Dr.rabia's Article in Medicine

939 Ly294002 in PI3K inhibitor
Ly294002 is such an important PI3K inhibitor. Today, I would look back the classic article to review some information. The article “A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4- morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002)” provides much important information.The article was published on the journal of biological chemistry in 1994.
Posted on Feb-03-2012

663 AR-42 FUNCTIONS AGAINST NEUROFIBROMATOSIS TYPE 2
Histone deacetylases is the name given to the enzymes responsible of catalyzing the removal of acetyl groups attached to lysine residues. These histone deacetylases have ability of increases the condensation of chromatin material and represses the transcription process. Including this these histone deacetylases causes epigenetic silencing.
Posted on Jan-20-2012

565 Compound libraries provide a variety of compounds which can be used to induce or inhibit apoptosis
It is the beauty of nature that it keeps a check on each and every reaction taking place within us. There is a discipline not only in the creation of newer entities but there is also decency in the destruction of older ones when not required. The programmed destruction of cells is called as apoptosis.
Posted on Jan-18-2012

571 Role of PD0325901 in MEK1/2, kinase inhibitor, compound libraries
Various mutations are mainly the cause cancer or tumor growth. A good number of pathways have been studied so far in order understand the mechanism of cancer growth and proliferation. Among these pathways the most important one is the Ras originated and to downstream Raf-MEK1/MEK2-ERK1/ERK2.
Posted on Jan-18-2012

702 Test of signaling pathways in cervical cancer
In this poster, I would introduce a new article published in cancer research and I wanna to recommend a way to discovery the relationship between gene expression and cancer in vivo. Researchers in this article just gave an example and we could do more study in similar way in future.
Posted on Jan-16-2012

731 Target focused compound libraries are based on the designing of inhibitors
Presently a wide range of approaches are available for the high throughput screening of compound libraries. Broadly the screening may be target oriented or diversity oriented screening. The high cost of screening whit lesser chances of successful hits is the main bottleneck in exponential rate of screening. Target focused approach eases this bottleneck to a greater extent.
Posted on Jan-16-2012

822 In VX-745is the p38 it is responsible for the stimulation of various inflammatory responses
There are good numbers of intracellular signaling pathways are activated in response to extracellular stimuli. Amongst all these important signaling pathways the MAPK (kinase of mitogen activated protein) is one of the vital pathways. In this it the p38 it is responsible for the stimulation of various inflammatory responses by activating the inflammatory mediators. Kinase inhibitors are very effective against the it pathway.
Posted on Jan-16-2012

3913 Study and research of Foretinib in Renal Cell Carcinoma
Foretinib, in advanced metastatic solid tumors. Foretinib was identified by high-throughput screening and rationally developed to act as both a proliferation inhibitor (Met) and an angiogenesis inhibitor (VEGFR) in order to test the hypothesis that antitumor activity could be combined in a single agent.
Posted on Jan-13-2012

803 Autodock as an example of Cloud Computing in HTS
High throughput screening technology is no more straight forward and conventional as it was in the early period of discovery. Since its discovery in 1990s’ a lot of modifications have been imparted to improve the parameters of HTS.
Posted on Jan-13-2012

777 Foretinib inhibits both Met and VEGFR in a balanced manner
The role of mesechymal-epithelial transition (Met) tyrosine kinase in various cancers has been discussed in previous posts. Briefly, Met is one of the most frequently dysregulated pathways in human cancers. Patients with constitutively active Met tend of have aggressive cancers that are resistant to chemotherapy and, therefore, carry poor prognoses.
Posted on Jan-12-2012

728 LAQ824 targets regulators of cell cycle and growth
HDAC inhibitors have great potential to destroy tumor and cancer cells. LAQ824 is one of HDAC inhibitors as different animal xenografts had depicted the role of this compound during various experiments. The mechanism of action is similar as in other such inhibitors. The LAQ824 arrest the growth of cell by cell cycle arrest or inducing apoptosis.
Posted on Jan-10-2012

735 Phosphorylation pathway of ERK5 is inhibited by BIX02189
ERK5 is an important MAPK family member. It must be in activated form for the proper growth and maintenance of the neuronal cells and tissues. Phosphorylation pathway of ERK5 is inhibited by BIX02189. And this BIX 02189 is an effective key to analyze the function of ERK5 and the pathways activated by it. Molecular size of ERK1/2 is half of the size of ERK5 indeed while the amino terminals of both are almost homologous.
Posted on Jan-09-2012

950 Entinostat performs almost similar functions as Belinostat and Panobinostat
Entinostat, is also known with different other names such as MS-275, SNDX-275 and MS-27-275. This compound is among HDAC inhibitors and is selective for HDAC1 and HDAC3. It performs almost similar functions as Belinostat and Panobinostat which are HDAC inhibitors. In human beings under in vivo conditions Entinostat is known to show a great anti tumor activity.
Posted on Jan-09-2012

1905 BIX 02188 FOR STEADY FLOW
A steady blood flow is the only case of prevention of atherosclerosis. A shear stress can cause the prevention of hardening of blood vessels. So when a shear stress is exerted by flow of fluid, it results in the in vivo prevention of atherosclerosis. Atherosclerosis leading to oxidative stress also accompanied with expression of VCAM1 increased inflammation.
Posted on Jan-09-2012

572 AR-42 (HDAC-42) in the inhibition of various cancer cells
AR-42 is a new histone deacetylase inhibitor like vorinostat which regulates apoptosis via different pathways. It affects different cell cycle stages leading to the inhibition of cell proliferation in an effective manner. Proteins like tubulin and histones are also affected by this inhibitor.
Posted on Jan-04-2012

610 CUDC-101 IS AN INHIBITOR WITH MULTIPLE TARGETS
CUDC-101 is a novel compound which inhibits multiple targets. The effect of this inhibitor is on variety of protein groups for example receptors of kinases, different growth factor receptors like EGFR and HER2, in tumor cells. This is an efficient inhibitor of both classes of HDACs (class I and II).
Posted on Jan-04-2012

410 Regorafenib inhibits multiple kinases and controls the process of angiogenesis efficiently
A tumor needs a continuous blood supply for its growth beyond 1-2mm in dimension. The process of angiogenesis is related with the development of new blood vessels from the older ones and this process maintains a constant supply of oxygen to the growing tumor. The members belonging to the VEGF family promote the process of angiogenesis.
Posted on Dec-23-2011

481 Development of High throughput screening technology
High throughput screening technology has played a key role in the development of inhibitors against particular targets via in vitro assays. However every inhibitor cannot be used directly as a drug.
Posted on Dec-23-2011

396 The process of HTS becomes useful only when the results of screening analysis are visualized
The key strategy of drug development in the contemporary era involves the screening of compound libraries. The process of HTS becomes useful only when the results of screening analysis are visualized. This visualization is accomplished by performing high quality HTS assays which employ certain radioactive, fluorescence or other biophysical methods to see the changes.
Posted on Dec-23-2011

721 ROLE OF BIX02188 IN THE STUDY OF ERK5
Being a potent inhibitor of ERK5 and MEK5, BIX02188 helped in the study of the effects of steady flow of blood. It also helped to prove that ERK5 is very essential for the growth of the neuronal tissues.
Posted on Nov-09-2011