The aim of the 6th RSC-BMCS Fragment-based Drug Discovery meeting will be to continue the focus on case studies in Fragment-based Drug Discovery that have delivered compounds to late stage medicinal chemistry, preclinical or clinical programmes. The Fragment series was started in 2007 and continues with the theme, having over three-quarters of the presentations focused on case studies. The conference will include successful examples from all types of fragment-based approaches, including high concentration, NMR, SPR and X-ray screening ...
TY - CHAP. T1 - Fragment-based drug discovery in academia. T2 - Experiences from a tuberculosis programme. AU - Heikkila, T.J.. AU - Surade, S.. AU - Silvestre, H.L.. AU - Dias, M.V.B.. AU - Ciulli, A.. AU - Bromfield, K.. AU - Scott, D.. AU - Howard, N.. AU - Wen, S.. AU - Wei, A.H.. AU - Osborne, D.. AU - Abell, C.. AU - Blundell, T.L.. PY - 2009. Y1 - 2009. N2 - The problems associated with neglected diseases are often compounded by increasing incidence of antibiotic resistance. Patient negligence and abuse of antibiotics has lead to explosive growth in cases of tuberculosis, with some M. tuberculosis strains becoming virtually untreatable. Structure-based drug development is viewed as cost-effective and time-consuming method for discovery and development of hits to lead compounds. In this review we will discuss the suitability of fragment-based methods for developing new chemotherapeutics against neglected diseases, providing examples from our tuberculosis programme.. AB - The problems ...
http://www.transparencymarketresearch.com/pressrelease/fragment-based-drug-discovery-market.htm. Fragment screening services and fragment optimization collectively form the fragment-based drug discovery market. Fragment screening segment was further segmented into biophysical services and non-biophysical services. Biophysical services are further segmented into techniques such as Nuclear Magnetic Resonance (NMR) Spectroscopy, Differential scanning Fluorimetry (DSF) Assay (Thermal Shift), Fluorescence Polarization (FP), Isothermal Titration Calorimetry (ITC), X-ray Crystallography, Surface Plasmon Resonance, Biolayer Interferometry, Mass Spectrometry, Capillary Electrophoresis, and others (biochemical assays). NMR was the largest segment of the FBDD market, accounting for approximately 19.7% share in 2014. The technique is expected to maintain its leadership position during the forecast period. Advantages of NMR such as high reliability, easy operability, and wide versatility are likely to fuel ...
D. A. Erlanson Introduction to Fragment-Based Drug Discovery T. G. Davies Ian J. Tickle Fragment Screening Using X-Ray Crystallography S. Roughley L. Wright P. Brough A. Massey R. E. Hubbard Hsp90 Inh
BALTIMORE, June 30, 2017 /PRNewswire/ -- AgeneBio Receives Grant from Alzheimers Drug Discovery Foundation for Drug-Discovery Program to Delay the Onset of Alzheimers Dementia. Novel GABA-A program targets hippocampal overactivity that leads to neurodegeneration and cognitive decline in Alzheimers disease patients.
Fragment-based drug discovery is an emerging process that has gained popularity in recent years. The process starts from small molecules called fragments. One major step in fragment-based drug discovery is fragment screening, which is a strategy to screen libraries of small molecules to find hits. The strategy in theory is more efficient than traditional high-throughput screening that works with larger molecules. As fragments intrinsically possess weak affinity to a target, detection techniques of high sensitivity to affinity are required for fragment screening. Furthermore, the use of different screening methods is necessary to improve the likelihood of success in finding suitable fragments. Since no single method can work for all types of screening, there is a demand for new techniques. The aim of this thesis is to introduce weak affinity chromatography (WAC) as a novel technique for fragment screening.. WAC is, as the name suggests, an affinity-based liquid chromatographic technique that ...
The conjugation of the small ubiquitin-like modifier (SUMO) to protein substrates is an important post-translational modification that has ramifications for cancer and other diseases. As the sole E2 enzyme in the tightly regulated E1/E2/E3 SUMOylation enzymatic cascade, Ubc9 plays a central role in the conjugation of all three SUMO isoforms to a variety of protein targets. Although Ubc9 is viewed as a promising anti-cancer drug target, the development of small-molecule Ubc9 inhibitors has proven to be very difficult. In the past decade, fragment-based drug design has emerged as a powerful approach to identify ligands for challenging protein targets that can provide excellent starting points for the development of potent inhibitors. By X-ray crystallographic fragment screening, we have identified two small-molecule fragments that bind to Ubc9 at a location that is distal from its active site. Although these fragments have weak affinity for Ubc9, biochemical assays have confirmed that they inhibit ...
REVISED APPLICATION RECEIPT DATE: NATIONAL COOPERATIVE DRUG DISCOVERY RESEARCH ON OPPORTUNISTIC INFECTIONS Release Date: October 8, 1998 PA NUMBER: PA-98-100 P.T. National Institute of Allergy and Infectious Diseases National Cancer Institute Application Receipt Date: January 20, 1999 PURPOSE PA-98-100, NATIONAL COOPERATIVE DRUG DISCOVERY RESEARCH ON OPPORTUNISTIC INFECTIONS, appeared in the NIH Guide on August 25, 1998. The application receipt date in that program announcement was November 19, 1998. In order to provide applicants with more time to prepare their applications for research project (R01) grants, the receipt date for applications has been extended to January 20, 1999. INQUIRIES Written and telephone inquiries are encouraged. The opportunity to clarify any issues or questions from potential applicants is welcome. Barbara Laughon, Ph.D. Division of AIDS National Institute of Allergy and Infectious Diseases 6003 Executive Boulevard, Room 2C26 - MSC 7620 Bethesda, MD 20892-7620 ...
World Congress on Drug discovery & Development -2016, Indian Institute of Science, Jul 18-20, 2016, Bangalore, Karnataka. Browse other events at Indian Institute of Science, Bangalore
High-throughput screening remains one of the most powerful, unbiased approaches for small molecule drug discovery.. Today, the toolbox for high-throughput screening features traditional label-dependent approaches and novel label-free technologies. Researchers determine which methodology offers the most promising path forward for their target, taking into account assay sensitivity, data quality, costs, and speed. Moreover, many companies opt to outsource drug discovery efforts to contract research organizations, which offer a particular expertise and an established discovery infrastructure to lead hit identification and hit-to-lead programs.. In this white paper, we discuss important aspects to consider when choosing a methodology for drug discovery. ...
