Develop novel therapeutic approaches based on centrosomal clustering To further develop our first prototype
inhibitors of centrosomal clustering preclinically and to establish a robust and specific high throughput
small molecule screen Discover key events in myeloma pathogenesis To investigate the pivotal transition from the pre-malignant, asymptomatic to malignant, symptomatic stages of plasma cell dyscrasias in order to understand the pathophysiology and thereby identify novel targets Translate
small molecule therapeutics from bench to clinical trials To evaluate novel agents in the preclinical setting and to initiate early phase clinical trials in hematologic malignancies
with focus on multiple myeloma
After completing his PhD, he moved to Northwestern University for a year as a Postdoctoral Scientist working
with small -
molecule inhibitors of Type III secretion in Pseudomonas aeruginosa.
He went on to a postdoctoral position
with Dr. Iwao Ojima evaluating anti-tubercular compound series that inhibit the cell division protein FtsZ and screening computationally designed
small molecule inhibitors of Botulinum neurotoxin.
The combined treatment of ActD
with leptomycin B, a
small molecule nuclear export
inhibitor, has been shown to successfully lead to the accumulation of transcriptionally active p53 in the nuclei of human papillomavirus positive cervical carcinoma cells, resulting in apoptosis of the cells [16].
«Scientists can now, at the click of a button and at a single online location, rapidly identify the biological and structural characteristics of an actual or potential drug target, find the genes and proteins that it interacts
with, assess its structural druggability and identify any
small molecule chemical
inhibitors.
The discovery of
small molecule regulators (activators or
inhibitors) of epigenetic modification enzymes provides researchers
with pharmacological tools
with which to investigate the biological consequences of chromatin modifications.
Abbreviations: Aβ, amyloid β - peptide; AD, Alzheimer's disease; ALS, amyotrophic lateral sclerosis; Ambra1, activating
molecule in Beclin -1-regulated autophagy; AMPK, AMP - activated protein kinase; APP, amyloid precursor protein; AR, androgen receptor; Atg, autophagy - related; AV, autophagic vacuole; Bcl, B - cell lymphoma; BH3, Bcl - 2 homology 3; CaMKKβ, Ca2 + - dependent protein kinase kinase β; CHMP2B, charged multivesicular body protein 2B; CMA, chaperone - mediated autophagy; 2 ′ 5 ′ ddA, 2 ′, 5 ′ - dideoxyadenosine; deptor, DEP - domain containing mTOR - interacting protein; DRPLA, dentatorubral pallidoluysian atrophy; 4E - BP1, translation initiation factor 4E - binding protein - 1; Epac, exchange protein directly activated by cAMP; ER, endoplasmic reticulum; ERK1 / 2, extracellular - signal - regulated kinase 1/2; ESCRT, endosomal sorting complex required for transport; FAD, familial AD; FDA, U.S. Food and Drug Administration; FIP200, focal adhesion kinase family - interacting protein of 200 kDa; FoxO3, forkhead box O3; FTD, frontotemporal dementia; FTD3, FTD linked to chromosome 3; GAP, GTPase - activating protein; GR, guanidine retinoid; GSK3, glycogen synthase kinase 3; HD, Huntington's disease; hiPSC, human induced pluripotent stem cell; hVps, mammalian vacuolar protein sorting homologue; IKK,
inhibitor of nuclear factor κB kinase; IMPase, inositol monophosphatase; IP3R, Ins (1,4,5) P3 receptor; I1R, imidazoline - 1 receptor; JNK1, c - Jun N - terminal kinase 1; LC3, light chain 3; LD, Lafora disease; L - NAME, NG - nitro - L - arginine methyl ester; LRRK2, leucine - rich repeat kinase 2; MIPS, myo - inositol -1-phosphate synthase; mLST8, mammalian lethal
with SEC13 protein 8; MND, motor neuron disease; mTOR, mammalian target of rapamycin; mTORC, mTOR complex; MVB, multivesicular body; NAC, N - acetylcysteine; NBR1, neighbour of BRCA1 gene 1; NOS, nitric oxide synthase; p70S6K, ribosomal protein S6 kinase - 1; PD, Parkinson's disease; PDK1, phosphoinositide - dependent kinase 1; PE, phosphatidylethanolamine; PI3K, phosphoinositide 3 - kinase; PI3KC1a, class Ia PI3K; PI3KC3, class III PI3K; PI3KK, PI3K - related protein kinase; PINK1, PTEN - induced kinase 1; PKA, protein kinase A; PLC, phospholipase C; polyQ, polyglutamine; PS, presenilin; PTEN, phosphatase and tensin homologue deleted from chromosome 10; Rag, Ras - related GTP - binding protein; raptor, regulatory - associated protein of mTOR; Rheb, Ras homologue enriched in brain; rictor, rapamycin - insensitive companion of mTOR; SBMA, spinobulbar muscular atrophy; SCA, spinocerebellar ataxia; SLC, solute carrier; SMER,
small -
molecule enhancer of rapamycin; SMIR,
small -
molecule inhibitor of rapamycin; SNARE, N - ethylmaleimide - sensitive factor - attachment protein receptor; SOD1, copper / zinc superoxide dismutase 1; TFEB, transcription factor EB; TOR, target of rapamycin; TSC, tuberous sclerosis complex; ULK1, UNC -51-like kinase 1; UVRAG, UV irradiation resistance - associated gene; VAMP, vesicle - associated membrane protein; v - ATPase, vacuolar H + - ATPase; Vps, vacuolar protein sorting
This preclinical work led to the development of a novel anti-androgen ARN - 509, a
small -
molecule inhibitor discovered in collaboration
with UCLA chemist Michael Jung, which targets the increased levels of androgen receptor found in hormone - refractory disease.
Unfortunately, not every gene product can be targeted
with conventional
small molecule inhibitors.
More recently, the team published the structure of Eis in complex
with two potent
inhibitors they'd discovered using high - throughput screening of approximately 123,000
small molecules.