Abstract:
:Fatty acid synthase (FASN) is the enzyme that catalyzes the de novo synthesis of fatty acids in cells. Because of the strong expression in many cancers, FASN is an attractive and tractable target for therapeutic intervention. The discovery and development of pharmacologic agents that block FASN activity highlight the promise of these anticancer compounds. FASN inhibitors have also proven to be invaluable in developing a better understanding of the contribution of FASN and fatty acid synthesis to tumor cells. Recent advances in the development of crystal structures of FASN have provided promise towards the development of novel FASN inhibitors. This review outlines the preclinical development of FASN inhibitors, their antitumor effects and the strategies underway to develop novel inhibitors.
journal_name
Expert Opin Investig Drugsjournal_title
Expert opinion on investigational drugsauthors
Kridel SJ,Lowther WT,Pemble CW 4thdoi
10.1517/13543784.16.11.1817subject
Has Abstractpub_date
2007-11-01 00:00:00pages
1817-29issue
11eissn
1354-3784issn
1744-7658journal_volume
16pub_type
杂志文章,评审abstract::Endothelin (ET) is a pivotal physiological regulator of blood pressure through its effects on blood vessels, heart, lung and kidneys, and the ET system can be overactive in disorders such as pulmonary hypertension, heart failure and renal disease. Such observations stimulated interest among scientists and pharmaceutic...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.13.11.1419
更新日期:2004-11-01 00:00:00
abstract::The increasing frequency of fungal infections in immunocompromised patients together with the emergence of strains resistant to currently used antifungal drugs point to an increased need for a new class of antimycotics. Antimicrobial peptides are promising candidates for the treatment of fungal infections since they h...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.11.2.309
更新日期:2002-02-01 00:00:00
abstract::Introduction: Therapeutic oligonucleotides have emerged as a promising new class of drug that could silence undruggable targets; they can potentially treat metabolic liver diseases such as nonalcoholic fatty liver disease (NAFLD), hereditary hemochromatosis and alpha 1 antitrypsin deficiency. Areas covered: This artic...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1080/13543784.2021.1879792
更新日期:2021-01-29 00:00:00
abstract::INH-A21 is an experimental human immune globulin for intravenous infusion (IGIV) derived from donors specifically selected for elevated levels of antibodies against the Staphylococcal fibrinogen-binding proteins, serine aspartate dipeptide repeat G and clumping factor A. Phase II results demonstrated that infusions of...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.15.6.703
更新日期:2006-06-01 00:00:00
abstract::Oxcarbazepine (OXC) was introduced in 1990 and is now registered in 54 countries worldwide as monotherapy, as add-on treatment for partial seizures, with or without secondarily generalised seizures, and primary generalised tonic-clonic seizures. OXC and its active metabolite, monohydroxy derivative (MHD), block voltag...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.8.7.1103
更新日期:1999-07-01 00:00:00
abstract::Psoriasis is a chronic skin disorder characterised by inflammation producing red, thickened areas with a flaky white build-up. Efalizumab is a humanised monoclonal IgG1 antibody that inhibits the binding of T lymphocytes to endothelial cells and their subsequent migration. In patients suffering from plaque psoriasis, ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.13.5.551
更新日期:2004-05-01 00:00:00
abstract:INTRODUCTION:Sorafenib is an oral multikinase inhibitor with anti-angiogenic and anti-proliferative activity that is indicated for use in hepatocellular and renal cell carcinomas. Sorafenib is being developed in a number of solid tumors, including breast cancer (BC). AREAS COVERED:A series of four randomized, double-b...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2012.689824
更新日期:2012-08-01 00:00:00
abstract::The eating disorders anorexia nervosa, bulimia nervosa and binge eating disorder are common, significant public health problems which are treated with nutritional, psychotherapeutic and pharmacological interventions. A number of drugs (mostly antidepressant drugs) are currently used in their treatment to some benefit,...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.12.3.491
更新日期:2003-03-01 00:00:00
