FGFR2 kinase domain in complex with a Pyrazolo[1,5-a]pyrimidine analog (Compound 29)

Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.

FGFR-2,K-sam,KGFR,Keratinocyte growth factor receptor

MGSSHHHHHHSSGLVPRGSHMLAGVSEYELPEDPKWEFPRDKLTLGKPLGEGAFGQVVMAEAVGIDKDKPKEAVTVAVKM
LKDDATEKDLSDLVSEMEMMKMIGKHKNIINLLGACTQDGPL(PTR)VIVEYASKGNLREYLRARRPPGME(PTR)SYDI
NRVPEEQMTFKDLVSCTYQLARGMEYLASQKCIHRDLAARNVLVTENNVMKIADFGLARDINNIDYYKKTTNGRLPVKWM
APEALFDRVYTHQSDVWSFGVLMWEIFTLGGSPYPGIPVEELFKLLKEGHRMDKPANCTNELYMMMRDCWHAVPSQRPTF
KQLVEDLDRILTLTTNEE

MGSSHHHHHHSSGLVPRGSHMLAGVSEYELPEDPKWEFPRDKLTLGKPLGEGAFGQVVMAEAVGIDKDKPKEAVTVAVKM
LKDDATEKDLSDLVSEMEMMKMIGKHKNIINLLGACTQDGPLYVIVEYASKGNLREYLRARRPPGMEYSYDINRVPEEQM
TFKDLVSCTYQLARGMEYLASQKCIHRDLAARNVLVTENNVMKIADFGLARDINNIDYYKKTTNGRLPVKWMAPEALFDR
VYTHQSDVWSFGVLMWEIFTLGGSPYPGIPVEELFKLLKEGHRMDKPANCTNELYMMMRDCWHAVPSQRPTFKQLVEDLD
RILTLTTNEE

0.1 M Sodium citrate pH 5.2; 28% w/w PEG 4,000; 0.2 M Ammonium acetate

FGFR, inhibitor, kinase, gatekeeper, hyperphosphatemia, STRUCTURAL PROTEIN

(chain 'A' and (resid 468 through 484 or (resid 485 and (name N or name CA or name C or name O or name CB )) or resid 486 through 493 or (resid 494 and (name N or name CA or name C or name O or name CB )) or resid 495 through 511 or (resid 512 and (name N or name CA or name C or name O or name CB )) or resid 513 through 521 or resid 523 through 592 or (resid 596 through 597 and (name N or name CA or name C or name O or name CB )) or resid 598 through 651 or (resid 657 through 661 and (name N or name CA or name C or name O or name CB )) or resid 662 through 682 or (resid 683 and (name N or name CA or name C or name O or name CB )) or resid 684 through 709 or (resid 710 through 711 and (name N or name CA or name C or name O or name CB )) or resid 712 through 716 or (resid 717 and (name N or name CA or name C or name O or name CB )) or resid 718 through 719 or (resid 720 and (name N or name CA or name C or name O or name CB )) or resid 721 through 755 or (resid 756 and (name N or name CA or name C or name O or name CB )) or resid 757 through 762))

(chain 'B' and (resid 468 through 469 or (resid 470 and (name N or name CA or name C or name O or name CB )) or resid 471 through 472 or (resid 473 and (name N or name CA or name C or name O or name CB )) or resid 474 through 504 or (resid 505 through 507 and (name N or name CA or name C or name O or name CB )) or resid 508 through 509 or (resid 510 through 512 and (name N or name CA or name C or name O or name CB )) or resid 513 through 555 or (resid 556 and (name N or name CA or name C or name O or name CB )) or resid 557 through 587 or (resid 588 through 589 and (name N or name CA or name C or name O or name CB )) or resid 590 through 620 or (resid 621 and (name N or name CA or name C or name O or name CB )) or resid 622 through 651 or resid 657 through 714 or (resid 715 and (name N or name CA or name C or name O or name CB )) or resid 716 through 762))

MLAGVSEYELPEDPKWEFPRDKLTLGKPLGEGCFGQVVMAEAVGIDKDKPKEAVTVAVKMLKDDATEKDLSDLVSEMEMM
KMIGKHKNIINLLGACTQDGPLYVIVEYASKGNLREYLRARRPPGMEYSYDINRVPEEQMTFKDLVSCTYQLARGMEYLA
SQKCIHRDLAARNVLVTENNVMKIADFGLARDINNIDYYKKTTNGRLPVKWMAPEALFDRVYTHQSDVWSFGVLMWEIFT
LGGSPYPGIPVEELFKLLKEGHRMDKPANCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRILTLTTNEE