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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
1993 62
1994 78
1995 87
1996 93
1997 85
1998 93
1999 93
2000 96
2001 85
2002 93
2003 98
2004 84
2005 71
2006 83
2007 112
2008 97
2009 75
2010 98
2011 100
2012 74
2013 78
2014 72
2015 66
2016 54
2017 54
2018 71
2019 34
2020 0
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2,007 results
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Page 1
Neurokinin-1 receptor antagonists as antitumor drugs in gastrointestinal cancer: A new approach.
Muñoz M and Coveñas R. Saudi J Gastroenterol 2016 - Review. PMID 27488320 Free PMC article.
After binding to the neurokinin-1 (NK-1) receptor, the undecapeptide substance P (SP) regulates GI cancer cell proliferation and migration for invasion and metastasis, and controls endothelial cell proliferation for angiogenesis. ...NK-1 receptor antagonists are safe and well tolerated. Thus, the NK-1 receptor could be considered as a new target in GI cancer and NK-1 receptor antagonists (eg, aprepitant) could be a new promising approach for the treatment of GI cancer....
After binding to the neurokinin-1 (NK-1) receptor, the undecapeptide substance P (SP) regulates GI cancer cell p …
Glioma and Neurokinin-1 Receptor Antagonists: A New Therapeutic Approach.
Muñoz M and Coveñas R. Anticancer Agents Med Chem 2019 - Review. PMID 29692265
Substance P (SP), through the neurokinin (NK)-1 receptor, controls cancer cell proliferation by activating c-myc, mitogenactivated protein kinases, activator protein 1 and extracellular signal-regulated kinases 1 and 2. ...CONCLUSION: The NK-1 receptor plays a crucial role in glioma and NK-1 receptor antagonists could be used as anti-glioma drugs....
Substance P (SP), through the neurokinin (NK)-1 receptor, controls cancer cell proliferation by activating c-myc, mitog …
Substance P and the Neurokinin-1 Receptor: The New CRF.
Schank JR and Heilig M. Int Rev Neurobiol 2017 - Review. PMID 29056150
Substance P (SP) is an 11-amino acid neuropeptide of the tachykinin family that preferentially activates the neurokinin-1 receptor (NK1R). ...Given promising clinical findings for the efficacy of NK1R antagonists on craving in alcoholics, along with recent data suggesting that a number of negative results from NK1R trials were likely due to insufficient receptor occupancy, the NK1R merits being revisited as a target for the development of novel pharmacotherapeutics for addiction....
Substance P (SP) is an 11-amino acid neuropeptide of the tachykinin family that preferentially activates the neurokinin-1 r
Crystal structures of the human neurokinin 1 receptor in complex with clinically used antagonists.
Schöppe J, et al. Nat Commun 2019. PMID 30604743 Free PMC article.
Here we report high-resolution crystal structures of the human NK(1) receptor (NK(1)R) bound to two small-molecule antagonist therapeutics - aprepitant and netupitant and the progenitor antagonist CP-99,994. ...Taken together, these co-structures provide a comprehensive structural basis of NK(1)R antagonism and will facilitate the design of new therapeutics targeting the neurokinin receptor family....
Here we report high-resolution crystal structures of the human NK(1) receptor (NK(1)R) bound to two small-molecule a
Neurokinin 1 receptor antagonists in the prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant.
Rapoport BL, et al. Future Oncol 2018. PMID 29130344
Improved understanding of CINV pathophysiology has triggered the development of new antiemetic therapeutic options, such as selective neurokinin-1 (NK(1)) receptor antagonists (RAs), which effectively prevent CINV when added to a standard antiemetic regimen (serotonin-3 RA and dexamethasone). Aprepitant and its water-soluble prodrug, fosaprepitant dimeglumine, are the most widely used NK(1) RAs, with extensive clinical use worldwide. ...
Improved understanding of CINV pathophysiology has triggered the development of new antiemetic therapeutic options, such as selective neu
Neurokinin 1 receptor signaling in endosomes mediates sustained nociception and is a viable therapeutic target for prolonged pain relief.
Jensen DD, et al. Sci Transl Med 2017. PMID 28566424 Free PMC article.