abstract::Anorexia nervosa (AN), bulimia nervosa (BN) and binge eating disorder (BED) each occur in about 0.5-1.5% of the population in westernised countries, and primarily affect women. At present, a variety of pharmacological treatments are used in addition to psychotherapy, with antidepressants being most the common. Current...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.6.4.427
更新日期:1997-04-01 00:00:00
abstract:INTRODUCTION:Therapeutic options for mycosis fungoides and Sézary syndrome include a variety of immunomodulatory, epigenetic, and cytotoxic options; however, none has been demonstrated to be efficacious for all patients, or to deliver deep and durable responses to the majority of patients. In this review, we examine th...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1080/13543784.2018.1498081
更新日期:2018-08-01 00:00:00
abstract::Therapeutic angiogenesis is a novel approach to the treatment of ischaemic or occlusive coronary and peripheral vascular disease. The therapeutic concept is based on the restoration of distal blood flow by the enlargement of existing vessels and tissue perfusion by the induction of new capillaries. Initial studies hav...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.13.10.1319
更新日期:2004-10-01 00:00:00
abstract::While oral formulations of agonists at the serotonin (5-HT) receptor subdivisions 5-HT(1B/1D)--the "triptan" class of drugs--dominate the market for migraine therapy and while still more triptans are under development, recent research efforts have also explored other pharmacological avenues, which are mostly based on ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.11.12.1813
更新日期:2002-12-01 00:00:00
abstract:INTRODUCTION:In 2010, about 8.8 million new cases of tuberculosis were recorded and 1.1 million people died of tuberculosis worldwide. Although numbers are in decrease since 2006, tuberculosis still represents a global issue and a major public health threat, due to appearance of multidrug-resistant and extensively drug...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2012.724397
更新日期:2012-12-01 00:00:00
abstract::In spite of tremendous efforts to control cancer, the mortality associated with this disease has been increasing in developed countries in the recent decades. Inadequate efficiency of existing therapeutic regimens and the rise of multi-drug resistant cancer cells are the main factors which require a broadening of inve...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.9.6.1243
更新日期:2000-06-01 00:00:00
abstract::Diminished efficacy in terms of clinical relapses and lesion load on magnetic resonance images for patients developing neutralising antibodies (NAbs) to recombinant IFN-beta may be found in multiple sclerosis. NAbs become detectable over the first few years of therapy, disappearing during the treatment course in some ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.12.7.1153
更新日期:2003-07-01 00:00:00
abstract::With the current standard chemotherapy regimens only approximately 25% of acute myelogenous leukaemia (AML) patients survive > 5 years. Aurora kinases are overexpressed in many human cancers. VX-680 inhibited Aurora-A, -B, -C and the FMS-like tyrosine kinase-3 with apparent inhibitory constants of 0.6, 18, 4.6 and 30 ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.13.9.1199
更新日期:2004-09-01 00:00:00
abstract:INTRODUCTION:Oxidative stress toxicity (OST) has been implicated in almost all pathological conditions. Despite the widespread use of natural antioxidants, no pharmaceutical antioxidants have yet been developed or prescribed in medical practise. Antioxidant drugs such as Deferiprone and N-acetylcysteine can target esse...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1080/13543784.2019.1631284
更新日期:2019-07-01 00:00:00
abstract:INTRODUCTION:Erectile function is an important aspect in the quality of life of many men. For men with erectile dysfunction (ED), a spectrum of treatment options exists. Novel therapies for ED are currently being developed in order to delay surgical placement of a penile prosthesis - the final step in the management of...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1080/13543784.2017.1324570
更新日期:2017-06-01 00:00:00
abstract:INTRODUCTION:Due to improvements in our understanding of the pathogenesis of systemic lupus erythematosus (SLE), several target drugs have been and are being developed. One of the possible targets in SLE is co-stimulation between antigen-presenting cells and T cells. Abatacept is a co-stimulation moderator approved for...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2016.1154943
更新日期:2016-01-01 00:00:00
