Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T95913
|
||||
Former ID |
TTDR00356
|
||||
Target Name |
Phosphoinositide 3 kinase
|
||||
Gene Name |
PIK3CG
|
||||
Synonyms |
PI 3-kinase; PI3K; Phosphoinositol-3 kinase; PI3-kinase p110 subunit gamma; PI3K; PI3Kgamma; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, gamma isoform; Phosphoinositide 3-Kinase gamma; PtdIns-3-kinase p110; PIK3CG
|
||||
Target Type |
Successful
|
||||
Disease | Arthritis [ICD9: 710-719; ICD10: M00-M25] | ||||
Advanced solid tumor; Non-hodgkin's lymphoma [ICD9: 140-199, 200, 202, 202.8, 210-229; ICD10: C00-C75, C7A, C7B, C81-C86, C82-C85, D10-D36, D3A] | |||||
Angioedema; Myocardial infarction [ICD9: 277.6, 410, 995.1; ICD10: D84.1, I21, I22, T78.3] | |||||
Advanced solid tumor [ICD9: 140-199; ICD10: C00-C75, C7A, C7B] | |||||
Breast cancer [ICD9: 174, 175; ICD10: C50] | |||||
Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99] | |||||
Cardiovascular disorder [ICD10: I00-I99] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Diffuse large B-cell lymphoma [ICD9: 200; ICD10: C83.3] | |||||
Enthesopathy; Type 2 diabetes [ICD9:726, 250; ICD10: M76-M77.9, E11] | |||||
Endometrial cancer [ICD9: 182; ICD10: C54.1] | |||||
Glioma [ICD9: 191; ICD10: C71] | |||||
Hematologic malignancies [ICD9: 200-209; ICD10: C81-C86] | |||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86] | |||||
Metastatic breast cancer; Endometrial cancer; Lymphoma [ICD9: 140-199, 140-229, 174, 175, 182.0, 202.8, 210-229; ICD10: C50, C81-C86] | |||||
Non-hodgkin's lymphoma [ICD10: C85] | |||||
Prostate cancer [ICD9: 185; ICD10: C61] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Type 2 diabetes [ICD9: 250; ICD10: E11] | |||||
Function |
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4- phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5- bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Participates in cellular signaling in response to various growth factors. Involved in the activation of AKT1 upon stimulation by receptor tyrosine kinases ligands such as EGF, insulin, IGF1, VEGFA and PDGF. Involved in signaling via insulin-receptor substrate (IRS) proteins. Essential in endothelial cell migration during vascular development through VEGFA signaling, possibly by regulating RhoA activity. Required for lymphatic vasculature development, possibly by binding to RAS and by activation by EGF and FGF2, but not by PDGF. Regulates invadopodia formation in breast cancer cells through the PDPK1- AKT1 pathway. Participates in cardiomyogenesis in embryonic stem cells through a AKT1 pathway. Participates in vasculogenesis in embryonic stem cells through PDK1 and protein kinase C pathway. Has also serine-protein kinase activity: phosphorylates PIK3R1 (p85alpha regulatory subunit), EIF4EBP1 and HRAS.
