abstract：:Magnetic nanoparticles (MNPs) play a vital role for improved imaging applications. Recently, a number of studies demonstrate MNPs can be applied for targeted delivery, sustained release of therapeutics, and hyperthermia. Based on stable particle size and shape, biocompatibility, and inherent contrast enhancement chara...

journal_title：Drug discovery today

authors： Chowdhury P,Roberts AM,Khan S,Hafeez BB,Chauhan SC,Jaggi M,Yallapu MM

更新日期：2017-08-01 00:00:00

abstract：:Rab GTPases constitute the largest family of small GTPases. Rabs regulate not only membrane trafficking but also cell signaling, growth and survival, and development. Increasingly, Rabs and their effectors are shown to be overexpressed or subject to loss-of-function mutations in a variety of disease settings, includin...

journal_title：Drug discovery today

authors： Qin X,Wang J,Wang X,Liu F,Jiang B,Zhang Y

更新日期：2017-08-01 00:00:00

abstract：:This review provides an update on the promises and pitfalls when using in vitro bioassays to evaluate beneficial and adverse health effects of botanicals and botanical preparations. Important issues addressed in the paper are: (i) the type of assays and biological effects available; (ii) false-positives, false-negativ...

journal_title：Drug discovery today

authors： Prinsloo G,Papadi G,Hiben MG,de Haan L,Louisse J,Beekmann K,Vervoort J,Rietjens IMCM

更新日期：2017-08-01 00:00:00

abstract：:Gastric bypass surgery is effectively a polypharmacological approach for treatment of obesity, type 2 diabetes and nonalcoholic steatohepatitis (NASH). The gastric bypass mimetic approaches reviewed are fixed-dose combinatorial pharmacological approaches. There are two key concepts incorporated into these gastric bypa...

journal_title：Drug discovery today

authors： Boettcher BR

更新日期：2017-08-01 00:00:00

abstract：:Immunotherapies have changed the treatment strategy of some types of tumor including melanoma and, more recently, non-small-cell lung cancer (NSCLC). Immune checkpoints are crucial for the maintenance of self-tolerance and it is known that some tumors use checkpoint systems to evade antitumor immune response. The trea...

journal_title：Drug discovery today

authors： Dal Bello MG,Alama A,Coco S,Vanni I,Grossi F

更新日期：2017-08-01 00:00:00

abstract：:Translating academic medical research into new therapies is an important challenge for the biopharmaceutical industry and investment communities, which have historically favored later-stage assets with lower risk and clearer commercial value. The Stanford SPARK program is an innovative model for addressing this challe...

journal_title：Drug discovery today

authors： Kim ES,Omura PMC,Lo AW

更新日期：2017-07-01 00:00:00

abstract：:With the aging of the general population, there is an increasing need for bone defect repair, prompting the development of reliable alternatives to autologous bone grafting, without the usually associated major drawbacks (i.e., limited volume and severe postoperative pain). Given the crucial role that miRNAs appear to...

journal_title：Drug discovery today

authors： Scimeca JC,Verron E

更新日期：2017-07-01 00:00:00

abstract：:Current advances in systems biology suggest a new change of paradigm reinforcing the holistic nature of the drug discovery process. According to the principles of systems biology, a simple drug perturbing a network of targets can trigger complex reactions. Therefore, it is possible to connect initial events with final...

journal_title：Drug discovery today

authors： Cruz-Monteagudo M,Schürer S,Tejera E,Pérez-Castillo Y,Medina-Franco JL,Sánchez-Rodríguez A,Borges F

更新日期：2017-07-01 00:00:00

abstract：:Kidneys have a major role in normal physiology and metabolic homeostasis. Loss or impairment of kidney function is a common occurrence in several metabolic disorders, including hypertension and diabetes. Chronic kidney disease (CKD) affect nearly 10% of the population worldwide; ranks 18th in the list of causes of dea...

journal_title：Drug discovery today

authors： Kota SK,Kota SB

更新日期：2017-07-01 00:00:00

abstract：:Regenerative approaches are promising avenues to effectively cure diseases rather than merely treating symptoms, but are associated with concerns around proliferation in other organs. Given that targeted delivery holds the promise of delivering a drug precisely to its desired site of action, usually with the prospect ...

