ReviewBiochemical pharmacology2010
Development of small-molecule inhibitors of the group I p21-activated kinases, emerging therapeutic targets in cancer.
Review in Biochemical pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
21 citing papers in PubMed, 41 citations in OpenAlex.
- Identification of a novel PAK1 inhibitor to treat pancreatic cancer.Acta pharmaceutica Sinica. B · 2020Article
- PAK1 silencing is synthetic lethal with CDK4/6 inhibition in gastric cancer cells via regulating PDK1 expression.Human cell · 2020Article
- Solution structures and biophysical analysis of full-length group A PAKs reveal they are monomeric and auto-inhibited inThe Biochemical journal · 2019Article
- Blood Pressure Control by a Secreted FGFBP1 (Fibroblast Growth Factor-Binding Protein).Hypertension (Dallas, Tex. : 1979) · 2018Article
- Small molecules that allosterically inhibit p21-activated kinase activity by binding to the regulatory p21-binding domain.Experimental & molecular medicine · 2016Article
- Targeting Rho-GTPases in immune cell migration and inflammation.British journal of pharmacology · 2014Review
- Republished: tracing PAKs from GI inflammation to cancer.Postgraduate medical journal · 2014Article
- P21-activated kinase in inflammatory and cardiovascular disease.Cellular signalling · 2014Review
- PAK1: A Therapeutic Target for Cancer Treatment.ACS medicinal chemistry letters · 2013Article
- Synergistic activation of p21-activated kinase 1 by phosphatidylinositol 4,5-bisphosphate and Rho GTPases.The Journal of biological chemistry · 2013Article
- Development of EHop-016: a small molecule inhibitor of Rac.The Enzymes · 2013Review
- Modulation of apoptotic pathways by human papillomaviruses (HPV): mechanisms and implications for therapy.Viruses · 2012Review
- Group I p21-activated kinases (PAKs) promote tumor cell proliferation and survival through the AKT1 and Raf-MAPK pathways.Molecular cancer research : MCR · 2012Article
- Molecular pathways: targeting p21-activated kinase 1 signaling in cancer--opportunities, challenges, and limitations.Clinical cancer research : an official journal of the American Association for Cancer Research · 2012Review
- The art of filling protein pockets efficiently with octahedral metal complexes.Angewandte Chemie (International ed. in English) · 2012Article
- Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase.The Journal of biological chemistry · 2012Article
- 3D structure analysis of PAKs: A clue to the rational design for affinity reagents and blockers.Cellular logistics · 2012Article
- Small molecule inhibitors of the HPV16-E6 interaction with caspase 8.Bioorganic & medicinal chemistry letters · 2012Article
- Inhibition of p21 activated kinase (PAK) reduces airway responsiveness in vivo and in vitro in murine and human airways.PloS one · 2012Article
- Aplysqualenol A binds to the light chain of dynein type 1 (DYNLL1).Angewandte Chemie (International ed. in English) · 2011Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The p21-activated kinases (PAKs), immediate downstream effectors of the small G-proteins of the Rac/cdc42 family, are critical mediators of signaling pathways regulating cellular behaviors and as such, have been implicated in pathological conditions including cancer. Recent studies have validated the requirement for PAKs in promoting tumorigenesis in breast carcinoma and neurofibromatosis. Thus, there has been considerable interest in the development of inhibitors to the PAKs, as biological markers and leads for the development of therapeutics. While initial approaches were based on screening for competitive organic inhibitors, more recent efforts have focused on the identification of allosteric inhibitors, organometallic ATP-competitive inhibitors and the use of PAK1/inhibitor crystal structures for inhibitor optimization. This has led to the identification of highly selective and potent inhibitors, which will serve as a basis for further development of inhibitors for therapeutic applications.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.