|
||||
BioChemical Class |
Kinase
|
||||
Target Validation |
T17917
|
||||
UniProt ID | |||||
EC Number |
EC 2.7.11.1
|
||||
Sequence |
MELENYKQPVVLREDNCRRRRRMKPRSAAASLSSMELIPIEFVLPTSQRKCKSPETALLH
VAGHGNVEQMKAQVWLRALETSVAADFYHRLGPHHFLLLYQKKGQWYEIYDKYQVVQTLD CLRYWKATHRSPGQIHLVQRHPPSEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGL VTPRMAEVASRDPKLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDT PGAILQSFFTKMAKKKSLMDIPESQSEQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNG EEIHVVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRK FRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFTEEVLWNVWLEFSIKI KDLPKGALLNLQIYCGKAPALSSKASAESPSSESKGKVQLLYYVNLLLIDHRFLLRRGEY VLHMWQISGKGEDQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHQPTPDPEG DRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQ QEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYL LQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAY LRGCGTAMLHDFTQQVQVIEMLQKVTLDIKSLSAEKYDVSSQVISQLKQKLENLQNSQLP ESFRVPYDPGLKAGALAIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQ DMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTVGNTG AFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMITETGNL FHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGTSGKKTSPHFQKFQDICVKAYLAL RHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKNEEDAKKYFLDQIEVCRDKGW TVQFNWFLHLVLGIKQGEKHSA |
||||
Structure |
1E8Y; 1E8Z; 1HE8; 2A4Z; 2A5U; 2CHW; 2CHX; 2CHZ; 2V4L; 3APC; 3APD; 3APF; 3CSF; 3CST; 3DBS; 3DPD; 3ENE; 3IBE; 3L08; 3L13; 3L16; 3L17; 3L54; 3LJ3; 3MJW; 3ML8; 3ML9; 3NZS; 3NZU; 3OAW; 3P2B; 3PRE; 3PRZ; 3PS6; 3QAQ; 3QAR; 3QJZ; 3QK0; 3R7Q; 3R7R; 3S2A; 3SD5; 3T8M; 3TJP; 3TL5; 3ZVV; 3ZW3; 4ANU; 4ANV; 4ANW; 4ANX; 4AOF; 4DK5; 4EZJ; 4EZK; 4EZL; 4F1S; 4FA6; 4FAD; 4FHJ; 4FHK; 4FJY; 4FJZ; 4FLH; 4FUL; 4G11; 4GB9; 4HLE; 4HVB; 4J6I; 4KZ0; 4KZC; 4PS3; 4PS7; 4PS8; 4URK; 4WWN; 4WWO; 4WWP; 2ENQ; 2RD0; 3HHM; 3HIZ; 3ZIM; 4JPS; 4L1B; 4L23; 4L2Y; 4OVU; 4OVV; 4TUU; 4TV3; 4WAF
|
||||
Drugs and Mode of Action | |||||
Drug(s) | CHU | Drug Info | Registered | Enthesopathy; Type 2 diabetes | [548663] |
BAY 80-6946 | Drug Info | Phase 3 | Non-hodgkin's lymphoma | [542801], [549051] | |
Buparlisib | Drug Info | Phase 3 | Breast cancer | [523929], [542804] | |
IPI-145 | Drug Info | Phase 3 | Arthritis | [532543], [542746] | |
Rigosertib | Drug Info | Phase 3 | Solid tumours | [532659], [542777] | |
BEZ235 | Drug Info | Phase 2 | Solid tumours | [542866], [548508] | |
CLR-1404 | Drug Info | Phase 2 | Cancer | [524202] | |
GDC0941 | Drug Info | Phase 2 | Advanced solid tumor; Non-hodgkin's lymphoma | [541027], [548661] | |
PF-04691502 | Drug Info | Phase 2 | Endometrial cancer | [523615], [542851] | |
PF-05212384 | Drug Info | Phase 2 | Cancer | [533132], [542855] | |
PX-866 | Drug Info | Phase 2 | Cancer | [523422], [542856] | |
SAR245409 | Drug Info | Phase 2 | Cancer | [524422] | |
XL147 | Drug Info | Phase 2 | Cancer | [533087], [542879] | |
BGT226 | Drug Info | Phase 1/2 | Solid tumours | [531639], [542867] | |
CLR-1401 | Drug Info | Phase 1/2 | Cancer | [523773] | |
CLR457 | Drug Info | Phase 1/2 | Advanced solid tumor | [524832] | |
TG100-115 | Drug Info | Phase 1/2 | Angioedema; Myocardial infarction | [536497], [541054] | |
CH-5132799 | Drug Info | Phase 1 | Solid tumours | [531469], [542708] | |
CUDC-907 | Drug Info | Phase 1 | Diffuse large B-cell lymphoma | [550573] | |
DS-7423 | Drug Info | Phase 1 | Solid tumours | [549261] | |
GDC-0980 | Drug Info | Phase 1 | Advanced solid tumor; Non-hodgkin's lymphoma | [550796] | |
GSK2126458 | Drug Info | Phase 1 | Lymphoma | [533074] | |
P-7170 | Drug Info | Phase 1 | Cancer | [524177] | |
PA-799 | Drug Info | Phase 1 | Solid tumours | [549160] | |
Perifosine | Drug Info | Phase 1 | Solid tumours | [521489], [542448] | |
PQR309 | Drug Info | Phase 1 | Pain | [543099] | |
SAR245408 + MSC1936369B | Drug Info | Phase 1 | Solid tumours | [523487] | |
