Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome

…, CM Sun, MK Vallone, TM Woo, CJ Molineaux… - Cancer research, 2007 - AACR
Clinical studies with bortezomib have validated the proteasome as a therapeutic target for
the treatment of multiple myeloma and non-Hodgkin's lymphoma. However, significant …

A phase 1 dose escalation study of the safety and pharmacokinetics of the novel proteasome inhibitor carfilzomib (PR-171) in patients with hematologic malignancies

…, AK Stewart, M Vallone, CJ Molineaux… - Clinical Cancer …, 2009 - AACR
Purpose: Carfilzomib (formerly PR-171) is a novel proteasome inhibitor of the epoxyketone
class that is selective and structurally distinct from bortezomib. Proteasome inhibition by …

Pharmacokinetics, pharmacodynamics, metabolism, distribution, and excretion of carfilzomib in rats

…, H Wong, MK Bennett, CJ Molineaux, CJ Kirk - Drug metabolism and …, 2011 - ASPET
Carfilzomib [(2S)-N-[(S)-1-[(S)-4-methyl-1-[(R)-2-methyloxiran-2-yl]-1-oxopentan-2-ylcarbamoyl]-2-phenylethyl]-2-[(S)-2-(2-morpholinoacetamido)-4-phenylbutanamido]-4-…

A phase I single-agent study of twice-weekly consecutive-day dosing of the proteasome inhibitor carfilzomib in patients with relapsed or refractory multiple myeloma or …

…, RL Comenzo, A Wong, LA Kunkel, CJ Molineaux… - Clinical cancer …, 2012 - AACR
Purpose: Carfilzomib is a next-generation, selective, proteasome inhibitor with clinical activity
in relapsed and/or refractory multiple myeloma. The objectives of this phase I study were to …

Development of C5a receptor antagonists. Differential loss of functional responses.

…, SJ Siciliano, G Van Riper, CJ Molineaux… - … (Baltimore, Md.: 1950 …, 1994 - journals.aai.org
C5a is a 74-amino acid glycoprotein generated on activation of the C system. The responses
evoked by C5a, both in vitro and in vivo, and its association with inflammatory diseases, …

The amino terminus of the human C5a receptor is required for high affinity C5a binding and for receptor activation by C5a but not C5a analogs.

…, G Van Riper, SJ Siciliano, CJ Molineaux… - Journal of Biological …, 1994 - ASBMB
The binding domain of the human C5a receptor consists of two distinct and physically
separable subsites. One of these sites binds the C-terminal 8 amino acids of C5a and is as yet …

Dynorphin-A-(1-8) is contained within vasopressin neurosecretory vesicles in rat pituitary

MH Whitnall, H Gainer, BM Cox, CJ Molineaux - Science, 1983 - science.org
Dynorphin-A-(1-8), an opioid peptide widely distributed in the rat central nervous system, is
present in vasopressin-containing neurosecretory cells terminating in the neural lobe of the …

Endopeptidase‐24.15 is the primary enzyme that degrades luteinizing hormone releasing hormone both in vitro and in vivo

CJ Molineaux, A Lasdun, C Michaud… - Journal of …, 1988 - Wiley Online Library
The concentration of luteinizing hormone releasing hormone (LHRH) (pGlu‐His‐Trp‐Ser‐Tyr‐Gly‐Leu‐Arg‐Pro‐Gly‐NH
2 ), which reaches the anterior pituitary via the hypothalamo‐…

Substrate-related potent inhibitors of brain metalloendopeptidase

M Orlowski, C Michaud, CJ Molineaux - Biochemistry, 1988 - ACS Publications
Revised Manuscript Received September 17, 1987 abstract: Rat brain metalloendopeptidase
(EC 3.4. 24.15) generates Leu-and Met-enkephalinfrom several larger opioid peptides and …

Increased dynorphin immunoreactivity in spinal cord after traumatic injury

AI Faden, CJ Molineaux, JG Rosenberger, TP Jacobs… - Regulatory peptides, 1985 - Elsevier
Opiate antagonists, at high doses, have been shown to improve physiological variables and
outcome after experimental spinal injury. Dynorphin appears to be unique amongst opioids …