After 20 years of sometimes quiet growth, fragment-based drug discovery (FBDD) has become mainstream. More than 30 drug candidates derived from fragments have entered the clinic, with two approved and several more in advanced trials. FBDD has been widely applied in both academia and industry, as evi …
The reason for the low number of successful new CNS drugs is the subject of debate, although it is undoubtedly related to their higher attrition rate during development, particularly from issues related to failures of on-target biological hypotheses. To address this problem, there has been a recent emphasis on research to tackle these issues at an earlier stage in the drug discovery pathway. In particular, there has been increased interest in target discovery both for the identification of novel targets and reducing the subsequent failure from incorrect biological hypotheses through early validation.. Target discovery, which involves the identification and early validation of disease-modifying targets, is an essential first step in the drug discovery process. Furthermore, although the knowledge of the target for a small molecule drug is not required by the FDA for drug development, it is crucial information if the drug discovery process is to be made more efficient and effective. Identifying the ...
TY - JOUR. T1 - Semantic text mining in early drug discovery for type 2 diabetes. AU - Hansson, Lena K.. AU - Hansen, Rasmus Borup. AU - Pletscher-Frankild, Sune. AU - Berzins, Rudolfs. AU - Hansen, Daniel Hvidberg. AU - Madsen, Dennis. AU - Christensen, Sten B.. AU - Revsbech Christiansen, Malene. AU - Boulund, Ulrika. AU - Wolf, Xenia Asbæk. AU - Kjærulff, Sonny Kim. AU - van de Bunt, Martijn. AU - Tulin, Søren. AU - Jensen, Thomas Skøt. AU - Wernersson, Rasmus. AU - Jensen, Jan Nygaard. PY - 2020. Y1 - 2020. N2 - BACKGROUND: Surveying the scientific literature is an important part of early drug discovery; and with the ever-increasing amount of biomedical publications it is imperative to focus on the most interesting articles. Here we present a project that highlights new understanding (e.g. recently discovered modes of action) and identifies potential drug targets, via a novel, data-driven text mining approach to score type 2 diabetes (T2D) relevance. We focused on monitoring trends and ...
Jim Wells (UCSF) gave a magisterial keynote address that emphasized how useful fragments can be for tackling difficult targets such as protein-protein interactions (PPIs). In fact, many of the talks in the protein-protein interaction track relied on fragments. Thats not to say its easy. Rod Hubbard (University of York and Vernalis) emphasized that advancing fragments to leads against such targets can take a long time and often requires patience that strains the management of many organizations. Fragment hits against PPIs usually have lower ligand efficiencies (0.23-0.25 kcal/mol/HA if youre lucky), and improving potency can be a bear. Rhian Holvey (University of Cambridge) presented a nice example of how she was able to find millimolar fragments that bind to the anti-mitotic target TPX2, potentially blocking its interaction with importin-alpha, but even structural information was not enough to get to potent inhibitors ...
One theme throughout the conference was the observation that fragments bind at multiple sites on proteins. Harren noted that Astex researchers have found fragments bound (crystallographically) to 54 sites on 25 targets - an average of 2.2 sites per target. Some targets are even more site-rich: Joe Patel (AstraZeneca) performed a crystallographic screen on a complex of Ras and SOS and found four binding sites, including one previously discussed here. In this effort, 1200 fragments were screened in pools of 4, and in one case two fragments from the same pool each bound only when they were both present at the same time - each fragment alone showed no binding by NMR or crystallography ...
The Selcia Fragment Library is available in conjunction with its CEfrag™ screening service and consists of approximately 1400 compounds.
Chris is a leader in pharmaceutical research with expertise in fragment-based drug discovery, structure-based drug design, target analysis, kinases, phosphodiesterases, nuclear hormone receptors, and proteases. In his current role, as Associate Director of Structural Biology at Astra Zeneca, he is leading a team of scientists supporting pipeline projects with structural insights.. In his previous role as a senior principal scientist at Pfizer for over 13 years, he developed the core capabilities in macromolecular crystallography with emphasis on the application of structural information in the drug discovery process. Chris acquired a D. Phil in macromolecular crystallography and was also a postdoctoral research associate at the University of Oxford.. Chris has been an enthusiastic contributor and strong supporter of the Cambridge Pharmaceutical Consortium. The consortium has brought together pharmaceutical companies, the University of Cambridge, the Medical Research Councils Laboratory of ...
ZoBio offers Fragment-Based Drug Discovery research services on a fee-for-service basis to customers across the pharmaceutical & biotechnology industries.
ZoBio offers Fragment-Based Drug Discovery research services on a fee-for-service basis to customers across the pharmaceutical & biotechnology industries.
In 2009, the same development team created Adam, a robot scientist that became the first machine to independently discover new scientific knowledge. They used the knowledge from that experiment to create Eve with the purpose of speeding up the drug discovery process and make it more economical. In the published study, the researchers discuss describe how the robot is able to identify promising new drug candidates for malaria and other neglected tropical diseases, such as African sleeping sickness and Chagas disease.. Neglected tropical diseases are a scourge of humanity, infecting hundreds of millions of people, and killing millions of people every year, said Steve Oliver, a professor from the Cambridge Systems Biology Centre and the Department of Biochemistry at the University of Cambridge. We know what causes these diseases and that we can, in theory, attack the parasites that cause them using small molecule drugs. But the cost and speed of drug discovery and the economic return make them ...
Novartis Institutes for BioMedical Research, Cambridge, USA. Affinity proteomics and target identification for small molecule drug candidates. Affinity proteomics has become a valuable tool in preclinical small molecule drug discovery, in particular in the context of target identification and elucidation of the mechanism of action for drug candidates from phenotypic and pathway-centric approaches to drug discovery. Quantitative chemoproteomics, employing variations of a competition-based approach to small molecule affinity chromatography and mass spectrometry-based protein identification and quantitation, identifies cellular protein interactors and thus potential targets of drug candidates under conditions approximating the disease-relevant in vivo situation. Several examples will be presented and discussed in the context of orthogonal approaches to the generation of target hypotheses. On the other hand, the identification of protein-protein interactions using e.g. an affinity-tagged bait ...