SAR245409/MSC1936369B combination therapy | Drug Info | Phase 1 | Solid tumours | [523487] | |
SF1126 | Drug Info | Phase 1 | Solid tumours | [548503] | |
VS-5584 | Drug Info | Phase 1 | Solid tumours | [532167], [543098] | |
ZSTK474 | Drug Info | Phase 1 | Cancer | [532539], [542881] | |
Adyvia | Drug Info | Discontinued in Phase 2 | Type 2 diabetes | [547734] | |
GDC-0084 | Drug Info | Discontinued in Phase 1 | Glioma | [549369] | |
GSK1059615 | Drug Info | Discontinued in Phase 1 | Metastatic breast cancer; Endometrial cancer; Lymphoma | [548760] | |
LY294002 | Drug Info | Terminated | Cancer | [541270], [546293] | |
PX-867 | Drug Info | Terminated | Cardiovascular disorder | [548762] | |
SCR-44001 | Drug Info | Terminated | Cancer | [548121] | |
Wortmannin | Drug Info | Terminated | Hematologic malignancies | [541309], [546241] | |
Inhibitor | 2-(4-Morpholinyl)-8-Phenyl-4h-1-Benzopyran-4-One | Drug Info | [551393] | ||
3-(4-morpholinothieno[3,2-d]pyrimidin-2-yl)phenol | Drug Info | [528931] | |||
5-QUINOXALIN-6-YLMETHYLENE-THIAZOLIDINE-2,4-DIONE | Drug Info | [551374] | |||
AEZS-126 | Drug Info | [543561] | |||
AS-604850 | Drug Info | [527706] | |||
BAG956 | Drug Info | [537458] | |||
Buparlisib | Drug Info | [537633] | |||
CH-5132799 | Drug Info | [531469] | |||
CHU | Drug Info | [543562] | |||
CLR-1401 | Drug Info | [543561] | |||
CLR-1404 | Drug Info | [543561] | |||
CU-906 | Drug Info | [543561] | |||
CZC 24832 | Drug Info | [531889] | |||
CZC-19091 | Drug Info | [543562] | |||
Dual PI3K/mTOR inhibitors | Drug Info | [543561] | |||
GDC-0084 | Drug Info | [544240] | |||
GDC0941 | Drug Info | [537458], [537633] | |||
GSK1059615 | Drug Info | [537633] | |||
Her2- and PSA-targeted TGX-D1 | Drug Info | [531442] | |||
HM-5016699 | Drug Info | [543561] | |||
HS-173 | Drug Info | [531383] | |||
KU-0060648 | Drug Info | [532428] | |||
LOR-220 | Drug Info | [543561] | |||
LY-292223 | Drug Info | [526022] | |||
LY-293646 | Drug Info | [526022] | |||
LY294002 | Drug Info | [550797] | |||
Multiform PI3K inhibitors | Drug Info | [543561] | |||
Myricetin | Drug Info | [551393] | |||
P-6915 | Drug Info | [543561] | |||
P-7170 | Drug Info | [543561] | |||
PF-03772304 | Drug Info | [532819] | |||
PF-4989216 | Drug Info | [543561] | |||
PI-103 | Drug Info | [537458] | |||
PI-3065 | Drug Info | [532839] | |||
PIK-75 | Drug Info | [528931] | |||
PKI-402 | Drug Info | [530561] | |||
PP121 | Drug Info | [529744] | |||
PQR309 | Drug Info | [543561] | |||
PX-866 | Drug Info | [537633] | |||
SAR245408 + MSC1936369B | Drug Info | [543562] | |||
SAR245409 | Drug Info | [551615] | |||
SAR245409/MSC1936369B combination therapy | Drug Info | [543562] | |||
SCR-44001 | Drug Info | [531187] | |||
TG100-115 | Drug Info | [536301], [536380], [536962] | |||
TGX-221 | Drug Info | [527515] | |||
VE-822 | Drug Info | [532144] | |||
Wortmannin | Drug Info | [535473], [535536], [537458] | |||
WX-037 | Drug Info | [543561] | |||
Modulator | Adyvia | Drug Info | |||
BAY 80-6946 | Drug Info | ||||
BEZ235 | Drug Info | ||||
BGT226 | Drug Info | [531639] | |||
CLR457 | Drug Info | [1572591] | |||
CUDC-907 | Drug Info | ||||
DS-7423 | Drug Info | [532664] | |||
GDC-0980 | Drug Info | [531658] | |||
GSK2126458 | Drug Info | ||||
IPI-145 | Drug Info | [532543] | |||
PA-799 | Drug Info | ||||
Perifosine | Drug Info | ||||
PF-04691502 | Drug Info | ||||
PF-05212384 | Drug Info | [533132] | |||
PX-867 | Drug Info | [532491] | |||
Rigosertib | Drug Info | [532659] | |||
SF1126 | Drug Info | ||||
VS-5584 | Drug Info | [532167] | |||
XL147 | Drug Info | ||||
ZSTK474 | Drug Info | [532539] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Inositol phosphate metabolism | ||||
ErbB signaling pathway | |||||
Ras signaling pathway | |||||
Rap1 signaling pathway | |||||
cGMP-PKG signaling pathway | |||||
cAMP signaling pathway | |||||