We report that the substance P (SP) neurokinin 1 receptor (NK(1)R) signals from endosomes to induce sustained excitation of spinal neurons and pain transmission and that specific antagonism of the NK(1)R in endosomes with membrane-anchored drug conjugates provides more effective and sustained pain relief than conventional plasma membrane-targeted antagonists. ...Cholestanol conjugation amplified and prolonged the antinociceptive actions of NK(1)R antagonists. These results reveal a critical role for endosomal signaling of the NK(1)R in the complex pathophysiology of pain and demonstrate the use of endosomally targeted GPCR antagonists....
We report that the substance P (SP) neurokinin 1 receptor (NK(1)R) signals from endosomes to induce sustained ex …
Neurokinin-1 receptor antagonists: review of their role for the prevention of chemotherapy-induced nausea and vomiting in adults.
Karthaus M, et al. Expert Rev Clin Pharmacol 2019 - Review. PMID 31194593
Introduction: The addition of neurokinin-1 receptor antagonists (NK(1)RAs) to standard prophylaxis of 5-hydroxytryptamine-3 RA (5-HT(3)RA) plus dexamethasone more effectively prevents chemotherapy-induced nausea and vomiting (CINV) associated with highly and moderately emetogenic chemotherapy. ...The availability of IV and oral formulations of NK(1)RAs and NK(1)RA-5-HT(3)RA fixed combinations offers further utility, particularly for those patients unsuited for oral administration. ...
Introduction: The addition of neurokinin-1 receptor antagonists (NK(1)RAs) to standard prophylaxis of 5-h …
Efficacy of neurokinin-1 receptor antagonists in the prevention of chemotherapy-induced nausea and vomiting in patients receiving carboplatin-based chemotherapy: A systematic review and meta-analysis.
Di Maio M, et al. Crit Rev Oncol Hematol 2018 - Review. PMID 29548482 Free article.
According to current ESMO - MASCC guidelines, a combination of a neurokinin-1 receptor antagonist (NK1RA), dexamethasone and a 5-HT3 receptor antagonist (5-HT3RA) is recommended to prevent carboplatin-induced emesis, albeit with moderate level of confidence and not unanimous consensus. ...Addition of NK1RA improves CR in all phases: acute phase, 94.5% vs. 90.1%; delayed phase, 76.4% vs. 61.7%; overall period, 75.3% vs. 60.4%. ...
According to current ESMO - MASCC guidelines, a combination of a neurokinin-1 receptor antagonist (NK1RA), dexam …
Clinical pharmacology of neurokinin-1 receptor antagonists for the treatment of nausea and vomiting associated with chemotherapy.
Rapoport B and Smit T. Expert Opin Drug Saf 2017 - Review. PMID 28460548
Areas covered: Information on pharmacology and safety of the NK-1 RAs derived from PubMed showed that all bind the NK-1 receptor with high affinity and selectivity. There is substantial variation in the disposition and time course in the body of NK-1 RAs because of the differential effects of hepatic metabolism. ...
Areas covered: Information on pharmacology and safety of the NK-1 RAs derived from PubMed showed that all bind the NK-1 rec
Human acute myeloid leukemia cells express Neurokinin-1 receptor, which is involved in the antileukemic effect of Neurokinin-1 receptor antagonists.
Molinos-Quintana A, et al. Invest New Drugs 2019. PMID 29721755
The substance P/neurokinin-1 receptor system has been implicated in tumor cell proliferation. Neurokinin-1 receptor has been identified in different solid tumors but not frequently in hematopoietic malignant cells. ...We also observed that four different Neurokinin-1 receptor antagonists (L-733,060, L-732,138, CP 96-345 and aprepitant) elicited inhibition of acute myeloid leukemia cell growth lines in a concentration-dependent manner, while growth inhibition was only marginal in lymphocytes; the specific antitumor action of Neurokinin-1 receptor antagonists occurs via the Neurokinin-1 receptor, and leukemia cell death is due to apoptosis. ...
The substance P/neurokinin-1 receptor system has been implicated in tumor cell proliferation. Neurokinin-1
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