PROTAC Targets

September 27-30, 2022

Boston Convention and Exhibition Center

Booth #336

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PROTAC Targets

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PROTAC Targets

Targeted protein degraders (TPD) are a new class of therapeutic drugs, which may solve the problem of drug targeting in a new way. Targeted protein degradation agents - including molecular gels and heterobifunctional molecules - are a rapidly developing class of drugs with potential for cancer and other diseases.

Protein degradation targeted chimeric Technology (PROTAC) uses heterobifunctional small molecular compounds to bring the target protein closer to the E3 ligase in cells, and specifically degrades the target protein by using the ubiquitin proteasome protein degradation pathway in vivo. PROTAC molecule is composed of three parts, one end is a specific E3 ligase ligand, the other end is a specific ligand of the target protein, and the middle linker, so as to form a "target protein protac-e3 ligase" ternary complex.

At present, a variety of strategies have been developed for cancer treatment, such as small molecule inhibitors, monoclonal antibodies, RNA interference and CRISPR/Cas9; Due to its unique chemical and biological characteristics, PROTAC has unique advantages and disadvantages in cancer treatment. The advantages of PROTAC include: event driven activity, targeting non pharmaceutical proteins, overcoming traditional drug resistance, etc. Disadvantages include membrane permeability, off target toxicity, etc.

From the perspective of targets, according to the latest statistics in December 2021, more than 130 PROTAC targets have been reported, and the number of degradable targets reported from 2020 to 2021 (about 90) has completely exceeded the total amount of the previous 18 years, indicating that the era of protein degradation is coming.

In the reported studies, researchers prefer to choose kinase as the target of protein degradation. According to incomplete statistics, about 54 kinases can be degraded by protein degrading agents based on PROTAC. At present, 518 kinases have been found. According to the classification of human kinase map, Creative BioMart provides the kinases that can be degraded as "degradable kinases" below. In the "degradable" kinase table, according to the classification method of kinase map, only CK1 and CaMK kinase groups have not reported related PROTAC. RTKs and CMGCS kinases have been reported to have the most degradable targets, 19 and 14, respectively, accounting for more than half of the total number of degradable kinases.

Besides the PROTAC targets, E3 ligases is also important for PROTAC. Only a relatively small number of E3 ligases out of the >600 E3 ligases encoded by human genomes have been exploited by small molecules for TPD applications.

To support PROTAC research and therapeutics, Creative BioMart provides our customers with a list of recombinant E3 proteins to effectuate TPD.