Chemokine signaling pathway | |||||
HIF-1 signaling pathway | |||||
FoxO signaling pathway | |||||
Phosphatidylinositol signaling system | |||||
Sphingolipid signaling pathway | |||||
mTOR signaling pathway | |||||
PI3K-Akt signaling pathway | |||||
AMPK signaling pathway | |||||
Apoptosis | |||||
Adrenergic signaling in cardiomyocytes | |||||
VEGF signaling pathway | |||||
Osteoclast differentiation | |||||
Focal adhesion | |||||
Signaling pathways regulating pluripotency of stem cells | |||||
Platelet activation | |||||
Toll-like receptor signaling pathway | |||||
Jak-STAT signaling pathway | |||||
Natural killer cell mediated cytotoxicity | |||||
T cell receptor signaling pathway | |||||
B cell receptor signaling pathway | |||||
Fc epsilon RI signaling pathway | |||||
Fc gamma R-mediated phagocytosis | |||||
TNF signaling pathway | |||||
Leukocyte transendothelial migration | |||||
Neurotrophin signaling pathway | |||||
Cholinergic synapse | |||||
Inflammatory mediator regulation of TRP channels | |||||
Regulation of actin cytoskeleton | |||||
Insulin signaling pathway | |||||
Progesterone-mediated oocyte maturation | |||||
Estrogen signaling pathway | |||||
Prolactin signaling pathway | |||||
Thyroid hormone signaling pathway | |||||
Oxytocin signaling pathway | |||||
Regulation of lipolysis in adipocytes | |||||
Type II diabetes mellitus | |||||
Non-alcoholic fatty liver disease (NAFLD) | |||||
Aldosterone-regulated sodium reabsorption | |||||
Carbohydrate digestion and absorption | |||||
Bacterial invasion of epithelial cells | |||||
Chagas disease (American trypanosomiasis) | |||||
Toxoplasmosis | |||||
Amoebiasis | |||||
Hepatitis C | |||||
Hepatitis B | |||||
Measles | |||||
Influenza A | |||||
HTLV-I infection | |||||
Epstein-Barr virus infection | |||||
Pathways in cancer | |||||
Viral carcinogenesis | |||||
Proteoglycans in cancer | |||||
MicroRNAs in cancer | |||||
Colorectal cancer | |||||
Renal cell carcinoma | |||||
Pancreatic cancer | |||||
Endometrial cancer | |||||
Glioma | |||||
Prostate cancer | |||||
Melanoma | |||||
Chronic myeloid leukemia | |||||
Acute myeloid leukemia | |||||
Small cell lung cancer | |||||
Non-small cell lung cancer | |||||
Central carbon metabolism in cancer | |||||
Choline metabolism in cancer | |||||
PathWhiz Pathway | Inositol Metabolism | ||||
Phosphatidylinositol Phosphate Metabolism | |||||
Intracellular Signalling Through Adenosine Receptor A2a and Adenosine | |||||
Intracellular Signalling Through Adenosine Receptor A2b and Adenosine | |||||
Fc Epsilon Receptor I Signaling in Mast Cells | |||||
Reactome | PI3K Cascade | ||||
GPVI-mediated activation cascade | |||||
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants | |||||
PI3K events in ERBB4 signaling | |||||
PIP3 activates AKT signaling | |||||
GAB1 signalosome | |||||
PI3K events in ERBB2 signaling | |||||
PI3K/AKT activation | |||||
Role of phospholipids in phagocytosis | |||||
Tie2 Signaling | |||||
Constitutive Signaling by Aberrant PI3K in Cancer | |||||
DAP12 signaling | |||||
Role of LAT2/NTAL/LAB on calcium mobilization | |||||
Nephrin interactions | |||||
Costimulation by the CD28 family | |||||
CD28 dependent PI3K/Akt signaling | |||||
gamma signalling through PI3Kgamma | |||||
G alpha (q) signalling events | |||||
G alpha (12/13) signalling events | |||||
VEGFA-VEGFR2 Pathway | |||||
Interleukin-3, 5 and GM-CSF signaling | |||||
Constitutive Signaling by EGFRvIII | |||||
FGFR1 | |||||
FGFR2 | |||||
FGFR3 | |||||
FGFR4 | |||||
Interleukin receptor SHC signaling | |||||
Regulation of signaling by CBL | |||||
WikiPathways | Toll-like receptor signaling pathway | ||||
Serotonin HTR1 Group and FOS Pathway | |||||
DNA Damage Response (only ATM dependent) | |||||
G13 Signaling Pathway | |||||
Regulation of Actin Cytoskeleton | |||||
Insulin Signaling | |||||
IL-4 Signaling Pathway | |||||