The University of Michigan Center for the Discovery of New Medicines has awarded early-stage funding for seven new drug discovery projects by faculty from across U-M. Six of the projects focus on treating disease including heart failure, runaway cell division in cancer, hypertension, Crohns disease, a genetic heart disorder and neurological damage. The deadline for the next round of grant proposals is April 20. Learn more and apply.
By Rich Soll, SVP of Research Service Division at WuXi AppTec (@richsollwx). From developing new paradigms for early-stage drug discovery for rare and common diseases to fostering the convergence of peptide nanotechnology, and launching scientific experiments in space, Israeli biochemist Ehud Gazit is wearing many hats these days.. In his role as academic director at the newly-formed Blavatnik Center for Drug Discovery (BCDD) at Tel Aviv University in Israel, Gazit is leading efforts to provide the missing link that may enable many scientific discoveries to evolve into beneficial drugs. The Center is uniquely dedicated to translational science by helping researchers turn their discoveries into effective pharmaceuticals.. Gazit - also a biophysicist and nanotechnologist - stays active in his university lab, which explores biological and bio-inspired molecular self-assembly. The lab studies the organization of biological systems in diverse fields, including amyloid diseases, diabetes, virology, ...
Drug Discovery Today is a review journal, published as monthly 12 double issues. The journal covers the whole of the preclinical drug discovery process, from target identification and validation, through hit identification, lead identification and optimisation, though to candidate selection. The reviews are at the cutting edge of the science underpinning drug discovery, written by experts in their respective fields and cover all aspects of drug discovery from state-of-the-art genomic and proteomic approaches to target identification, through the most innovative computational approaches drug design, the science driving medicinal chemistry and the translation of these sciences to therapies
3rd Drug Discovery Re-Invented Conference is organized between 21 Feb and 24 Feb 2017. The Conference venue is Fiesta Americana Condesa in Cancun, Mexico. It will be a trend-setting Conference, illustrious as one of the most inventive meetings within the Medical, Pharmacology, Pharmaceutical, Drug Development, Biotechnology, Biosciences and Natural Products aspects. 3rd Drug Discovery Re-Invented Conference is once Conference. The organizer of the Drug Discovery Re-Invented 2017, 3rd Drug Discovery Re-Invented Conference is Fusion Conferences Limited. Let Cancun must do holiday attractions make you fall in love with this city when you are there for Drug Discovery Re-Invented 2017. Here are top notch things to do in Cancun ...
It aims to bring together leading academic researchers and research scholars to exchange and share their experiences and research results on all aspects of Drug Discovery, Designing and Development. It also provides a premier interdisciplinary platform for researchers, practitioners and educators to present and discuss the most recent innovations, trends, and concerns as well as practical challenges encountered and solutions adopted in the fields of Drug Discovery, Designing and Development ...
Scientists demonstrate new method of producing a specific class of organic compounds, which promises to accelerate drug discovery research for several diseases.. Several drugs, including those for depression, schizophrenia, and malaria, would not be if not for a type of organic chemical compound called alicyclic compounds. These compounds are 3D structures formed when three or more carbon atoms join in a ring via covalent bonds, but the ring is not aromatic.. Aromatic compounds (or arenes) are another class of organic compounds which are 2D structures with reactive properties distinct from those of alicyclic compounds. A well-known example is benzene, the six-carbon ring comprising alternating single- and double-bonds between the carbon atoms.. By dearomatizing arenes, one can get alicyclic compounds. In fact, this dearomatization is one of the most powerful ways of obtaining alicyclic compounds. But some of the most abundantly available arenes, such as benzene and naphthalene, are very stable, ...
The original iPS methods employed retroviruses to introduce the four cDNAs into cells7,8. Until recently, the majority of methods have relied on viral introduction of one form or another - a technique that often results in multiple random integration events, running the risk of insertion activation/inactivation which raises safety issues for downstream applications. In the process of reprogramming, the viral sequences are in - activated and the endogenous genes encoding the reprogramming factors reactivated but concerns surround the continued overexpression of pluripotency genes and the effects this has on a cells ability to be differentiated, or maintain that state in cell transplantation scenarios, risking the eventual formation of teratomas.. A significant technical development came recently with the effective introduction into somatic cells of a single vector expressing all four factors as a single cistron (either using a plasmid, lentivirus or transposon vectors) and then removal of all ...
Posted on Oct. 21, 2014 UNCs pharmacy school has received a $3 million gift from philanthropist and pharmaceutical-industry executive Fred Eshelman 72.. Eshelmans gift will support the work of the schools Center for Integrative Chemical Biology and Drug Discovery. The center is dedicated to evaluating and developing potential drug targets discovered by UNC faculty.. The UNC Eshelman School of Pharmacy, one of the nations top pharmacy schools, ranks second in total research funding and has the No. 2 doctor of pharmacy program in the nation, according to U.S. News & World Report.. Researchers at UNC often discover interesting biological systems that could represent novel drug targets. These targets can be thought of as locks, and the Center for Integrative Chemical Biology and Drug Discovery studies the locks to see whether a pharmaceutical key can be created to stop or start biological processes related to diseases.. The center bridges the gap that exists between the biological sciences ...
Today I wanted to highlight books specifically on medicinal chemistry and drug discovery. Those are always festive additions to the holiday season, right? This
WARNER, Digby F and MIZRAHI, Valerie. Approaches to target identification and validation for tuberculosis drug discovery: A University of Cape Town perspective. SAMJ, S. Afr. med. j. [online]. 2012, vol.102, n.6, pp.457-461. ISSN 2078-5135.. Tuberculosis (TB) disproportionately affects a few high-burden countries including South Africa. In these regions, basic TB research is rare, endemic countries being valued primarily as sites for drug trials and clinical studies. Our basic mycobacterial research focuses on current approaches to drug target identification and validation within the context of international trends in TB drug discovery. Increased funding for TB drug development globally prompted a significant shift in the composition of drug discovery consortia, with academic laboratories assuming a major role in collaboration with industrial partners. This hybrid model holds promise for the expansion of local programmes, especially where actively supported by government. However, the ...