journal_title：Drug discovery today

authors： Valeur E,Knerr L,Ölwegård-Halvarsson M,Lemurell M

更新日期：2017-06-01 00:00:00

abstract：:Diabetes mellitus (DM) is associated with an increased risk of cardiovascular disease (CVD). Inhibitors of proprotein convertase subtilisin/kexin type 9 (PCSK9) have emerged as effective low-density lipoprotein cholesterol-lowering compounds. Although the results of available epidemiological, preclinical, and clinical...

journal_title：Drug discovery today

authors： Momtazi AA,Banach M,Pirro M,Stein EA,Sahebkar A

更新日期：2017-06-01 00:00:00

abstract：:The growing application of nanomaterials in healthcare products (i.e., cosmetics, medical devices, and medicinal products) has encouraged the upgrade of the regulatory framework within the European Community to better control their use and manage the risk of negative effects on human health and environment. Unfortunat...

journal_title：Drug discovery today

authors： Musazzi UM,Marini V,Casiraghi A,Minghetti P

更新日期：2017-06-01 00:00:00

abstract：:Current multiparameter optimization (MPO) strategies make use of few experimental physicochemical descriptors (i.e., solubility at physiological pH and lipophilicity in the octanol/water system). Here, we show how new trends in drug discovery (i.e., large and flexible molecules for 'difficult' targets) call for the in...

journal_title：Drug discovery today

authors： Caron G,Ermondi G

更新日期：2017-06-01 00:00:00

abstract：:Proteomic-based techniques provide a powerful tool for identifying the full spectrum of protein targets of a drug, elucidating its mechanism(s) of action, and identifying biomarkers of its efficacy and safety. Herein, we outline the technological advancements in the field, and illustrate the contribution of proteomics...

journal_title：Drug discovery today

authors： Banfi C,Baetta R,Gianazza E,Tremoli E

更新日期：2017-06-01 00:00:00

abstract：:Records about the traditional uses of medicinal plants can be considered useful in bioprospecting (i.e., the search for new active agents or lead structures in nature). Several sources like Egyptian papyri, early modern herbals and pharmacopoeias have been studied in this respect. It is proposed to use recordings of b...

journal_title：Drug discovery today

authors： Helmstädter A

更新日期：2017-05-01 00:00:00

abstract：:Many pharmaceutical companies aim to reduce reactive metabolite formation by chemical modification at early stages of drug discovery. A practice often applied is the detection of stable trapping products of electrophilic intermediates with nucleophilic trapping reagents to guide rational structure-based drug design. T...

journal_title：Drug discovery today

authors： Brink A,Pähler A,Funk C,Schuler F,Schadt S

更新日期：2017-05-01 00:00:00

abstract：:Pancreatic cancer is one of the most aggressive and lethal human malignancies. Drug therapies and radiotherapy are used for treatment as adjuvants to surgery, but outcomes remain disappointing. Advances in tissue engineering suggest that 3D cultures can reflect the in vivo tumor microenvironment and can guarantee a ph...

journal_title：Drug discovery today

authors： Totti S,Vernardis SI,Meira L,Pérez-Mancera PA,Costello E,Greenhalf W,Palmer D,Neoptolemos J,Mantalaris A,Velliou EG

更新日期：2017-04-01 00:00:00

abstract：:Tuberculosis drug discovery has shifted in recent years from a primarily target-based approach to one that uses phenotypic high-throughput screens. As examples of this, through our EU-funded FP7 collaborations, New Medicines for Tuberculosis was target-based and our more-recent More Medicines for Tuberculosis project ...

journal_title：Drug discovery today

authors： Mikušová K,Ekins S

更新日期：2017-03-01 00:00:00

abstract：:Natural products (NPs) have been at the origin of several established drugs against tuberculosis (TB). Although the current clinical TB pipeline does not feature any candidates derived from new NP scaffolds, numerous novel NPs or NP analogs have been discovered in the recent past with promising activity against Mycoba...

journal_title：Drug discovery today

authors： Dong M,Pfeiffer B,Altmann KH

更新日期：2017-03-01 00:00:00

abstract：:Covalent allosteric modulators possess the pharmacological advantages (high potency, extended duration of action and low drug resistance) of covalent ligands and the additional benefit of the higher specificity and lower toxicity of allosteric modulators. This approach is gaining increasing recognition as a valuable t...

journal_title：Drug discovery today

authors： Lu S,Zhang J

更新日期：2017-02-01 00:00:00

abstract：:Over the past three decades, statins have become the cornerstone of prevention and treatment of atherosclerotic cardiovascular and metabolic diseases. Albeit generally well tolerated, these drugs can elicit a variety of muscle-associated symptoms that represent the most important reason for treatment discontinuation. ...