Copper homeostasis | |||||
Signaling of Hepatocyte Growth Factor Receptor | |||||
Transcriptional activation by NRF2 | |||||
IL1 and megakaryotyces in obesity | |||||
Signaling by ERBB4 | |||||
Signaling by ERBB2 | |||||
Fc epsilon receptor (FCERI) signaling | |||||
PI Metabolism | |||||
Interleukin-2 signaling | |||||
Fcgamma receptor (FCGR) dependent phagocytosis | |||||
Signaling by SCF-KIT | |||||
DAP12 interactions | |||||
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R) | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
PIP3 activates AKT signaling | |||||
Integrated Pancreatic Cancer Pathway | |||||
Prostate Cancer | |||||
Signaling Pathways in Glioblastoma | |||||
TSLP Signaling Pathway | |||||
Regulation of Microtubule Cytoskeleton | |||||
TSH signaling pathway | |||||
SREBP signalling | |||||
TCR signaling | |||||
Signaling by PDGF | |||||
Signaling by Insulin receptor | |||||
Signaling by FGFR | |||||
Signaling by EGFR | |||||
NGF signalling via TRKA from the plasma membrane | |||||
Nephrin interactions | |||||
Interleukin-3, 5 and GM-CSF signaling | |||||
GPVI-mediated activation cascade | |||||
GPCR downstream signaling | |||||
Costimulation by the CD28 family | |||||
Cell surface interactions at the vascular wall | |||||
MicroRNAs in cardiomyocyte hypertrophy | |||||
Angiogenesis | |||||
Regulation of toll-like receptor signaling pathway | |||||
AMPK Signaling | |||||
References | |||||
Ref 521489 | ClinicalTrials.gov (NCT00019656) Perifosine in Treating Patients With Refractory Solid Tumors or Hematologic Cancer. U.S. National Institutes of Health. | ||||
Ref 523422 | ClinicalTrials.gov (NCT01331083) A Phase II Study of PX-866 in Patients With Recurrent or Metastatic Castration Resistant Prostate Cancer. U.S. National Institutes of Health. | ||||
Ref 523487 | ClinicalTrials.gov (NCT01357330) Oral SAR245408 (XL147) and Oral MSC1936369B in Patients With Locally Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 523615 | ClinicalTrials.gov (NCT01430585) Pre-Operative Study of PF-4691502 With Letrozole Compared To Letrozole Alone In Patients With Early Breast Cancer. U.S. National Institutes of Health. | ||||
Ref 523773 | ClinicalTrials.gov (NCT01516905) PET/CT Imaging of Malignant Brain Tumors With a Novel Radioiodinated Phospholipid Ether Analogue 124I-NM404. U.S. National Institutes of Health. | ||||
Ref 523929 | ClinicalTrials.gov (NCT01610284) Phase III Study of BKM120/Placebo With Fulvestrant in Postmenopausal Patients With Hormone Receptor Positive HER2-negative Locally Advanced or Metastatic Breast Cancer Refractory to Aromatase Inhibitor. U.S. National Institutes of Health. | ||||
Ref 524177 | ClinicalTrials.gov (NCT01762410) Clinical Study of Oral PI3K/mTOR Inhibitor in Patients With Advanced Refractory Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 524202 | ClinicalTrials.gov (NCT01778088) Open-Label Study of I-131-CLR1404 in Subjects With Recurrent Glioma. U.S. National Institutes of Health. | ||||
Ref 524422 | ClinicalTrials.gov (NCT01936363) Trial of Pimasertib With SAR245409 or Placebo in Ovarian Cancer. U.S. National Institutes of Health. | ||||
Ref 524832 | ClinicalTrials.gov (NCT02189174) Study of CLR457 Administered Orally in Adult Patients With Advanced Solid Malignancies. U.S. National Institutes of Health. | ||||
Ref 531469 | The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81. | ||||
Ref 531639 | Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8. | ||||
Ref 532167 | VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013 Feb;12(2):151-61. | ||||
Ref 532539 | Combination of the PI3K inhibitor ZSTK474 with a PSMA-targeted immunotoxin accelerates apoptosis and regression of prostate cancer. Neoplasia. 2013 Oct;15(10):1172-83. | ||||
Ref 532543 | PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74. | ||||