Full Text CA-97-006 CANCER DRUG DISCOVERY: DIVERSITY GENERATION AND SMART ASSAYS NIH GUIDE, Volume 26, Number 15, May 9, 1997 RFA: CA-97-006 P.T. 34 Keywords: Cancer/Carcinogenesis Chemistry, Organic Medicinal Chemistry Chemotherapeutic Agents Drug Design National Cancer Institute Letter of Intent Receipt Date: June 20, 1997 Application Receipt Date: August 22, 1997 PURPOSE The Developmental Therapeutics Program (DTP), Division of Cancer Treatment, Diagnosis and Centers (DCTDC), National Cancer Institute (NCI) invites Program Project grant applications (P01s) proposing innovative combinatorial approaches to the generation of structural diversity and smart assay development for cancer drug discovery (Nature, Supplement to Volume 384, Issue No. 6604, November 7, 1996). Applications responsive to this RFA will bring together chemists and biologists who will propose novel approaches to the discovery of compound classes potentially active against cancer. This initiative seeks to catalyze the ...
Drug Discovery Today is a review journal, published as monthly 12 double issues. The journal covers the whole of the preclinical drug discovery process, from target identification and validation, through hit identification, lead identification and optimisation, though to candidate selection. The reviews are at the cutting edge of the science underpinning drug discovery, written by experts in their respective fields and cover all aspects of drug discovery from state-of-the-art genomic and proteomic approaches to target identification, through the most innovative computational approaches drug design, the science driving medicinal chemistry and the translation of these sciences to therapies
We see confirmation bias in drug discovery all the time. For instance, if molecular dynamics or fragment-based drug discovery or machine learning or some other technique, say Method X, is your favorite technique for discovering drugs, then you will keep on tracking successful applications of this technique without keeping track of the failures. Why would you do this? Several reasons, some of which are technological and some are sociological. You may have been trained in Method X since graduate school; method X is thus what you know and do best, and you dont want to waste time learning Method Y. Method X might legitimately have had one big success, and you might therefore believe in it - even with an n of 1. Method X might just be easy to use; in that case you are transformed into the man who looks for his keys under the streetlight, not because thats where they are but thats where its easiest to look. Method X could be a favorite of certain people who you admire, and certain other people who ...
This work aims to show on a very concrete example that simulations (In-Silico experiments) can help drug discovery process and therapeutic strategies searc
SELECTBIO is thrilled to announce the continuation of Epigenetics in Drug Discovery for 2017.. The event will form part of the multi-track conference, Advances in Drug Discovery, and will run alongside three additional tracks: Antibodies in Drug Discovery, Academic Drug Discovery and Stem Cells in Drug Discovery.. As a multi-track event, delegates will have unrestricted access to all conference tracks and networking opportunities. Attracting researchers from both academia and industry, this track will explore the latest opportunities and challenges for epigeneticists looking to discover and develop new molecular entities. Topics to be addressed include, assays for Methyltranferases and Demethylases, Bromodomain inhibitor discovery, indications beyond cancer, Non-BET Bromodomains and of course updates in Oncology ...
Network approaches have demonstrated their potential impact on health-related research, including gene/protein characterization and drug design and side effects (14, 18, 19, 22, 36, 52), yet demonstrations that network information can inform drug target discovery are still limited. Here, we present the first confirmation that virus and host protein interaction data can be integrated to improve large-scale drug target discovery (specifically antiviral target discovery) and reveal additional insights into virus-host interactions. The positions of virus-interacting proteins suggest that the influenza virus has evolved to interact with proteins that influence network behavior, regardless of known abundance-degree biases in PPI data generation (which has not previously been demonstrated). The virus-specific subnetwork reveals that there is a set of proteins with moderately high betweenness in the total network yet low betweenness in the subnetwork. While these proteins may be of high importance to ...
Drug discovery in the ovarian cancer arena continues to launch important new clinical trials. Many biologic agents are being studied in phase II and phase III clinical trials for recurrent disease. These agents include compounds that disrupt angiogenesis through a variety of mechanisms. Other oncogenic pathways are also specifically targeted such as PARP, MEK, and topoisomerase inhibitors which are currently being studied in phase III trials. Various cytotoxic agents, as well as therapeutic vaccines, are also under investigation, and continue to demonstrate promising new data. The relevant agents in the treatment of ovarian cancer which have demonstrated positive phase II activity will be discussed.
Announcement: Due to ongoing concerns over COVID-19 we wanted to reassure all attendees that this event is still going ahead. However, if you or your company has changed its travel and attendance policy relating to this matter, we are able to grant remote/virtual access. Please contact a member of the SMi Team for more information [email protected] SMi group presents the launch of the inaugural AI in Drug Discovery conference taking place in London on 16th-17th March, 2020. AI-empowered machine learning technologies hold the potential of reducing drug discovery associated costs by US$ 70 billion in the upcoming 10 years. With an estimated +39% CAGR, AI in drug discovery is leading the way into a shorter, cheaper and more successful R&D era where compound generation is automated, drug synthesis is predictable and undruggable diseases are finally being targeted.. The presence of AI in drug discovery is tangible with the majority of drug discovery scientist already working with ...
Announcement: Due to ongoing concerns over COVID-19 we wanted to reassure all attendees that this event is still going ahead. However, if you or your company has changed its travel and attendance policy relating to this matter, we are able to grant remote/virtual access. Please contact a member of the SMi Team for more information [email protected] SMi group presents the launch of the inaugural AI in Drug Discovery conference taking place in London on 16th-17th March, 2020. AI-empowered machine learning technologies hold the potential of reducing drug discovery associated costs by US$ 70 billion in the upcoming 10 years. With an estimated +39% CAGR, AI in drug discovery is leading the way into a shorter, cheaper and more successful R&D era where compound generation is automated, drug synthesis is predictable and undruggable diseases are finally being targeted.. The presence of AI in drug discovery is tangible with the majority of drug discovery scientist already working with ...
Human cancer cell lines are an integral part of drug discovery practices. However, modeling the complexity of cancer utilizing these cell lines on standard plastic substrata, does not accurately represent the tumor microenvironment. Research into developing advanced tumor cell culture models in a three-dimensional (3D) architecture that more prescisely characterizes the disease state have been undertaken by a number of laboratories around the world. These 3D cell culture models are particularly beneficial for investigating mechanistic processes and drug resistance in tumor cells. In addition, a range of molecular mechanisms deconstructed by studying cancer cells in 3D models suggest that tumor cells cultured in two-dimensional monolayer conditions do not respond to cancer therapeutics/compounds in a similar manner. Recent studies have demonstrated the potential of utilizing 3D cell culture models in drug discovery programs; however, it is evident that further research is required for the development of
The recent boom of the proteomics field, or the analysis of the ever dynamic organismal proteome, has brought many advances with respect to the very nature of how the current drug discovery process is undertaken. The potential the field of proteomics brings in for identifying proteins involved in disease pathogenesis and physiological pathway reconstruction facilitates the ever increasing discovery of new, novel drug targets, their respective modes of action mechanistically, and their biological toxicology (Page).. The challenge in the drug discovery process is to find the exact causes of an underlying disease and find a way to negate them or bring them to normal levels. A mechanistic understanding of the nature of the disease in question is essential if we are to elucidate any target-specific remedy for it. While the causes of many documented clinical problems vary greatly in their nature and origin, in some cases, the cause is found at the protein level, involving protein function, protein ...
