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*  Hutchison Medi Pharma | Pipeline Overview
Moreover, other drug development companies have tried to design small molecule Syk inhibitors for the treatment of chronic ... HMPL-523 is a potent and highly selective oral inhibitor specifically designed to overcome these off-target toxicity issues. We ... However, designing an efficacious and safe Syk inhibitor for a major chronic disease has proven to be exceptionally difficult ... We also expect HMPL-689 will have low risk of drug accumulation and drug-to-drug interaction. Given this, we believe that HMPL- ...
  http://www.hmplglobal.com/en/pipeline-overview/
*  In vitro evaluation of functional interaction of integrin αvβ3 and matrix metalloprotease-2
Design and Therapeutic Application of Matrix Metalloproteinase Inhibitors. Chem. Rev. 1999;99(9):2735-2776. [PubMed] ... Therapeutic strategies can be small molecule drugs, macromolecular drugs, prodrugs, or drug delivery systems, and the knowledge ... specifically MMP-2, to activate drugs have been investigated in recent years. MMP-2 has been utilized for designing prodrugs ... designed with fluorescent probes for monitoring peptide cleavage. MMP-RGD was bound to integrin αvβ3 with equal affinity ...
  http://pubmedcentralcanada.ca/pmcc/articles/PMC2790922/
*  Frontiers | Targeting protein-protein interactions in complexes organized by A kinase anchoring proteins | Pharmacology
Furthermore, development of novel classes of small molecules involved in displacement of AKAP-bound signal molecules is now ... Furthermore, development of novel classes of small molecules involved in displacement of AKAP-bound signal molecules is now ... Targeting AKAP coordinated protein complexes with high-affinity peptidomimetics or small molecules to tease apart distinct ... Targeting AKAP coordinated protein complexes with high-affinity peptidomimetics or small molecules to tease apart distinct ...
  https://www.frontiersin.org/articles/10.3389/fphar.2015.00192/full
*  Discovery and development of neuraminidase inhibitors - Wikipedia
... with rational structure-based drug design and can be categorized into four groups. Zanamivir analogues are designed to improve ... Nevertheless, most of the well studied vNEU inhibitors have shown very little affinity for hNEU except for the influenza drug ... are very similar with the exception of the glycerol side chain which offers some strategic options in designing inhibitors ... With better X-ray crystal structure a number of important residues in the active site were identified, specifically C4 hydroxyl ...
  https://en.wikipedia.org/wiki/Discovery_and_development_of_neuraminidase_inhibitors
*  An Integrated Computational and Experimental Binding Study Identifies the DNA Binding Domain as the Putative Binding Site of...
... is as a potential drug target for cancer and inflammation. Strategies to block STAT3 dimerization ha.. ... This new class of STAT3 inhibitors may serve as important drug leads or probes for the design and studies of STAT3 DNA-binding ... Although several STAT3 inhibitors have been hypothesized to bind in the STAT3 SH2 domain, the binding sites for small molecule ... Compounds with modifications of the R2 group were also designed to expand the structural diversity keeping drug-likeness in ...
  https://www.omicsonline.org/open-access/an-integrated-computational-and-experimental-binding-study-identifies-the-dna-binding-domain-as-the-putative-binding-site-of-novel-2169-0138-1000142.php?aid=86256
*  Protease-Activated Drug Development
... the peptide substrate was also used to design a DOX prodrug that can be specifically activated by MMP-2 [159]. ALB was ... Phase III trial comparing paclitaxel poliglumex vs docetaxel in the second-line treatment of non-small-cell lung cancer. Br J ... Analysis of the acute and chronic wound environments: The role of proteases and their inhibitors. Wound Repair Regen. 1999;7: ... Novel antitumor prodrugs designed for activation by matrix metalloproteinases-2 and -9. Mol Pharm. 2004;1:9-22 ...