Ref 532659 | Phase I study of oral rigosertib (ON 01910.Na), a dual inhibitor of the PI3K and Plk1 pathways, in adult patients with advanced solid malignancies. Clin Cancer Res. 2014 Mar 15;20(6):1656-65. | ||||
Ref 533074 | Dual PI3K/mTOR inhibitors, GSK2126458 and PKI-587, suppress tumor progression and increase radiosensitivity in nasopharyngeal carcinoma. Mol Cancer Ther. 2015 Feb;14(2):429-39. | ||||
Ref 533087 | Phase II study of the PI3K inhibitor pilaralisib (SAR245408; XL147) in patients with advanced or recurrent endometrial carcinoma. Gynecol Oncol. 2015 Feb;136(2):246-53. | ||||
Ref 533132 | First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer. Clin Cancer Res. 2015 Apr 15;21(8):1888-95. | ||||
Ref 536497 | Pharmacologic therapeutics for cardiac reperfusion injury. Expert Opin Emerg Drugs. 2007 Sep;12(3):367-88. | ||||
Ref 541027 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5682). | ||||
Ref 541054 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5715). | ||||
Ref 541270 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6004). | ||||
Ref 541309 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6060). | ||||
Ref 542448 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7424). | ||||
Ref 542708 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7743). | ||||
Ref 542746 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7795). | ||||
Ref 542777 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7833). | ||||
Ref 542801 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7875). | ||||
Ref 542804 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7878). | ||||
Ref 542851 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7936). | ||||
Ref 542855 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7940). | ||||
Ref 542856 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7941). | ||||
Ref 542866 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7950). | ||||
Ref 542867 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7951). | ||||
Ref 542879 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7963). | ||||
Ref 542881 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7965). | ||||
Ref 543098 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8382). | ||||
Ref 543099 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8383). | ||||
Ref 546241 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007058) | ||||
Ref 546293 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007287) | ||||
Ref 547734 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018893) | ||||
Ref 548121 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022134) | ||||
Ref 548503 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026065) | ||||
Ref 548508 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026094) | ||||
Ref 548661 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027517) | ||||
Ref 548663 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027532) | ||||
Ref 548760 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028447) | ||||
Ref 548762 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028453) | ||||
Ref 549051 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031792) | ||||
Ref 549160 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033063) | ||||
Ref 549261 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034336) | ||||
Ref 526022 | Bioorg Med Chem Lett. 2001 Apr 9;11(7):909-13.LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family. | ||||
Ref 527515 | PI 3-kinase p110beta: a new target for antithrombotic therapy. Nat Med. 2005 May;11(5):507-14. Epub 2005 Apr 17. | ||||
Ref 527706 | Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43. Epub 2005 Aug 28. | ||||
Ref 528931 | Bioorg Med Chem. 2007 Sep 1;15(17):5837-44. Epub 2007 Jun 6.Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. | ||||
Ref 529744 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. | ||||