Source: Expert Opinion on Drug Discovery - November 28, 2018 Category: Drugs & Pharmacology Authors: Antonio Jes ús Banegas-Luna Baldomero Imbern ón Antonio Llanes Castro Alfonso P érez-Garrido Jos é Pedro Cerón-Carrasco Sandra Gesing Ivan Merelli Daniele D Agostino Horacio P érez-Sánchez Source Type: research. Advances in distributed computing with modern drug discovery ...
PCMD-ICCBS & Embassy of France Pakistan are jointly organizing 4th Pak-France Bi-National Workshop on Drug Discovery and Molecular Medicine in October 2015
This project completed in December 2015.. New Insecticides for Malaria Control: Discovery Research for the Identification of New Chemical Entities for Malaria Control was a continuation of research initiated under the FNIHs Vector-based Control of Transmission: Discovery Research (VCTR) program. VCTR was itself an extension of the Bill & Melinda Gates Foundations Grand Challenges in Global Health initiative. As a subset of activities under the VCTR program, the New Insecticides for Malaria Control program addressed the urgent need for new chemicals to kill mosquitoes that transmit malaria. Current efforts rely heavily on the use of available insecticides for use on bednets, for indoor residual spraying and for application of chemical larvicides. Available insecticides are limited in number and the only one class of compound (pyrethroids) can safely be used on bednets. The situation is grim as mosquitoes have evolved resistance to the compounds currently in use. This program sought to address ...
The global Drug Discovery Informatics Market is projected to grow at a CAGR of 12.6% over the forecast period. Drug discovery is a multidisciplinary process used by researchers to encounter highly interconnected and complex meta data with the unprecedented availability of instrumentation and information technology. It is a capital-intensive, complicated, and a lengthy procedure, which demands expertise from pharmaceutical and multiple other scientific disciplines.. The advanced information technology has redefined the traditional drug discovery process and the research productivity of computational chemistry application is providing substantial benefits to drug discovery informatics platform.. Inexpensive computing is transforming the face of modern discovery informatics. The redefinition of drug discovery informatics is serving scientists with decision support tools and the rise in data culture is driving the growth of drug discovery informatics market.. Get Sample PDF and read more details ...
Title:In Silico Systems Pharmacology to Assess Drugs Therapeutic and Toxic Effects. VOLUME: 22 ISSUE: 46. Author(s):Alejandro Aguayo-Orozco, Karine Audouze, Soren Brunak and Olivier Taboureau. Affiliation:Novo Nordisk Foundation Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen. Keywords:Systems pharmacology, biological network, drug, protein-protein interactions, pathways, gene expression, pharmacogenomics, toxicity.. Abstract:For many years, the one target, one drug paradigm has been the driving force behind developments in pharmaceutical research. With the recent advances in molecular biology and genomics technologies, the focus is shifting toward drug-holistic systems based approaches (i.e. systems pharmacology). The integration of large and diverse amount of data from chemistry and biology coupled with the development and the application of network-based approaches to cope with these data is the next paradigm of drug discovery. ...
Lawrence Toll Ph.D. a renowned scientist whose research focuses on the management of pain and drug addiction through pharmacology and new drug discovery recently joined Florida Atlantic University as a professor in the Department of Biomedical Science in the Charles E. Schmidt College of Medicine and as an investigator in ...
Title:Predicting Targeted Polypharmacology for Drug Repositioning and Multi- Target Drug Discovery. VOLUME: 20 ISSUE: 13. Author(s):X. Liu, F. Zhu, X. H. Ma, Z. Shi, S. Y. Yang, Y. Q. Wei and Y. Z. Chen. Affiliation:State Key Laboratory of Biotherapy, Sichuan University, Chengdu 610064, P. R. China.. Keywords:Computer aided drug design, drug discovery, drug repositioning, gene expression, multi-target, network pharmacology, systems pharmacology, virtual screening. Abstract:Prediction of polypharmacology of known drugs and new molecules against selected multiple targets is highly useful for finding new therapeutic applications of existing drugs (drug repositioning) and for discovering multi-target drugs with improved therapeutic efficacies by collective regulations of primary therapeutic targets, compensatory signalling and drug resistance mechanisms. In this review, we describe recent progresses in exploration of in-silico methods for predicting polypharmacology of known drugs and new molecules ...
at Purdue.. The partnership helps to advance the Purdue Moves drug discovery initiative to translate basic research into life-changing treatments.. Philip Low, Purdues Ralph C. Corley Distinguished Professor of Chemistry and inaugural director of the Purdue Center for Drug Discovery, says Houston Methodist is one of the top clinical trial hospitals in the world and has built an infrastructure that quickly brings innovations to the clinic. The collaboration will make that infrastructure available to Purdue researchers in the same way it would be available to the institutes own faculty.. They know exactly how to bring a drug from the bench top to the bedside and, so, with the strengths that we have at Purdue in discovering new drugs, Houston Methodist makes an ideal partner to really complete the entire journey from discovery to delivery, he says.. The partnership is flexible and discussions are ongoing about the details of collaborative initiatives. An educational collaboration is important ...
Resource for professionals in the drug development industry- Information on drug discovery and early-stage drug development, discovery technology and more
Grand Valley State Universitys chemistry department will be hosting professor Brian Shoichet Thursday, Oct. 5, and Friday, Oct. 6, for a public lecture and seminar on the discovery of drugs and the advancements and challenges of modern medicine.
Led by Dr. Andrei Ivanov, The ECBDC Computational Chemical Biology and Systems Pharmacology (CCBSP) team utilizes state-of-the-art bioinformatics, computational modeling, and systems biology approaches to study and regulate the molecular connectivity between the biological pathways to facilitated target discovery and therapeutic development ...