PROTAC Targets

TKL ACTR2BRAFLIMK2RIPK1ACTR2BDLKLRRK1RIPK2 ALK1ALK2ALK4ALK7HH498LRRK2RIPK3ILKLZKSgk288IRAK1MISR2TAK1IRAK2MLK1TESK1ANKRD3IRAK3MLK2TESK2ARAFIRAK4KSR1TGFBR1TGFBR2MLK3BMPR1AMLK4BMPR1BMLKLBMPR2LIMK1RAF1
CMGC CCRKCDK11CDKL4ERK1HIPK4p38γICKJNK1p38PITSLRECDK1/CDC2CDK12CDKL5ERK2CDK2CDK13CLK1ERK3CDK3CDK14CLK2ERK4JNK2PRP4CDK4CDK15CLK3ERK5JNK3SRPK1CDK5CDK16CLK4MAKERK7GSK3aGSK3bSRPK2CDK6CDK7CDK8CDK17CDK18MOKMSSK1DYRK1ADYRK1BCDKL1DYRK2HIPK1NLKCDK9CDKL2DYRK3HIPK2p38aCDK10CDKL3DYRK4HIPK3p38b
AGC MSK2LATS1NDR1AKT1GPRK7PKCgPKN3RSKL2AKT2AKT3BARK1GRK2p70S6KMAST1PKCdPKCPRKXSGK1LATS2NDR2PKCEPRKYSGK2RHODKGRK1SGK3SGK494YANK1RSK1p90RSKYANK2BARK2GRK3MAST2p70S6KbPKCnROCK1CRIKMAST3PDK1ROCK2DMPK1MAST4PKACaPKCTDMPK2MASTLPKACbPKG1RSK2YANK3GPRK4MRCKaPKACgPKG2RSK3MRCKPKCaPKN1PRK1RSK4PKN2PRK2RSKL1GPRK5GPRK6MSK1PKCb
Atypical Brd3ADCK1RIOK1ADCK2Brd4RIOK2ADCK3BrdTRIOK3ADCK4ChaK1SMG1ADCK5Chak2TIF1aAlphaK1DNAPKTIF1bAlphak2 AlphaK3MTORFRAPTRRAPATMEEF2KTIF1gPDHK1ATRPDHK2BCKDKPDHK3Brd2PDHK4
CAMK AMPKa1caMLCKLKB1NuaK2QIKSIK2Trb1ObscurinPASKTrb2Trb3AMPKa2CASKMAPKAPKK2QSKMAPKAPK3MAPKAPK5PHKY1BRSKCHK1SgK085BRSK2CHK2SgK495TrioTSSK1TSSK2CaMK1aDAPK1MARK1PHKY2SIKCaMK1bCaMK1gDAPK3PIM1PIM2skMLCKsmMLCKDAPK2MARK2MARK3TSSK3CaMK1dDCAMKL1MARK4PIM3SNRKTSSK4CaMK2aDCAMKL2MELKPKD1PKCmSPEGAPEG1VACAMKLCaMK2bDCAMKL3MNK1PKD2PKD3SSTKCaMK2gDRAK1CaMK2dDRAK2MNK2STK33NIM1PSKH1TitinTTNCaMK4HUNKNuaK1ARK5PSKH2Trad
Non-RTK ABLACKARGBLKBMXETKBRKBTKCSKCTKFAKFERFESFGRFRKFYNHCKITKJAK1JAK2JAK3LCKLYNPYK2SRCSRMSYKTECTNK1TXKTYK2YESZAP70
RTK ALKINSRAXLIRRCCK4PTK7KDRVEGFR2cSF1RFMSKITLMR1AATKDDR1DDR2EGFRLMR2LMR3EphA1EphA2LTKMEREphA3METMUSKEphA5EphA6PDGFRaPDGFRbEphA7RETRONEphA8EphA10EphB1EphB2ROR1ROR2ROSEphB3RYKSuRTK106TIE1EphB4EphB6FGFR1TIE2TEKFGFR2TRKAFGFR3TRKBFGFR4FLTVEGFR1FLT3FLT4EGFR3HER2TRKCTYRO3SKYHER4HER3IGF1R
STE ASK1MAP3K5MEK5MAP2K5MIYO3ASTLK5LYK5ASK2MAP3K6MEKK1MAP3K1MYO3BSTLK6ALS2CR2COTTPL2MEKK2MAP3K2NIKTAK1MAP3K7OSR1PAK1GCKMEKKMAP3K3TAO1HPK1MKK3MAP2K3TAO2PSKKHS1KHS2MKK4SEK1MAP2K4PAK2TAO3JIKMKK6MAP2K6PAK3YSK1SOK1ZC1HGKZC2TNIKZC3MINKLOKMKK7MAP2K7PAK4MAP3KAMST1PAK5PAK6SLKMAP3K8MST2MEK1MAP2K1MST3ZC4NRKMEK2MAP2K2MST4STLK3SPAK
CK1 CK1aCK1a2  CK1d  CK1e  CK1g1  CK1g2  CK1g3TTBK1ITBK2VRK1VRK2VRK3
Others AAK1AurAAurBAurcBIKEBMP2KBUB1BUBRICaMKK1CaMKK2CDC7CK2a1CK2a2SgK269SgK307TEX14CLIK1KISNEK9PLK4TTKCLIK1LMOSNEK10PRPKULK1SaK424SgK493RIOK2FusedMPSK1NEK11RNAseLULK2GAKMYT1NRBP1SBKULK3GCN2NEK1NRBP2SCYL1SgK496ULK4HaspinNEK2PEKPERKCCL14SlobWee1HRINEK3PIK3R4SCYL3CCL15STK31Wee1BIKKaCHUKNEK4PINK1SgK069TBCKWnk1IKKBNEK5PKRSgKO71TBK1Wnk2IKKENEK6PLK1SaK110TLK1Wnk3SgK196SgK223IREIERN1NEK7PLK2TLK2Wnk4IRE2ERN2NEK8PLK3TOPKPBK

E3 ligases

Can't find what you are looking for exactly? We can still help! Creative BioMart has focused on protein production and purification for years, and our custom-service team is capable of creating the protein that suits your experimental needs.

What else? We can also provide PROTACs services, including:

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