abstract:INTRODUCTION:Alzheimer's disease (AD) is the most common cause of dementia in the elderly. Pharmacological treatment of AD includes Anticholinesterase Inhibitors (AChEIs) for mild-moderate AD, and memantine for severe AD. These drugs provide mainly symptomatic short-term benefits without clearly influencing the progres...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1080/13543784.2017.1265504
更新日期:2017-01-01 00:00:00
abstract:INTRODUCTION:Dasatinib is a novel tyrosine kinase inhibitor with activity against the Src family kinases. The Src pathway is active in breast cancer and has been shown to promote cell proliferation, invasiveness, and metastases. Preclinical data support the use of dasatinib to inhibit breast cancer cell growth, modulat...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.2013.793308
更新日期:2013-06-01 00:00:00
abstract::Introduction: Osteoarthritis (OA) is the most common form of arthritis. Knee OA is associated with joint pain, activity limitation, physical disability, reduced health-related quality of life, and increased mortality. To date, all pharmacologic treatments for OA are directed toward pain management. Lorecivivint (LOR) ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1080/13543784.2020.1842357
更新日期:2020-12-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:Antibacterial drug discovery and development has slowed considerably in recent years, with novel classes discovered decades ago and regulatory approvals tougher to get. Traditional approaches and the newer genomic mining approaches have not yielded novel classes of antibacterial compounds. Inste...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543780903505092
更新日期:2010-02-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:Contrasting with the broad activation of the PI3K/AKT/mammalian target of rapamycin (mTOR) survival pathway in most cancer, activity of rapalogues appears to be restricted to a few tumor types. AREAS COVERED IN THIS REVIEW:The analysis of molecular activity of the PI3K/AKT/mTOR pathway and resi...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2010.499121
更新日期:2010-08-01 00:00:00
abstract:INTRODUCTION:Peripheral arterial disease (PAD) is a manifestation, and marker of severity, of a generalized atherosclerotic process. Antiplatelet therapy is recommended to prevent cardiovascular events but much of the evidence to support this is drawn from studies on older drugs. AREAS COVERED:In this review, the auth...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2014.974803
更新日期:2014-12-01 00:00:00
abstract::Urinary tract infections (UTIs) are one of the most common reasons people seek medical attention. There are > 50% of women who will have at least one UTI during their lifetime and most of these will require a physician visit and antibiotic treatment. The high prevalence continues to the in-patient setting where genito...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.15.5.519
更新日期:2006-05-01 00:00:00
abstract::Innate immune mechanisms respond rapidly to bacterial infection. A key cellular component of the innate immune response is the neutrophil, whose cytoplasmic granules contain a variety of antimicrobial proteins and peptides. Among these is the bactericidal/permeability-increasing protein (BPI), a cationic 55 kDa protei...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.11.2.159
更新日期:2002-02-01 00:00:00
abstract::High-density lipoprotein (HDL) therapy is a novel and emerging area of therapeutic development in the cardiovascular field. It attempts to supplement and improve the vascular benefit exerted by other agents that are active on lipid metabolism, for example, hypolipidaemic drugs. Furthermore, it takes advantage of the n...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.15.3.227
更新日期:2006-03-01 00:00:00
abstract:INTRODUCTION:Progesterone receptor (PR) agonists (progestins) and antagonists are developed for female contraceptives. However, non-contraceptive applications of newer progestins and PR modulators are being given more attention. AREAS COVERED:The newer PR agonists including drospirenone, nomegestrol, trimegestone, die...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2012.642368
更新日期:2012-01-01 00:00:00
abstract::Age-related macular degeneration (AMD) is the leading cause of blindness in the Western world for those patients aged 50 years or older. Neovascular AMD, a subtype characterized by the growth of new, pathologic blood vessels, results in most of the cases of severe and rapid vision loss associated with AMD. A critical ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543780902855316
更新日期:2009-05-01 00:00:00