journal_title：Drug discovery today

authors： Muntean DM,Thompson PD,Catapano AL,Stasiolek M,Fabis J,Muntner P,Serban MC,Banach M

更新日期：2017-01-01 00:00:00

abstract：:A strategy for large-scale chiral resolution is illustrated by the isolation of pure enantiomer from a 5kg batch. Results from supercritical fluid chromatography will be presented and compared with normal phase liquid chromatography. Solubility of the compound in the supercritical mobile phase was shown to be the limi...

journal_title：Drug discovery today

authors： Leek H,Thunberg L,Jonson AC,Öhlén K,Klarqvist M

更新日期：2017-01-01 00:00:00

abstract：:The unique anti-atherosclerosis abilities and other cardioprotective properties make high-density lipoprotein (HDL) a promising solution in treating cardiovascular diseases. A number of studies showed that HDL-based therapy was well tolerated and has great potential in the future. Among all these new agents, the most ...

journal_title：Drug discovery today

authors： Cao YN,Xu L,Han YC,Wang YN,Liu G,Qi R

更新日期：2017-01-01 00:00:00

abstract：:Conventional mitogen-activated protein kinase (MAPK) family members are among the most sought-after oncogenic effectors for the development of novel human cancer treatment strategies. MEK5/ERK5 has been the less-studied MAPK subfamily, despite its increasingly demonstrated relevance in the growth, survival, and differ...

journal_title：Drug discovery today

authors： Simões AE,Rodrigues CM,Borralho PM

更新日期：2016-10-01 00:00:00

abstract：:The consensus hypothesis on coronary atherosclerosis suggests high LDL-C levels as the major cause and pursues it as the therapeutic target, explicitly assuming: (i) tunica intima of human coronaries consists of only one cell layer - endothelium, situated on a thin layer of scarcely cellular matrix; and (ii) subendoth...

journal_title：Drug discovery today

authors： Subbotin VM

更新日期：2016-10-01 00:00:00

abstract：:Spinal cord infarction (SCI) is a rare but disabling disorder caused by a wide spectrum of conditions. Given the lack of randomized-controlled trials, contemporary treatment concepts are adapted from guidelines for cerebral ischemia, atherosclerotic vascular disease, and acute traumatic spinal cord injury. In addition...

journal_title：Drug discovery today

authors： Nardone R,Pikija S,Mutzenbach JS,Seidl M,Leis S,Trinka E,Sellner J

更新日期：2016-10-01 00:00:00

abstract：:The Science for Life Laboratory Drug Discovery and Development (SciLifeLab DDD) platform reaches out to Swedish academia with an industry-standard infrastructure for academic drug discovery, supported by earmarked funds from the Swedish government. In this review, we describe the build-up and operation of the platform...

journal_title：Drug discovery today

authors： Arvidsson PI,Sandberg K,Forsberg-Nilsson K

更新日期：2016-10-01 00:00:00

abstract：:Antibodies (Abs) are regarded as a newly emerging form of therapeutics that can provide passive protection against influenza. Although the application of genomics in clinics has increased dramatically, the number of therapeutics available for the treatment of many diseases remains insufficient. To translate genomics i...

journal_title：Drug discovery today

authors： Yang HT,Yang H,Chiang JH,Wang SJ

更新日期：2016-10-01 00:00:00

abstract：:There is a continuing need to hasten and improve protein-ligand docking to facilitate the next generation of drug discovery. As the drug-like chemical space reaches into the billions of molecules, increasingly powerful computer systems are required to probe, as well as tackle, the software engineering challenges neede...

journal_title：Drug discovery today

authors： Trager RE,Giblock P,Soltani S,Upadhyay AA,Rekapalli B,Peterson YK

更新日期：2016-10-01 00:00:00

abstract：:The musculoskeletal system is an incredible machine that protects, supports and moves the human body. However, several diseases can limit its functionality, compromising patient quality of life. Designing novel pathological models would help to clarify the mechanisms driving such diseases, identify new biomarkers and ...