Ref 530561 | J Med Chem. 2010 Jan 28;53(2):798-810.Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402. | ||||
Ref 531187 | Early detection of response to experimental chemotherapeutic Top216 with [18F]FLT and [18F]FDG PET in human ovary cancer xenografts in mice. PLoS One. 2010 Sep 24;5(9):e12965. | ||||
Ref 531383 | Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis. J Med Chem. 2011 Apr 14;54(7):2455-66. | ||||
Ref 531442 | Development of a peptide-drug conjugate for prostate cancer therapy. Mol Pharm. 2011 Jun 6;8(3):901-12. | ||||
Ref 531469 | The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81. | ||||
Ref 531639 | Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8. | ||||
Ref 531658 | GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther. 2011 Dec;10(12):2426-36. | ||||
Ref 531889 | A selective inhibitor reveals PI3Kgamma dependence of T(H)17 cell differentiation. Nat Chem Biol. 2012 Apr 29;8(6):576-82. | ||||
Ref 532144 | Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation. Cell Death Dis. 2012 Dec 6;3:e441. | ||||
Ref 532167 | VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013 Feb;12(2):151-61. | ||||
Ref 532428 | 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem. 2013 Aug 22;56(16):6386-401. | ||||
Ref 532491 | Pharmacologic profiling of phosphoinositide 3-kinase inhibitors as mitigators of ionizing radiation-induced cell death. J Pharmacol Exp Ther. 2013 Dec;347(3):669-80. | ||||
Ref 532539 | Combination of the PI3K inhibitor ZSTK474 with a PSMA-targeted immunotoxin accelerates apoptosis and regression of prostate cancer. Neoplasia. 2013 Oct;15(10):1172-83. | ||||
Ref 532543 | PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74. | ||||
Ref 532659 | Phase I study of oral rigosertib (ON 01910.Na), a dual inhibitor of the PI3K and Plk1 pathways, in adult patients with advanced solid malignancies. Clin Cancer Res. 2014 Mar 15;20(6):1656-65. | ||||
Ref 532664 | Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220. | ||||
Ref 532819 | Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. ACS Med Chem Lett. 2012 Nov 7;4(1):91-7. | ||||
Ref 532839 | Inactivation of PI(3)K p110delta breaks regulatory T-cell-mediated immune tolerance to cancer. Nature. 2014 Jun 19;510(7505):407-11. | ||||
Ref 533132 | First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer. Clin Cancer Res. 2015 Apr 15;21(8):1888-95. | ||||
Ref 535473 | Estrogen regulation of c-fos gene expression through phosphatidylinositol-3-kinase-dependent activation of serum response factor in MCF-7 breast cancer cells. Biochem Biophys Res Commun. 2002 Jun 7;294(2):384-94. | ||||
Ref 535536 | Phosphatidylinositol 3-kinase/Akt signaling in the response of vascular endothelium to ionizing radiation. Cancer Res. 2002 Aug 15;62(16):4671-7. | ||||
Ref 536301 | PI3Kgamma inhibition: towards an 'aspirin of the 21st century'? Nat Rev Drug Discov. 2006 Nov;5(11):903-18. Epub 2006 Oct 13. | ||||
Ref 536380 | Isoform-selective PI3K inhibitors as novel therapeutics for the treatment of acute myocardial infarction. Biochem Soc Trans. 2007 Apr;35(Pt 2):204-6. | ||||
Ref 536962 | Aerosolized phosphoinositide 3-kinase gamma/delta inhibitor TG100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease. J Pharmacol Exp Ther. 2009 Mar;328(3):758-65. Epub 2008 Dec 4. | ||||
Ref 537458 | The PI3K/Akt pathway as a target in the treatment of hematologic malignancies. Anticancer Agents Med Chem. 2009 Jun;9(5):550-9. | ||||
Ref 537633 | Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44. | ||||
Ref 543561 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2155). | ||||
Ref 543562 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2156). | ||||
Ref 544240 | Current clinical development of PI3K pathway inhibitors in glioblastoma. Neuro Oncol. 2012 July; 14(7): 819-829. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.