  http://thno.org/v02p0156.htm
*  Protocols and Video Articles Authored by Peter Nagy (Translated to Norwegian)
Identification of Small Molecule Inhibitors of Tomato Bushy Stunt Virus Replication Methods in Molecular Biology (Clifton, N.J ... Favorable steric and electrostatic fit of a ligand to a receptor is of central interest in theoretical drug design. This paper ... This study was designed to find the missing disease-causing ABCA4 variation by a combination of next-generation sequencing (NGS ... Specifically, 2 × 10 mm samples for reproducing bottom-initiated radial fracture, complemented by 0.2 × 1 mm samples for ...
  https://www.jove.com/author/Peter_Nagy?language=Norwegian
*  Dimpy Kalia Research Group at the Department of Chemistry, Savitribai Phule Pune University
We are designing and testing rationally-designed libraries of small organic compounds as inhibitors of c-di-GMP signaling in ... and are therefore attractive scaffolds for drug design. We are developing facile routes for the synthesis of polysubstituted ... for cancer therapy wherein tumor marker-targeting antibody proteins are site-specifically conjugated to cytotoxic anticancer ... Indeed, the World Health Organization recently named drug-resistant bacteria as one of the top three global threats to human ...
  https://sites.google.com/site/dkaliagroup/
*  IJMS | Free Full-Text | Aptamers and Their Potential to Selectively Target Aspects of EGF, Wnt/β-Catenin and TGFβ-Smad Family...
Baines, I.C.; Colas, P. Peptide aptamers as guides for small-molecule drug discovery. Drug Discov. Today 2006, 11, 334-341. [ ... peptide aptamers specifically designed to bind the dimerization domain or the DNA-binding domain within Stat3 can abolish Stat3 ... Hong, C.C.; Yu, P.B. Applications of small molecule BMP inhibitors in physiology and disease. Cytokine Growth Factor Rev 2009, ... Unlike antibodies, peptide aptamers have a small size and a simple design, are in most cases independent of disulfide bonds, ...
  http://mdpi.com/1422-0067/14/4/6690/htm
*  JoVE | Peer Reviewed Scientific Video Journal - Methods and Protocols
Drug Design, optimization (mathematics), Amino Acids, Peptides, and Proteins, De novo protein and peptide design, Drug design, ... Unlike FRET, BiFC has little background fluorescence, little post processing of image data, does not require high ... and drug delivery. Designing materials based on the molecular-scale interactions between these proteins will help generate new ... A rank-ordered list of the sequences for each step of the process, along with relevant designed structures, provides the user ...
  https://www.jove.com/visualize/abstract/22509312/reduced-polymorphism-domains-involved-protein-protein
*  JoVE | Peer Reviewed Scientific Video Journal - Methods and Protocols
Local application of electric pulses to the tumour increases drug delivery into cells, specifically at the site of electric ... and drug delivery. Designing materials based on the molecular-scale interactions between these proteins will help generate new ... this tissue design can be applied to many organs other than heart with minimal design and material changes, and is meant to be ... Here, we present an example of integrated designs using layering of patterned cell sheets with two distinct types of biological ...
  https://www.jove.com/visualize/abstract/19956606/cross-species-genomic-analysis-identifies-mouse-model-as
*  会议日程 - 2015年PEGS蛋白与抗体研发工程峰会
10:00 Design and Develop Next-Generation Bispecific Antibodies with Good Drug Like Properties (DLP). Jinming Gu, Ph.D., Senior ... in which monoclonal antibodies are designed to deliver a cytotoxic drug selectively to antigen expressing cells. The site- ... 5:10 Designing and Engineering Novel Bispecific/Bifunctional Antibodies and Fusion Proteins for Enhanced Antitumor Activity. ... 1:50 Exceptionally Potent and Broad Inhibitors of HIV-1 based on Antibody Domains and One Domain Soluble CD4 Multivalent Fusion ...
  http://www.echinachem.com/events/PEGS/agenda.html
*  Renal Cancer Stem Cells: Characterization and Targeted Therapies
developed a drug delivery system which targets specifically gastric CSCs [118]. Indeed, chitosan-coated single wall carbon ... Drug Design, Development and Therapy, vol. 10, pp. 745-755, 2016. View at Publisher · View at Google Scholar ... "Treatment of triple-negative breast cancer with TORC1/2 inhibitors sustains a drug-resistant and notch-dependent cancer stem ... A series of innovative therapies aiming at eliminating CSCs have been designed to treat other types of cancer and have not been ...