journal_title：Drug discovery today

authors： Bersini S,Arrigoni C,Lopa S,Bongio M,Martin I,Moretti M

更新日期：2016-09-01 00:00:00

abstract：:In recent years, advances in tissue engineering and microfabrication technologies have enabled rapid growth in the areas of in vitro organoid development as well as organoid-on-a-chip platforms. These 3D model systems often are able to mimic human physiology more accurately than traditional 2D cultures and animal mode...

journal_title：Drug discovery today

authors： Skardal A,Shupe T,Atala A

更新日期：2016-09-01 00:00:00

abstract：:Proline-rich Akt substrate 40kDa (PRAS40) bridges cell signaling between protein kinase B (Akt) and the mammalian target of rapamycin complex 1 (mTORC1). Both Akt and mTORC1 can phosphorylate PRAS40. As a negative regulator of mTORC1, PRAS40 prevents the binding of mTOR to its substrates. The phosphorylation of PRAS40...

journal_title：Drug discovery today

authors： Chong ZZ

更新日期：2016-08-01 00:00:00

abstract：:Glycosaminoglycans (GAGs) are charged polysaccharides ubiquitously present at the cell surface and in the extracellular matrix. GAGs are crucial for cellular homeostasis, and their metabolism is altered during pathological processes. However, little consideration has been given to the regulation of the GAG milieu thro...

journal_title：Drug discovery today

authors： Ghiselli G,Maccarana M

更新日期：2016-07-01 00:00:00

abstract：:The use of computational filters for excluding supposedly nonspecific and promiscuous compounds from chemical libraries is a controversial issue, because many drugs used in clinics today would never reach the market if these filters were applied. In part, this conflict could be caused by the paradigm: one-drug-one-tar...

journal_title：Drug discovery today

authors： Senger MR,Fraga CA,Dantas RF,Silva FP Jr

更新日期：2016-06-01 00:00:00

abstract：:The energy substrate preference of the human heart is well regulated and is modified upon aging, in that the fetal heart uses glucose, whereas the adult heart utilizes fatty acids. Various human and animal studies suggest a shift in myocardial substrate utilization and decreased rate of myocardial fatty acid uptake an...

journal_title：Drug discovery today

authors： Arumugam S,Sreedhar R,Thandavarayan RA,Karuppagounder V,Watanabe K

更新日期：2016-06-01 00:00:00

abstract：:The intestinal epithelium is the main barrier restricting the oral delivery of low-permeability drugs. Over recent years, numerous nanocarriers have been designed to improve the efficiency of oral drug delivery. However, the intracellular processes determining the transport of nanocarriers across the intestinal epithe...

journal_title：Drug discovery today

authors： Fan W,Xia D,Zhu Q,Hu L,Gan Y

更新日期：2016-05-01 00:00:00

abstract：:For several decades, the pharmaceutical industry has suffered due to major issues such as reductions of the number of FDA approved drugs and biologics. Several analyses have been highlighted that the 'druglikeness' is one of the strategies to improve succeed rates of screening such as, for instance, high-throughput sc...

journal_title：Drug discovery today

authors： Mignani S,Huber S,Tomás H,Rodrigues J,Majoral JP

更新日期：2016-04-01 00:00:00

abstract：:The global burden of herpes simplex virus (HSV) legitimates the critical need to develop new prevention strategies, such as drugs and vaccines that are able to fight either primary HSV infections or reactivations. Moreover, the ever-growing number of patients receiving transplants increases the number of severe HSV in...

journal_title：Drug discovery today

authors： Clementi N,Criscuolo E,Cappelletti F,Burioni R,Clementi M,Mancini N

更新日期：2016-04-01 00:00:00

abstract：:The p53 family proteins are among the most appealing targets for cancer therapy. A deeper understanding of the complex interplay that these proteins establish with murine double minute (MDM)2, MDMX, and mutant p53 could reveal new exciting therapeutic opportunities in cancer treatment. Here, we summarize the most rele...

journal_title：Drug discovery today

authors： Gomes S,Leão M,Raimundo L,Ramos H,Soares J,Saraiva L

更新日期：2016-04-01 00:00:00

abstract：:Protein expression therapy using nucleic acid macromolecules (NAMs) as a new paradigm in medicine has recently gained immense therapeutic potential. With the advancement of nonviral delivery it has been possible to target NAMs against cancer, immunodeficiency and infectious diseases. Owing to the complex and fragile s...

journal_title：Drug discovery today

authors： Muralidhara BK,Baid R,Bishop SM,Huang M,Wang W,Nema S

更新日期：2016-03-01 00:00:00