... TIBCO Spotfire Lead Discovery provides an easy-to-use highly visu...SOMERVILLE Mass. Nov. 11 /- TIBCO SoftwareIn...In order to determine which compounds to synthesize to optimize thedr... Spotfire Lead Discovery enhances a chemists intuition and expertise...,TIBCO,Speeds,Drug,Discovery,for,Chemists,biological,advanced biology technology,biology laboratory technology,biology device technology,latest biology technology
SUNNYVALE, CA - November 17, 2008 - MDS Analytical Technologies, a leader in innovative solutions for drug-discovery and life-sciences research, today announced the delivery of the first three CellKeyTM384 Systems, the worlds first impedance-based, label-free, high-throughput instrument for use in drug-discovery research. Additional systems are scheduled to be delivered before the close of the calendar year.
Protein structure-based drug design has been contributing to the drug discovery process since the early 1990s. Structural knowledge on the exact interactions of drugs with their target proteins has been applied mainly to predict potency changes of chemically modified lead compounds.. With the 3D-structural information available today, additional aspects of the drug discovery process become predictable. Target-based virtual screening is being applied to identify new unexpected lead structures. Selectivity of compounds between homologous or orthologous proteins can be predicted, offering new possibilities to design selective compounds or predict the suitability of animal models for pharmacodynamic studies. Also the number of x-ray structures of proteins relevant for ADMET properties of drug molecules has remarkably increased during the last few years. This development offers the possibility to modulate or rationally design out unwanted ADMET properties. This covers aspects such as plasma protein ...
The Oregon Clinical and Translational Research Institute (OCTRI) and the Office of Technology Transfer & Business Development (TTBD) are pleased to announce a new funding opportunity to support drug discovery and therapeutic technology development efforts at OHSU.. The Biomedical Innovation Program (BIP) Drug Discovery/Therapeutic Track is a funding mechanism that aims to accelerate creative, trans-disciplinary drug discovery, and therapeutic development research. Examples of responsive projects may include (but are not limited to) research involving target validation, development of small molecules, antibodies, vaccines and biologics.. The current RFA can be found here ...
Recursion Pharmaceuticals has raised $60 million to step up its artificial intelligence-enabled drug discovery activities. The series B equips Recursion to move beyond its initial focus on repurposing molecules by applying its technology to the discovery of novel targets and drugs.. Salt Lake City, Utah-based Recursion is built upon an AI-powered approach to phenotypic screening and other aspects of the drug discovery process. The approach is underpinned by a fast-growing collection of cellular images and other data. By analyzing this resource with software incorporating computer vision, machine learning and neural networks, Recursion thinks it can spot changes in its data and, in doing so, discover novel biology, targets and drugs. ...
Author(s): Perez, Christian; Barkley-Levenson, Amanda M; Dick, Benjamin L; Glatt, Peter F; Martinez, Yadira; Siegel, Dionicio; Momper, Jeremiah D; Palmer, Abraham A; Cohen, Seth M | Abstract: Anxiety and depression are common, highly comorbid psychiatric diseases that account for a large proportion of worldwide medical disability. Glyoxalase 1 (GLO1) has been identified as a possible target for the treatment of anxiety and depression. GLO1 is a Zn2+-dependent enzyme that isomerizes a hemithioacetal, formed from glutathione and methylglyoxal, to a lactic acid thioester. To develop active inhibitors of GLO1, fragment-based drug discovery was used to identify fragments that could serve as core scaffolds for lead development. After screening a focused library of metal-binding pharmacophores, 8-(methylsulfonylamino)quinoline (8-MSQ) was identified as a hit. Through computational modeling and synthetic elaboration, a potent GLO1 inhibitor was developed with a novel sulfonamide core pharmacophore. A lead
Chris Abell is Professor of Biological Chemistry in the University of Cambridge. He heads a multidisciplinary research group interested in biological chemistry, with a focus on enzyme mechanism, structure and inhibition. In 1999, together with Tom Blundell and Harren Jhoti, he co-founded Astex Therapeutics, the leading company in fragment-based drug discovery. Astex was recently acquired by Otsuka for $0.9bn. Chris is collaborating on projects using fragment-based approaches to find small molecules that disrupt protein-protein interactions and inhibitors of enzymes from Mycobacterium tuberculosis. He also has major interests in the use of microdroplets to study biological reactions. Chris has published over 230 papers and held Visiting Professorships in France, Spain, New Zealand and Australia. He is also a co-founder of Akubio (2002), Sphere Fluidics (2010), and Aqdot (2013).. ...
Marco Albanese recently presented a poster on using fragment-based approaches to discover compounds targeting the ATP-binding domain of bacterial histidine kinases at the 7th RSC-BMCS Fragment-based Drug Discovery meeting in Cambridge. Bacterial histidine kinases (HKs) are part of two-component systems (TCSs), the most widespread means by which bacteria sense and adapt to external and internal stimuli. […]. ...
With the publication of Drug Discovery in Leishmaniasis by Luis Rivas and Carmen Gil, the Drug Discovery Series sees the milestone publication of 60 books in the series.. Led by Editor in Chief David Thurston, the series covers all aspects of drug discovery and medicinal chemistry making use of expert case studies to accessibly detail both fundamental science and cutting-edge technologies. Since 2010 with the publication of Metabolism, Pharmacokinetics and Toxicity of Functional Groups the series has gone on to cover hot topics from nanomedicines and epigenetics to anti-aging drugs and green chemistry.. Books in the series include:. ...
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Adipose Biology and Obesity Linked Insulin Resistance: A major research study in the laboratory focuses on the metabolic relationships between obesity and insulin action. This laboratory specifically examines cytoplasmic fatty acid binding proteins and their role(s) in mediating fatty acid metabolism in adipocytes and macrophages, particularly leukotriene synthesis. Using a combination of biochemical, biophysical and molecular methodologies, the laboratory studies the synthesis of inflammatory lipids in macrophages and other cells. Importantly, animal models either null or transgenic for fatty acid binding proteins reveal that intracellular lipid metabolism control the synthesis and secretion of adipose-derived cytokines (adipokines) linked to glucose and lipid metabolism in muscle and liver. Using a drug discovery approach, small molecule inhibitors of FABPs have been identified that exhibit anti-inflammatory properties in macrophages. Such studies provide a framework for the analysis of ...