  https://www.hindawi.com/journals/sci/2016/8342625/
*  Peptidomimetic - Wikipedia
A peptidomimetic is a small protein-like chain designed to mimic a peptide. They typically arise either from modification of an ... "Structure-based design of inhibitors of protein-protein interactions: Mimicking peptide binding epitopes". Angewandte Chemie ... In phage display, the DNA sequence that codes the potential drug-peptide is fusioned to the gene of the protein coat of ... In this case, a stapled BH3 helix was identified which specifically activates the mitochondrial apoptotic pathway by ...
  https://en.wikipedia.org/wiki/Peptidomimetic
*  Drug design - Wikipedia
Another important case study in rational drug design is imatinib, a tyrosine kinase inhibitor designed specifically for the bcr ... Small molecules (for example receptor agonists, antagonists, inverse agonists, or modulators; enzyme activators or inhibitors; ... Structure-based drug design attempts to use the structure of proteins as a basis for designing new ligands by applying the ... The first is referred to as ligand-based drug design and the second, structure-based drug design. Ligand-based drug design (or ...
  https://en.wikipedia.org/wiki/Drug_design
*  Antiviral drug - Wikipedia
... or by actually designing the candidate at the molecular level with a computer-aided design program. The target proteins can be ... Improved protease inhibitors are now in development. Protease inhibitors have also been seen in nature. A protease inhibitor ... Most of the antiviral drugs now available are designed to help deal with HIV, herpes viruses, the hepatitis B and C viruses, ... These small-molecule drugs target host-regulated processes involved in viral replication. ... A new dosage formulation of ...
  https://en.wikipedia.org/wiki/Antiviral_drug
*  Ram Samudrala - Wikipedia
... and drug repurposing in a shotgun manner, as well as in nanobiotechnology, such as engineering tooth tissue by designing novel ... where small multifunctional peptides that bind to inorganic substrates are designed computationally; and interactomics of ... Specifically, on a more grounded level, he has consistently taken part in, spoken at, and published in the proceedings of blind ... The NRW project harnessed the power of individual PCs via the Grid to perform its computations to help design better rice ...
  https://en.wikipedia.org/wiki/Ram_Samudrala
*  Discovery and development of direct Xa inhibitors - Wikipedia
To accomplish that, this part of the molecules is designed to have little formal interactions with FXa in that region. As there ... Other Xa inhibitors advantages are rapid onset/offset, few drug interactions and predictable pharmacokinetics. The rapid onset/ ... An important part of designing a compound, that is an ideal inhibitor to a certain target, is to understand the amino acid ... It is defined as the formation of insoluble fibrin by activated coagulation factors, specifically thrombin. These factors ...
  https://en.wikipedia.org/wiki/Discovery_and_development_of_direct_Xa_inhibitors
*  Ketogenic diet - Wikipedia
A small amount of MCT oil may be used to help with constipation or to increase ketosis. The classic ketogenic diet is not a ... In an attempt to control for this bias, modern study design prefers a prospective cohort (the patients in the study are chosen ... About 60% of patients will achieve control of their epilepsy with the first drug they use, whereas about 30% do not achieve ... In older protocols, the diet was initiated with a prolonged fast, designed to lose 5-10% body weight, and heavily restricted ...
  https://en.wikipedia.org/wiki/Ketogenic_diet
*  Optogenetics - Wikipedia
2016). "Optogenetics design of mechanistically-based stimulation patterns for cardiac defibrillation". Sci Rep. 6. doi:10.1038/ ... Lungu, Oana I.; Hallett, Ryan A.; Choi, Eun Jung; Aiken, Mary J.; Hahn, Klaus M.; Kuhlman, Brian (2012-04-20). "Designing ... January 2011). "Light modulation of cellular cAMP by a small bacterial photoactivated adenylyl cyclase, bPAC, of the soil ... Indeed, optogenetics papers in 2009 have also provided insight into neural codes relevant to autism, Schizophrenia, drug abuse ...
  https://en.wikipedia.org/wiki/Optogenetics