General Information of This Target
Target ID
PATR0KSWDD
Target Name
3-Phosphoinositide-dependent protein kinase 1 (PDPK1)
Gene Name
PDPK1
Gene ID
5170
Synonym
PDK1
Sequence
MARTTSQLYDAVPIQSSVVLCSCPSPSMVRTQTESSTPPGIPGGSRQGPAMDGTAAEPRP
GAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIK
ENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDET
CTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARAN
SFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYD
FPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLTA
YLPAMSEDDEDCYGNYDNLLSQFGCMQVSSSSSSHSLSASDTGLPQRSGSNIEQYIHDLD
SNSFELDLQFSEDEKRLLLEKQAGGNPWHQFVENNLILKMGPVDKRKGLFARRRQLLLTE
GPHLYYVDPVNKVLKGEIPWSQELRPEAKNFKTFFVHTPNRTYYLMDPSGNAHKWCRKIQ
EVWRQRYQSHPDAAVQ

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Family
the AGC Ser/Thr protein kinase family
Function
Serine/threonine kinase which acts as a master kinasephosphorylating and activating a subgroup of the AGC family of protein kinases. Its targets include: protein kinase B (PKB/AKT1PKB/AKT2PKB/AKT3)p70 ribosomal protein S6 kinase (RPS6KB1)p90 ribosomal protein S6 kinase (RPS6KA1RPS6KA2 and RPS6KA3)cyclic AMP-dependent protein kinase (PRKACA)protein kinase C (PRKCD and PRKCZ)serum and glucocorticoid-inducible kinase (SGK1SGK2 and SGK3)p21-activated kinase-1 (PAK1)protein kinase PKN (PKN1 and PKN2). Plays a central role in the transduction of signals from insulin by providing the activating phosphorylation to PKB/AKT1thus propagating the signal to downstream targets controlling cell proliferation and survivalas well as glucose and amino acid uptake and storage. Negatively regulates the TGF-beta-induced signaling by: modulating the association of SMAD3 and SMAD7 with TGF-beta receptorphosphorylating SMAD2SMAD3SMAD4 and SMAD7preventing the nuclear translocation of SMAD3 and SMAD4 and the translocation of SMAD7 from the nucleus to the cytoplasm in response to TGF-beta. Activates PPARG transcriptional activity and promotes adipocyte differentiation. Activates the NF-kappa-B pathway via phosphorylation of IKKB. The tyrosine phosphorylated form is crucial for the regulation of focal adhesions by angiotensin II. Controls proliferationsurvivaland growth of developing pancreatic cells. Participates in the regulation of Ca(2+) entry and Ca(2+)-activated K(+) channels of mast cells. Essential for the motility of vascular endothelial cells (ECs) and is involved in the regulation of their chemotaxis. Plays a critical role in cardiac homeostasis by serving as a dual effector for cell survival and beta-adrenergic response. Plays an important role during thymocyte development by regulating the expression of key nutrient receptors on the surface of pre-T cells and mediating Notch-induced cell growth and proliferative responses. Provides negative feedback inhibition to toll-like receptor-mediated NF-kappa-B activation in macrophages. Isoform 3 is catalytically inactive.

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Uniprot Entry
PDPK1_HUMAN
HGNC ID
HGNC:8816
KEGG ID
hsa:5170
Full List of The ADC Related to This Target
Investigative
Click To Hide/Show 4 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
Neolymphostin ADC 21
Trastuzumab A114C
ERBB2
Neolymphostin A
Mc-Val-Cit-PABC-DMEA
[1]
Neolymphostin ADC 22
Trastuzumab A114C
ERBB2
Neolymphostin A
PEG4-DMEA
[1]
Neolymphostin ADC 23
Trastuzumab A114C
ERBB2
Neolymphostin A
Mc-Val-Cit-PABC
[1]
Neolymphostin ADC 24
Trastuzumab A114C
ERBB2
Neolymphostin A
N-Methoxycarbonylmaleimide
[1]
References
Ref 1 Novel PIKK inhibitor antibody-drug conjugates: Synthesis and anti-tumor activity. Bioorg Med Chem Lett. 2019 Apr 1;29(7):943-947. doi: 10.1016/j.bmcl.2019.01.009. Epub 2019 Jan 11.

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