The origin of many modern drugs is derived from ethnopharmacology, traditional medicine, and reverse pharmacology. Natural products have been a boon for both organic as well as medicinal chemists and practitioners of traditional medicine in exploring new biosynthetic pathways, charting novel synthesis strategies, and finding cures for human diseases. However, there has been a de-emphasis on natural product-based drug discovery programs over the last 20 years by the pharmaceutical industry, in part because of a perceived promise of high-throughput screening and combinatorial chemistry which never came to fully meet heightened expectations ...
Liang Xu (2014-2015) Associate Professor, Department of Molecular Biosciences University of Kansas Fragment-based drug discovery for inhibitors of RNA-binding protein HuR
The Primer on Medical and Population Genetics is a series of informal weekly discussions of basic genetics topics that relate to human populations and disease. Experts from across the Broad Institute community give in-depth introductions to the basic principles of complex trait genetics, including human genetic variation, genotyping, DNA sequencing methods, statistics, data analysis, and more.
Cambridge, UK, September 3rd 2010 - Prosarix announces successful completed of EEDA funded program on the development of chiral SAR panels for drug discovery.. Pharmaceutical companies develop biologically active lead compounds using a variety of methods e.g. rational approaches (fragment-based discovery, computer-based design) or screening large collections of molecules (HTS - high throughput screening). From an identified hit, large numbers of structurally-related compounds are synthesised in order to optimise both the drug-like properties of the molecule and to define the maximum scope of protectable IP.. A recent trend by companies working in this structure activity relationship (SAR) stage of drug discovery is to utilise more complex molecular structures, which typically possess chirality, i.e. the compound can exist in two or more stereospecific forms. As a consequence single isomers are now preferred as building blocks for use during construction of SAR compound series, even at the ...
Our partner, a Hungarian start-up company has developed an advanced visualization, multi-layered databases, network analytical cloud-based software and webservice called Biomedical Information Navigator (BIN). This service has been developed to facilitate early drug target discovery and drug repurposing for pharma-related researchers, Contract Research Organizations, pharma companies.. ...
Systems Pharmacology and Translational Therapeutics involves the discovery of new drugs, the investigation of how drugs work and the use of drugs to probe mechanisms of disease that spans the most fundamental aspects of basic research, through transgenic animal models, to clinical investigation.
Consortium will use QSP to predict the immunogenicity of biologics and its impact on pharmacokinetics, efficacy and safety in diverse patient populations. PRINCETON, NJ - Jan. 25, 2017 - Certara®, the leading provider of decision support technology and consulting services for optimizing drug development and improving health outcomes, today announced that it is launching a Quantitative Systems Pharmacology (QSP) Immunogenicity Consortium. Modeled after Certaras highly successful Simcyp® Consortium, and believed to be the first of its kind, the QSP Immunogenicity Consortium brings together leading biopharmaceutical companies in a pre-competitive environment to cooperatively develop an Immunogenicity Simulator that will predict immunogenicity of biologics and its impact on their pharmacokinetics, efficacy and safety in diverse patient populations.. Immunogenicity is defined by the US Food and Drug Administration (FDA) as the propensity of the therapeutic protein product to generate immune ...
2. Some Background Information 49 3. Definitions and Terminology 52 4. The One Clause at a Time (OCAT) Approach 54 4. 1 Data Binarization 54 4. 2 The One Clause at a Time (OCAT) Concept 58 4. 3 A Branch-and-Bound Approach for Inferring Clauses 59 4. 4 Inference of the Clauses for the Illustrative Example 62 4. 5 A Polynomial Time Heuristic for Inferring Clauses 65 5. A Guided Learning Approach 70 6. The Rejectability Graph of Two Collections of Examples 72 6. 1 The Definition of the Rej ectability Graph 72 6. 2 Properties of the Rejectability Graph 74 6. 3 On the Minimum Clique Cover of the Rej ectability Graph 76 7. Problem Decomposition 77 7. 1 Connected Components 77 7. 2 Clique Cover 78 8. An Example of Using the Rejectability Graph 79 9. Conclusions 82 References 83 Authors Biographical Statement 87 Chapter 3 AN INCREMENTAL LEARNING ALGORITHM FOR INFERRING LOGICAL RULES FROM EXAMPLES IN THE FRAMEWORK OF THE COMMON REASONING PROCESS, by X. Naidenova 89 1. Introduction 90 2. A Model of Rule-Based
A raw dataset including measures and dimensions is processed, by a preprocessing module, using an algorithm that produces a preprocessed dataset such that at least one type of statistical analysis of the preprocessed dataset yields equal results to the same type of statistical analysis of the raw dataset. The preprocessed dataset is then analyzed by a statistical analysis module to identify subsets of the preprocessed dataset that include a non-random structure or pattern. The analysis of the preprocessed dataset includes the at least one type of statistical analysis that produces the same results for both the preprocessed and raw datasets. The identified subsets are then ranked by a statistical ranker based on the analysis of the preprocessed dataset and a subset is selected for visualization based on the rankings. A visualization module then generates a visualization of the selected identified subset that highlights a non-random structure of the selected subset.
Baseline characteristics were not different between cases and controls, except for beta-blocker use and which was higher in cases, and mean (SD) CFR which was lower in cases [1.19 (0.23) and 2.78 (0.78) in cases and controls respectively; p < 0.01]. We identified 5345 peptides corresponding to 209 proteins, and identified 197 proteins by peptides with suitable properties to infer relative quantitation values. While the calculated values for some proteins (e.g. vascular cell adhesion molecule-1, apolipoprotein C and Von Willebrand Factor) indicate fold-differences between groups, these are most likely a result of high values in only 1-2 patients and are not statistically significant ...
Baragana, B. , Hallyburton, I. , Lee, M. C. S. , Norcross, N. R. , Grimaldi, R. , Otto, T. D. , Proto, W. R. , Blagborough, A. M. , Meister, S. , Wirjanata, G. , Ruecker, A. , Upton, L. M. , Abraham, T. S. , Almeida, M. J. , Pradhan, A. , Porzelle, A. , Santos Martinez, M. , Bolscher, J. M. , Woodland, A. , Luksch, T. & 44 others Norval, S., Zuccotto, F., Thomas, J., Simeons, F., Stojanovski, L., Osuna-Cabello, M., Brock, P. M., Churcher, T. S., Sala, K. A., Zakutansky, S. E., Belén Jiménez-Díaz, M., Maria Sanz, L., Riley, J., Basak, R., Campbell, M., Avery, V. M., Sauerwein, R. W., Dechering, K. J., Noviyanti, R., Campo, B., Frearson, J. A., Angulo-Barturen, I., Ferrer-Bazaga, S., Javier Gamo, F., Wyatt, P. G., Leroy, D., Siegl, P., Delves, M. J., Kyle, D. E., Wittlin, S., Marfurt, J., Price, R. N., Sinden, R. E., Winzeler, E. A., Charman, S. A., Bebrevska, L., Gray, D. W., Campbell, S., Fairlamb, A. H., Willis, P. A., Rayner, J. C., Fidock, D. A., Read, K. D. & Gilbert, I. H. 18 Jun 2015 In ...
Free Online Library: Samaritan Discovers Long-Sought-After Small Molecule Drug That Induces Human Neuron Differentiation. by Business Wire; Business, international
VIDEO: Pre-clinical study shows MD Anderson-developed drug effective for mantle cell lymphoma treatment. A study at The University of Texas MD Anderson Cancer Center demonstrated how a small molecule drug discovered at the institution may help overcome resistance to treatment with ibrutinib in patients with mantle cell lymphoma. The drug, IACS-10759, was the first therapy to be developed from concept to clinical trial by MD Andersons Therapeutics Discovery division, a unique drug-discovery engine created to answer unmet patient needs. IACS-10759 is […]. Read More ». ...
12-13 June 2017, Hotel Palace in Berlin, Germany.. Oxford Global present the 18th Annual Drug Discovery Leaders Summit that brings together over 250 key opinion leaders and senior industry experts in drug discovery, to discuss the latest innovative discovery strategies in different therapeutic areas as well as the most effective enabling technologies and solutions. The co-located 5th Discovery Chemistry & Drug Design Congress provides an unprecedented opportunity to gain insights from key presenters of the computational chemistry, discovery chemistry and medicinal field.. You can download the agenda here:. ...
Corning Incorporated today announced its support of two scientific symposia that will focus on new drug discovery and life science research advances made possible through label-free detection technology.
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A widely used screening tool deployed in the early phases of drug discovery to weed out undesirable compounds is wrong so often it cant be trusted on its own, according to scientists at the University of North Carolina at Chapel Hill.. PAINS-or pan-assay interference compounds -are a prominent source of false positives in the drug-discovery process. PAINS are biologically active compounds that masquerade as potential drug candidates during the initial high volume screening used to search for possible new drugs. PAINS work by disrupting the assay technology used in the screening to report biological activity, but they are not active against the intended biological target.. Seven years ago, a team of scientists identified a set of a molecular fingerprints that they said could be used to identify PAINS compounds. They found 480 molecular fragments they called PAINS alerts. The presence of a PAINS alert in a compound meant the compound was a PAIN. Pharmaceutical scientist were grateful to finally ...
New York - September 19, 2019 - BOC Sciences, a New York-based supplier of various bio-chemicals such as inhibitors, APIs, metabolites and impurities, announced earlier this month to launch cell apoptosis assay service for scientists engaged in drug discovery research. With expertise and well-published cell based assays from BOC Sciences, researchers now dont need to worry about apoptosis detection anymore.. Apoptosis, or alternatively referred to as programmed cell death, plays an important role in many human diseases. Controlled by multiple signaling and effector pathways, apoptosis is found to be closely linked with caspase related apoptotic enzyme cascades, mitochondrial depolarization, DNA fragmentation and ultimately cell blebbing and destruction. This offers new insights for scientists who are seeking new treatment for various diseases: through approaches of genetically modulating these apoptosis-associated pathways, new therapies might be discovered. Many human conditions like ...
Natural Product Chemistry for Drug Discovery provides a comprehensive summary of where natural product chemistry is today in drug discovery. The book covers emerging technologies and case studies and is a source of up-to-date information on the topical subject of natural products.
The Chemical Genomics Facility (CGF) is a newly established facility at the Purdue Institute for Drug Discovery. The mission of the CGF is to provide expertise and resources for investigators from Purdue and others to access to the state-of-art technologies and instrumentation in high-throughput screening (HTS) and high content screen (HCS) to facilitate the identification of chemical tools to study biological pathways and the discovery of lead compounds for the development of novel therapeutics and diagnostic approaches. The facility is designed to be highly flexible in order to meet the needs of multiple users employing a range of assays from a wide range of disciplines. Our experienced facility staff work closely with each investigator and provide services through all stages of the lead discovery process. ...
Experiment is an online platform for funding and sharing scientific discoveries. Push the boundaries of knowledge in biology, chemistry, medicine, physics, computer science, paleontology, economics, engineering, neuroscience, and more.
Join the fight against disease by learning how to create better and safer drugs for society with a degree in Chemistry for Drug Discovery and Development. Our BSc (Hons) Chemistry for Drug Discovery and Development aims to develop skills in the design and development of active molecules, all the way through to the final pharmaceutical products available to patients. Students can gain knowledge of synthetic chemistry and develop experience in drug formulation and manufacture within the regulatory context of the pharmaceutical industry. This will involve substantial practical experience of advanced laboratory techniques. On this programme, students have the opportunity to develop a comprehensive knowledge of chemistry alongside subject-specific and generic skills to develop a strong understanding of how chemistry is applied to problems with direct impact on society. Our programmes are designed to produce highly employable graduates with a broad background in academic chemistry and significant
TY - JOUR. T1 - Discovery of novel drug targets and their functions using phenotypic screening of natural products. AU - Chang, Junghwa. AU - Kwon, Ho Jeong. PY - 2016/3/1. Y1 - 2016/3/1. N2 - Natural products are valuable resources that provide a variety of bioactive compounds and natural pharmacophores in modern drug discovery. Discovery of biologically active natural products and unraveling their target proteins to understand their mode of action have always been critical hurdles for their development into clinical drugs. For effective discovery and development of bioactive natural products into novel therapeutic drugs, comprehensive screening and identification of target proteins are indispensable. In this review, a systematic approach to understanding the mode of action of natural products isolated using phenotypic screening involving chemical proteomics-based target identification is introduced. This review highlights three natural products recently discovered via phenotypic screening, ...